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T0078 Lapatinib Lapatinib is a dual inhibitor of Lapatinib is a dual ErbB2/EGFR (IC50: 9.2/10.8 nM) inhibitor
T0078L Lapatinib ditosylate monohydrate Lapatinib is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib therapy is associated with transient elevations in
T0129 Sanguinarine chloride Sanguinarine chloride, a benzophenanthridine alkaloid, stimulates apoptosis by activating the production of reactive oxygen species (ROS).
T0373 Erlotinib Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
T0373L Erlotinib hydrochloride Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
T1144L Lidocaine Hydrochloride hydrate Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.
T1656 Vandetanib Vandetanib is a potent inhibitor of VEGFR2 (IC50: 40 nM). It also inhibits VEGFR3 and EGFR.
T1737 Genistein Genistein is an isoflavonoid derived from soy products. It inhibits protein-tyrosine kinase and topoisomerase-II (DNA TOPOISOMERASES, TYPE II), with antineoplastic and antitumor ac
T1761 PD153035 hydrochloride PD153035 hydrochloride (ZM 252868; AG 1517) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, CSF-1, and Src.
T1773 Afatinib Dimaleate Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with ant
T1985 WHI-P154 WHI-P154 is a potent JAK3 inhibitor.
T2032 WHI-P180 WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
T2035 WHI-P258 WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of new therapeutics.
T2041 PD153035 PD153035 hydrochloride is an effective and selective inhibitor of EGFR (Ki/IC50: 5.2/29 pM, in cell-free assays); little inhibitory against FGFR, PGDFR, InsR, CSF-1 and Src.
T2047 AG1478 AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor.
T2055 WS3 WS3, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
T2063 AG18 AG-18 inhibits EGFR with IC50 of 35 μM.
T2106 WS6 WS6, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
T2116 AEE788 AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
T2245 CL387785 CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR(IC50: 370+/-120 pM); is able to overcome resistance caused by the T790M mutation on a functional level.
T2280 Endoxifen Z-isomer Endoxifen (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.
T2303 Afatinib Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, respectively.
T2307 Icotinib Hydrochloride Icotinib Hydrochloride is the hydrochloride salt form of icotinib, an orally available quinazoline-based inhibitor of EGFR, with potential antineoplastic activity. Icotinib selecti
T2325 Neratinib Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.
T2327 Pelitinib Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
T2364 Irbinitinib Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
T2369 Rociletinib Rociletinib is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity.
T2446 KI8751 KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
T2460 JAK 3 inhibitor IV JAK 3 inhibitor IV is a JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.
T2479 Tyrphostin 9 Tyrphostin 9 is an Agricultural acaricide, now superseded. Tyrphostin 9 is firstly designed as an EGFR inhibitor
T2483 Dacomitinib Dacomitinib(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45.7 and 73.7 nM for EG
T2490 Osimertinib Osimertinib is a small molecule tyrosine kinase receptor inhibitor and antineoplastic agent that is used in the therapy of selected forms of advanced non-small cell lung cancer (NS
T2491 AZ5104 AZ5104 is a potent EGFR inhibitor.
T2501 Canertinib dihydrochloride Canertinib dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities.
T2600 AG490 AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn, Lck, Syk, Btk, and
T2642 PD173074 PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR an
T2705 Mutant EGFR inhibitor Mutant EGFR inhibitor is a selective and potent Mutated EGFR inhibitor, inhibits L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant.
T2851 Daphnetin Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit ant
T2859 Biochanin A Biochanin A is an isoflavone derivative isolated from red clover Trifolium pratense with anticarcinogenic properties. Biochanin A is a naturally occurring fatty acid amide hydrolas
T2959 Ginsenoside Rh2 Ginsenoside Rh2, an extract of red Panax ginseng, is a potent anti-inflammatory and anticancer drug.
T2995 Chrysophanic Acid Chrysophanic acid is an EGFR/mTOR pathway inhibitor, which can be found in rhubarb, and sorrel.
T3024 Avitinib Avitinib, also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic
T3059 AP26113 AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.
T3108 CUDC101 CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively.
T3192 NS1643 NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.
T3402 Ginsenoside Rg3 Ginsenoside Rg3 possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the proliferation of human
T3506 Nazartinib Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt,
T3545 RG 13022 RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM).
T3558 EBE-A22 EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
T3621 Brigatinib Brigatinib is a highly potent and selective ALK inhibitor.
T3634 Osimertinib mesylate Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor (IC50s: 12/1 nM for EGFR(L858R) and EGFR(L858R/T790M)).
T3659 AZD3759 AZD3759 is an orally active, effective and central nervous system-penetrant EGFR inhibitor. The IC50 values were 0.2, 0.3 and 0.2 nM for EGFR L858R mutant, TK wild-type, and Exon 1
T3721 Avitinib maleate Avitinib maleate is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (EGFR) inhibitor.
T3870 Cyasterone Cyasterone, a natural EGFR inhibitor, can inhibit the growth of A549 and MGC823 cells, via regulating EGFR signaling pathway, it may be a promising anti-cancer agent. Cyasterone ha
T4014 CP724714 CP-724714 is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), >640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc.
T4183 lavendustin A lavendustin A is a potent, cell-permeable inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase.
T4205 AG 494 AG-494 is an inhibitor of epidermal growth factor receptor kinase.
T4249 AZD3759 hydrochloride AZD3759 (hydrochloride) is an effective, orally active and central nervous system-penetrant EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.2/0.3/0.2 nM for EGFR (L85
T4296 MTX211 MTX-211, an inhibitor of EGFR and PI3K, is used for the therapy of cancer and other diseases.
T4326 AG 555 AG 555 is an EGFR tyrosine kinase inhibitor.
T6008 CNX2006 CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
T6036 Brivanib Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3.
T6039 TAK285 TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.
T6078 Saracatinib Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.
T6092 Sapitinib AZD8931, a reversible, ATP competitive inhibitor of EGFR(IC50=4 nM), ErbB2(IC50=3 nM) and ErbB3(IC50=4 nM), is more effective over Gefitinib or Lapatinib against NSCLC cell, 100-fo
T6124 Mubritinib Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
T6136 Canertinib Canertinib is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumour met
T6153 Icotinib Icotinib is an orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity.
T6196 PP1 PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
T6227 Benidipine hydrochloride Benidipine HCl, a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel.
T6235 Lapatinib Ditosylate Lapatinib is an effective EGFR and ErbB2 inhibitor (IC50: 10.8/9.2 nM for EGFR/ErbB2).
T6238 WZ4002 WZ4002 is a mutant-selective EGFR inhibitor for EGFR(L858R) and EGFR(T790M) with IC50 of 2 nM/8 nM.
T6266 PP2 PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
T6328 Desmethyl Erlotinib OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
T6331 AST-1306 TsOH AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, respectively.
T6427 Butein Butein, a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit EGFR.
T6619 OSI420 OSI-420 (Desmethyl Erlotinib, CP-473420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for human EGFR and EG
T6712 Tyrphostin AG 879 Tyrphostin AG 879 effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.
T6733 WZ3146 WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).
T6734 WZ8040 WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
T6824 EAI045 EAI045, an allosteric inhibitor, targets towards drug-resistant EGFR mutants but avoids the wild-type receptor.
T6918 Olmutinib Olmutinib is an orally available small molecule, a mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to
T6932 PD168393 PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.
T4185 lavendustin C Lavendustin C is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase.
T4485 Lazertinib Lazertinib is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R an
T4528 Tyrphostin AG 528 Tyrphostin AG 528 is an inhibitor of EGFR (IC50: 4.9 μM) and ErbB2 (IC50: 2.1 μM).
T4694 AG-1557 hydrochloride (189290-58-2(free base)) AG-1557 is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).
T2034 AG1557 AG-1557 is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).
T1181 Gefitinib Gefitinib is an EGFR tyrosine kinase inhibitor and can inhibit Tyr1173, Tyr992, Tyr1173 and Tyr992 (IC50s: 37/37/26/57 nM).
T5155 AG 99 AG-99 is an inhibitor of EGFR kinase (IC50: 10 µM in the human epidermoid carcinoma cell line A431).
T5168 EGFR Inhibitor EGFR inhibitor is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells.
T9905 Cetuximab (anti-EGFR) Cetuximab anti-EGFR) a novel molecular-targeted agentis an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand s
T5410 PD158780 PD 158780 reversibly inhibits auto and transphosphorylation of all four members of the ErbB receptor superfamily: EGFR, ErbB2, ErbB3, and ErbB4 (IC50s: 8μM, 49 nM, 52 nM, and 52 n
T9922 Matuzumab Matuzumab is a humanized monoclonal antibody used in cancer treatment. It has a high affinity for EGFR frequently associated with the growth of blood vessels in malignancy facilita
T9923 Nimotuzumab Nimotuzumab is a humanized therapeutic monoclonal antibody against epidermal growth factor receptor EGFR).
T9927 Panitumumab Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).
T5462 HS-10296 Hs-10296 is an inhibitor of EGFR activation mutation and tolerant mutation of EGFR T790M, which has only limited activity against wild-type EGFR.
T5475 ZD-4190 ZD-4190 is a inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cance
T5675 HS-10296 hydrochloride HS-10296 hydrochloride is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
T7198 E-4031 E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM)
T7175 AST2818 mesylate AST2818 mesylate,is an irreversible tyrosine kinase inhibitor that selectively inhibits EGFR mutations, especially T790M.
T7322 Theliatinib Theliatinib, a potent and highly selective EGFR inhibitor, with anti-tumor activity. Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant
T9905 Cetuximab (anti-EGFR) Cetuximab (anti-EGFR) is an inhibitor of epidermal growth factor receptor (EGFR).
T7649 Tyrphostin A1 Tyrphostin A1 is an inhibitor of EGFR tyrosine kinase .
TQ0092 Naquotinib Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR.
TQ0255 CK-101 CK-101 (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.
TQ0271 Falnidamol Falnidamol (BIBX 1382) is a selective and orally active inhibitor of EGFR tyrosine kinase (IC50: 3 nM).
TQ0293 AV-412 free base AV-412 free base is an EGFR inhibitor (IC50s: 0.75, 0.79, 0.5, 2.3, 19 nM for EGFR, EGFR(T790M), EGFR(L858R), EGFR(L858R/T790M) and ErbB2).
TQ0166 Tesevatinib Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4).
T1291 Cisapride Cisapride is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal peristalsis, increase
T3554 RG 14620 RG14620 is an epidermal growth factor receptor (EGFR) inhibitor.
T2S0961 Chalcone Chalcone is an aromatic ketone that forms the central core for a variety of important biological compounds, which are known collectively as chalcones.
T8189 Dihydroberberine Dihydroberberine has anti-atherosclerotic, anti-inflammatory, hypolipidemic and antitumor activities. It inhibits human ether-a-go-go-related gene (hERG) channels and remarkably re
T8151 Mobocertinib Mobocertinib is a potent  inhibitor of epidermal growth factor receptor (EGFR) and an antineoplastic agent
TN1410 Asperulosidic acid Asperulosidic acid has been recently used in chinese medicine as a useful drug against some tumors.
TN1871 Ligustroside Ligustroside shows little antioxidant, and anti-inflammatory properties, it shows a significant inhibition effect on prostaglandin E2 (PGE2)-release. Ligustroside shows moderate an
TN1912 Marinobufagenin Marinobufagenin, a cardiotonic steroid, its increased concentrations are important in the cardiac disease and oxidant stress state seen with renal failure.
TN2309 Withanolide A Withanolide A extends the lifespan in human EGFR-driven cancerous Caenorhabditis elegans.
T8460 Olmutinib Olmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor
T12130 Mutated EGFR-IN-2 Mutated EGFR-IN-2 is an inhibitor of mutant-selective EGFR.
T12131 Mutated EGFR-IN-3 Mutated EGFR-IN-3 is a ATP-competitive and highly selective allosteric dibenzodiazepinone EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) inhibitor(IC50 of 12 nM and 13 nM, respectiv
T12175 Naquotinib mesylate Naquotinib mesylate is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR).
T19489 O-Desmethyl gefitinib D8 O-Desmethyl gefitinib D8 is a deuterium labeled O-Desmethyl gefitinib that is an active metabolite of Gefitinib in human plasma.
T10965 DBPR112 DBPR112 has an IC50 of 15 nM and 48 nM for EGFRWT and EGFRL858R / T790M, respectively. It is an oral active epidermal growth factor receptor inhibitor based on furimidine. DBPR112
T8431 JCN037 JCN037 is potent, non-covalent and brain-penetrant inhibitor of EGFR(EGFR, p-wtEGFR and pEGFRvⅢ with IC50 of 2.49 nM, 3.95 nM, 4.48 nM , respectively).
T14138 AG-825 AG-825(Tyrphostin AG-825) is a potential agent for overcoming Mn-induced neurotoxicity or AD development[5] and is a selective and ATP-competitive ErbB2 inhibitor which suppresses
T14336 Allitinib Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib is an anilino-quinazoline compound and has an
T10256 Afatinib D6 Afatinib D6 (BIBW 2992 D6) is a deuterium-labeled Afatinib. Afatinib is an irreversible EGFR family inhibitor.
T13559 Astragaloside VI Astragaloside VI could improve wound healing by activating the EGFR/ERK signaling pathway.
T10419 AV-412 AV-412 is an EGFR inhibitor (EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M and ErbB2 with IC50s of 0.75, 0.79, 0.5, 2.3, 19 nM).
T11213L Epertinib Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity.
T12777 RTC-5 RTC-5 demonstrated efficacy against a xenograft model of an EGFR driven cancer without the neurotropic effects exhibited by the parent molecules. Its effects were attributed to con
T12912 Sigma-1 receptor antagonist 3 Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.
T13088 Tarloxotinib bromide Tarloxotinib bromide is an irreversible inhibitor of EGFR/HER2.
T11157L EGFR-IN-1 hydrochloride EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity. EGFR-IN-1 hydrochloride is
T11157 EGFR-IN-1 EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity. EGFR-IN-1 is an orally active and irrever
T11158 EGFR-IN-11 EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor
T11159 EGFR-IN-2 EGFR-IN-2 is a non-covalent, mutation-selective and irreversible second-generation EGFR inhibitor.
T11160 EGFR-IN-5 EGFR-IN-5 is a EGFR inhibitor, EGFR-IN-5 with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively.
T11161 EGFR-IN-7 EGFR-IN-7 is a selective and potent EGFR kinase inhibitor.
T11162 EGFR-IN-8 EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC. EGFR-IN-8 is a dual EGFR and c-Met inhibitor.
T11163 EGFR-IN-9 EGFR-IN-9 has antitumor activity. EGFR-IN-9 is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M).
T11164 EGFR mutant-IN-1 EGFR mutant- in-1, A 5-methylpyrimidopyridone derivative are effective selective EGFRL858R/T790M/C797S mutant inhibitors with IC50 of 27.5 nM, which significantly weakened EGFRWT e
T11213 Epertinib hydrochloride Epertinib hydrochloride shows potent antitumor activity. Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and
T10531 BGB-102 BGB-102 is a potent multi-kinase inhibitor against HER2, EGFR, and HER4 (IC50s: 18 nM, 9.6 nM, and 40.3 nM).
T10534 BI-4020 BI-4020 is a fourth-generation, non-covalent, and orally active inhibitor of EGFR tyrosine kinase.
T10556 BKI-1369 BKI-1369 is a bumped kinase inhibitor. BKI-1369 increases hERG-inhibitory activity (IC50:1.52 μM).
T11569 HKI-357 HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM). HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
T10802 CHMFL-EGFR-202 CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase (IC50s: 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases).
T13743 JH-XI-10-02 JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19. JH-XI-10-02 is a potent and selective degrader of CDK8, with an
T11717 JHU395 JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST. JHU395 is an orally-b
T16362 Nuvenzepine Nuvenzepine is an antagonist of mAChR. It has the potential for gastrospasm treatment.
T8534 Tyrphostin AG 112 Tyrphostin AG 112 is an inhibitor of EGFR phosphorylation.
T10433 Osimertinib dimesylate Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M).
T16492 PF-06459988 PF-06459988 is an irreversible T790M-Containing EGFR Mutants inhibitor.
T21312 Afatinib free base Afatinib is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively).
T16996 TAS6417 TAS6417 is an EGFR inhibitor and is an efficacious drug candidate for patients with NSCLC (IC50: ranging from 1.1-8.0 nM).
T22272 Lifirafenib Lifirafenib (BGB-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR an
T22296 Cisapride hydrate Cisapride acts directly as a selective agonist of serotonin 5-HT4 receptor with IC50 value of 0.483 μM. And It also acts indirectly as a parasympathomimetic.
T3851 Vicenin -2 Vicenin 2 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=43.83 μM) from the aerial parts of Desmodium styracifolium. Vicenin 2 is an inhibitor of α-glucosidase, PTP1B,
T3P2855 Chamigrenal β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7 macrophages. Chamig
TL0016 Sulforaphene Sulforaphene may be a potential anti- triple negative breast cancer natural compound and its /\''antiproliferation effects may be mediated by tumor suppressor Egr1; it has chemothe
TN2504 1,5-Dihydroxyxanthone 1,5-Dihydroxyxanthone exhibits the epidermal growth factor receptor (EGFR) -tyrosine kinase inhibitory activity, with the IC50 value of 90.34 nM. It may have anticholinesterase act
TN3042 4-Hydroxycinnamamide 4-Hydroxycinnamamide has antioxidant activity. 4-Hydroxycinnamamide derivatives are specific inhibitors of tyrosine-specific protein kinases.
TN3525 Boehmenan (±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive mann
TN3711 Corylifol C Corylifol C and, to a lesser extent, xanthoangelol are potent protein kinase inhibitors (inhibitory concentration 50% values for epidermal growth factor receptor (EGFR): 1.1 and 4.
TN4213 Hirsutenone Hirsutenone has potent antioxidant activity, it shows significant free radical scavenging activity and exhibits inhibition effect on the mitochondrial lipid peroxidation.Hirsutenon
TN4638 Neolinine Neolinine(at 10uM) shows significant hERG K+ channel inhibition activity.
TMA1944 Protopine hydrochloride Protopine has antiplatelet effects,which is due to inhibition on thromboxane formation and phosphoinositides breakdown and then lead to the decrease of intracellular calcium concen
TN5100 Taspine Taspine shows antitumor activity by modulating the EGFR signaling pathway of Erk1/2 and Akt in vitro and in vivo, it can inhibit growth and induce apoptosis of HUVEC in a dose-depe
T8679 Epidermal Growth Factor Epidermal Growth Factor binds to epidermal growth factor receptor (EGFR) and stimulates cell growth and proliferation. It is approved for the treatment of diabetic foot ulcers.
T1266 Terfenadine Terfenadine is a prodrug that is metabolized by intestinal CYP3A4 to the active form fexofenadine, a selective histamine H1-receptor antagonist with antihistaminic and non-sedative
T0801 Tannic acid Tannic acid is a novel hERG channel blocker.
T2894 Norcantharidin Norcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
T19814 CP-380736 CP-380736 is an epidermal growth factor receptor (EGFR) inhibitor. EGFR is a tyrosine kinase that activates MAPK, JNK, and Akt pathways, and is an important mediator of several typ
T8872 (Rac)-JBJ-04-125-02 JBJ-04-125-02 is effective as a single agent in both in vitro and in vivo models of EGFR-mutant lung cancer.
T8758 Poziotinib hydrochloride Poziotinib hydrochloride irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress th
T5437 Gefitinib-based PROTAC 3 Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3
T4612 NS309 NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90
T4612 NS309 NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90
T16369 O-Desmethyl gefitinib O-Desmethyl gefitinib inhibits EGFR (IC50: 36 nM in subcellular assays). In human plasma, O-Desmethyl gefitinib is an active metabolite of Gefitinib. The formation of O-desmethyl g
T8751 AZD8931 diFuMaric acid AZD8931 is a reversible and ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 (IC50 of 4 nM, 3 nM and 4 nM, respectively).
T8751 AZD8931 diFuMaric acid AZD8931 is a reversible and ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 (IC50 of 4 nM, 3 nM and 4 nM, respectively).
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