c-Kit | 陶素生化

c-Kit

T0093	Sorafenib tosylate	Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
T0093L	Sorafenib	Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-4/B-Raf).
T0097L	Pazopanib	Pazopanib, a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit a
T0374	Sunitinib Malate	Sunitinib is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
T0374L	Sunitinib	Sunitinib, a multi-targeted RTK inhibitor, is targeting PDGFRβ and VEGFR2 (Flk-1) with IC50 of 2 nM and 80 nM and also inhibits c-Kit.
T10157	Regorafénib N-oxyde (M2)	Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, RET, Kit, and Raf-1 (IC50s: 13/4.2/46, 1.5, 22, 7,
T10650	c-Kit-IN-2	c-Kit-IN-2 is a c-KIT inhibitor (IC50: 82 nM), shows superior antiproliferative activities against all the three GIST cell lines, GIST430, GIST882, and GIST48 (GI50s: 1, 3, and 2 n
T10801	CHMFL-ABL/KIT-155	CHMFL-ABL/KIT-155 is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s: 46 nM/75 nM). It arrests cell cycle progression and induces apoptosis.
T13178	Toceranib	Toceranib phosphate is an orally active inhibitor of tyrosine kinase (RTK) receptor, and it potently inhibits PDGFR, VEGFR, and Kit(with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR
T1448	Dasatinib	Dasatinib is a potent inhibitor of the Bcr-Abl and Src family (IC50s: 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit, and c-KitD816V, respectively).
T1448L	Dasatinib monohydrate	Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of th
T1452	Axitinib	Axitinib is an orally bioavailable tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nM for VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ, respectively.
T14928	Agerafenib hydrochloride	Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).
T15199	Edicotinib	Edicotinib is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 n
T1621	Imatinib Mesylate	Imatinib mesylate is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).
T1667	Tandutinib	Tandutinib (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold select
T1792	Regorafenib	Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor (IC50s: 1.5/2.5/4.2/7/13/22 nM for RET/C-RAF/VEGFR2/c-Kit/VEGFR1/PDGFRβ).
T1792L	Regorafenib monohydrate	Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, R
T1797	Cabozantinib Malate	Cabozantinib S-malate is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activ
T1830	BX795	BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, t
T1836	AZD2932	AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3, and c-Kit.
T1925	PLX647	PLX647 is a highly selective dual FMS/KIT kinase inhibitor (IC50: 28/16 nM).
T2070	CEP32496	CEP-32496 is a highly potent inhibitor of BRAF.
T2115	Pexidartinib	Pexidartinib is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.
T22303	Dasatinib hydrochloride	Dasatinib hydrochloride is a highly ATP competitive, potent, orally active inhibitor of dual Src/Bcr-Abl(with Ki values of 16 pM and 30 pM for Src and Bcr-Abl, respectively), and h
T2288	Motesanib	Motesanib is an orally bioavailable receptor tyrosine kinase inhibitor with potential antineoplastic activity. AMG 706 selectively targets and inhibits vascular endothelial growth
T2288L	Motesanib Diphosphate	Motesanib Diphosphate is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity.
T2341	KW2449	KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.
T2372	Ponatinib	Ponatinib is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
T2446	KI8751	KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
T2500	Cediranib	Cediranib (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar a
T2514	Linifanib	Linifanib (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib
T2516	Amuvatinib	Amuvatinib is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.
T2586	Cabozantinib	Cabozantinib (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50s: 0.035, 1.3, 4.6, 7 and 11.3 nM).
T2609	Masitinib	Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed un
T2668	JNK-IN-8	JNK-IN-8 is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ in A375 cell line.
T3452	ISCK03	ISCK03 is a selective SCF/c-Kit inhibitor.
T4053	AST 487	AST 487 is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
T4320	Flumatinib	Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.
T4332	c-Kit-IN-1	DCC-2618 is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).
T4409	Gilteritinib	Gilteritinib is a potent inhibitor at the FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preClinicalal studies,
T5109	Avapritinib	Avapritinib is a dual inhibitor of the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM).
T5164	Cabozantinib hydrochloride (849217-68-1(free base))	Cabozantinib (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).
T5409	AZD3229	AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. It demonstrates potent single-digit nM growth inhibition across a broad cell pane
T6078	Saracatinib	Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.
T6091	CP673451	CP-673451 is a specific inhibitor of PDGFRα/β (IC50: 10/1 nM) with antiangiogenic and antitumor activity and the selectivity is higher 450-fold than other angiogenic receptors.
T6097	GNF5837	GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM).
T6137	KRN633	KRN-633 is an effective VEGFR inhibitor. The IC50s of KRN-633 for VEGFR1, VEGFR2, and VEGFR3 is 170, 160 and 125 nM, respectively.
T6166	Telatinib	Telatinib is an effective inhibitor of VEGFR2/3, c-Kit, and PDGFRα. The IC50s of Telatinib forVEGFR2/3, c-Kit and PDGFRα are 6 nM/4 nM, 1 nM, and 15 nM, respectively.
T6193	Dovitinib Dilactic Acid	Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM,
T6196	PP1	PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
T6230	Imatinib	matinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit (IC50: 600/100/100 nM).
T6289	Dovitinib	Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit, IC50: 1/2 nM), also effective to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs (IC5
T6479	Dovitinib Lactate	Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (F
T6711	Tyrphostin AG 1296	Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
T6930	Pazopanib HCl	Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 14
T7499	TAK-779	TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).
T7861	Flumatinib mesylate	Flumatinib mesylate is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.
T7945	SU14813	SU14813 is a multi-receptor tyrosine kinase inhibitor with potent antiangiogenesis and antitumor activity (IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT).
T8482	Ripretinib	Ripretinib is an orally bioavailable inhibitor of KIT and PDGFRA.
T8541	Lenvatinib mesylate	Lenvatinib mesylate is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.
T8544	Masitinib mesylate	Masitinib mesylate is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;PDGFRα/β;LynB,respectively).
TQ0080	SU14813 maleate	SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT).
TQ0235	AC710	AC710 is a potent PDGFR inhibitor (Kds: 0.6, 1, 1.57, 1.3, 1 nM for FLT3, KIT, CSF1R, PDGFRα and PDGFRβ).