目录号 | 产品详情 | 靶点 | |
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T1656L | |||
Vandetanib Fumarate is an orally available tyrosine kinase inhibitor. Vandetanib Fumarate works by blocking RET (REarranged during Transfection), vascular endothelial growth factor receptor (VEGFR-2, VEGFR-3), and epidermal growth factor receptor and to a | |||
T78871 | |||
PLM-101是一种口服抗癌剂,针对FLT3和RET具有选择性抑制作用,有效抑制急性髓系白血病(AML)细胞。通过抑制RET,PLM-101促使FLT3的自噬降解,并且通过抑制PI3K和Ras/ERK信号通路来发挥其抗白血病的活性。在小鼠MV4-11侧翼异种移植模型中,PLM-101以口服剂量3及10 mg/kg显示出抗肿瘤效果,并且在同种异种移植小鼠模型中,剂量为40 mg/kg(口服)亦展现出明显的抗肿瘤功效。 | |||
T74020 | |||
O-Demethyl Lenvatinib 是Lenvatinib 的代谢物。Lenvatinib (E7080) 一种具有口服活性的,多靶点酪氨酸激酶抑制剂,VEGFR1-3、FGFR1-4、PDGFR、KIT 和RET,显示有效抗癌的活性。 | |||
T78203 | |||
NSC194598是一种p53 DNA结合抑制剂,其体外和体内抑制p53序列特异性DNA结合的IC50值分别约为180 nM和2-40 μM。在人甲状腺髓样癌TT细胞中,NSC194598能够干扰突变RET基因的转录激活。该化合物可应用于研究放射及化学疗法对正常组织造成的急性毒性。 | |||
T73033 | Trk receptor | ||
TRKII-IN-1 是一种有效的 II 型TRK抑制剂,对TRKA/B/C及TRKAG667C的IC50分别为3.3、6.4、4.3 和 9.4 nM。此外,TRKII-IN-1 对FLT3、RET和VEGFR2也具有抑制作用,其IC50分别为1.3、9.9 和 71.1 nM。TRKII-IN-1 主要用于TRK驱动的癌症研究。 | |||
T14282 | Others | ||
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret and is also a DNA repair suppressor through suppression of DNA repai | |||
T2094 | FGFR Trk receptor c-RET Bcr-Abl Aurora Kinase Autophagy | ||
Danusertib (PHA-739358) 是一种极光激酶抑制剂,能够抑制 Aurora A、Aurora B 和 Aurora C 的活性,IC50值分别为 13、79 和 61 nM。它是一种具有潜在抗肿瘤活性的小分子 3-氨基吡唑衍生物。 | |||
T64090 | |||
Regorafenib (BAY 73-4506) mesylate 是一种口服具有活力的多靶点受体酪氨酸激酶 (tyrosine kinase) 抑制剂,能够抑制VEGFR1/2/3 (IC50=13/4.2/46 nM),PDGFRβ (IC50: 22 nM),Kit (IC50: 7 nM),RET (IC50: 1.5 nM) 和 Raf-1 (IC50: 2.5 nM)。Regorafenib mesylate 具有强大的抗肿瘤和抗血管生成作用。 | |||
T38653 | |||
HG-7-85-01 is a type II ATP competitive inhibitor targeting wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. It effectively inhibits T315I mutant Bcr-Abl kinase, as well as KDR and RET kinases with IC50 values of 3 nM, 20 nM, and 30 nM, respectively. In contrast, HG-7-85-01 exhibits weak or no inhibition towards other kinases (IC50 >2 μM). Furthermore, this compound inhibits cell proliferation through the induction of apoptosis and by impeding cell-cycle progression. | |||
T2070 | Raf c-RET Bcr-Abl PDGFR Src c-Kit | ||
Agerafenib (CEP32496) 是口服高效的 BRAFV600E 抑制剂,Kd 为 14 nM。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-02270 | RET Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
RET Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 69.1 kDa and the accession number is P07949-1.
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TMPY-04418 | RET Protein, Human, Recombinant (aa 658-1114, His & GST) | Human | Baculovirus Insect Cells | ||
RET Protein, Human, Recombinant (aa 658-1114, His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 76.7 kDa and the accession number is P07949-1.
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TMPJ-00290 | GFR Alpha-2/GFRA2 Protein, Human, Recombinant (hFc & His) | Human | HEK293 Cells | ||
GDNF family receptor alpha-2 is a glycosylphosphatidylinosito l (GPI)-linked cell surface receptor. It is part of the GDNF receptor family. Glial cell line-derived neurotrophic factor (GDNF) and neurturin (NTN) are two structurally related, potent neurotrophic factors that play key roles in the control of neuron survival and differentiation. GFRA2 mediates the NRTN-induced autophosphorylation and activation of the RET receptor. It also able to mediate GDNF signaling through the RET tyrosine kinase receptor. It acts preferentially as a receptor for NTN compared to its other family member, GDNF family receptor alpha 1.
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TMPH-03247 | Artemin Protein, Rat, Recombinant (His & Myc) | Rat | E. coli | ||
Ligand for the GFR-alpha-3-RET receptor complex but can also activate the GFR-alpha-1-RET receptor complex. Supports the survival of sensory and sympathetic peripheral neurons in culture and also supports the survival of dopaminergic neurons of the ventral mid-brain. Strong attractant of gut hematopoietic cells thus promoting the formation Peyer's patch-like structures, a major component of the gut-associated lymphoid tissue. Artemin Protein, Rat, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 17.1 kDa and the accession number is Q6AYE8.
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TMPH-02842 | CD133/PROM1 Protein, Mouse, Recombinant (His & SUMO) | Mouse | E. coli | ||
May play a role in cell differentiation, proliferation and apoptosis. Binds cholesterol in cholesterol-containing plasma membrane microdomains and may play a role in the organization of the apical plasma membrane in epithelial cells. During early retinal development acts as a key regulator of disk morphogenesis. Involved in regulation of MAPK and Akt signaling pathways. In neuroblastoma cells suppresses cell differentiation such as neurite outgrowth in a RET-dependent manner.
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TMPK-00109 | Artemin Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
Artemin (ARTN) is a member of glial cell line-derived neurotrophic factor (GDNF) family of ligands, and its signaling is mediated via a multi-component receptor complex including the glycosylphosphatidylinositol-anchored GDNF family receptors a (GFRa1, GFRa3) and RET receptor tyrosine kinase. The major mechanism of ARTN action is via binding to a non-signaling co-receptor. The major function of ARTN is to drive the molecule to induce migration and axonal projection from sympathetic neurons.
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TMPY-04207 | Motilin Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
MLN (Motilin) is a Protein Coding gene. 3 alternatively spliced human isoforms have been reported. This gene encodes a small peptide hormone that is secreted by cells of the small intestine to regulate gastrointestinal contractions and motility. The encoded protein belongs to the motilin family. Proteolytic processing of the secreted protein produces the mature peptide and a byproduct referred to as motilin-associated peptide (MAP). MLN plays an important role in the regulation of Interdigestive Gastrointestinal Motility and indirectly causes rhythmic contraction of duodenal and colonic smooth muscle. Diseases associated with MLN include Gastroparesis and Duodenogastric Reflux. Among its related pathways are RET signaling and Signaling by GPCR.
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TMPH-00001 | CD133/PROM1 Protein-VLP, Human, Recombinant (His) | Human | HEK293 Cells | ||
May play a role in cell differentiation, proliferation and apoptosis. Binds cholesterol in cholesterol-containing plasma membrane microdomains and may play a role in the organization of the apical plasma membrane in epithelial cells. During early retinal development acts as a key regulator of disk morphogenesis. Involved in regulation of MAPK and Akt signaling pathways. In neuroblastoma cells suppresses cell differentiation such as neurite outgrowth in a RET-dependent manner. CD133/PROM1 Protein-VLP, Human, Recombinant (His) is expressed in HEK293 mammalian cells with C-10xHis tag. The predicted molecular weight is 96.7 kDa and the accession number is O43490.
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TMPJ-00100 | Artemin Protein, Human, Recombinant | Human | E. coli | ||
Human Artemin is a GDNF family ligand that is distantly related to the TGF-β superfamily of molecules. It is synthesized as a preproprotein, and contains a variable length pre-, or signal sequence, plus a 68 amino acid (aa) proregion and a 113 aa mature segment. Following synthesis and proteolytic processing, mature ARTN is secreted as a presumably glycosylated, 28 kDa disulfide-linked homodimer that contains three intrachain disulfide bonds and the typical TGF-β signature cysteine-knot motif. In the mature region, human ARTN is 89% and 88% aa identical to rat and mouse ARTN, respectively. Human ARTN is active on rodent cells. The receptor for ARTN has been identified as the ligand binding subunit GFRα-3 plus the signal transducing subunit, RET. The GFRα-1/RET receptor complex has also been suggested to be a ligand binding unit for ARTN. ARTN is known to be a chemoattractant for sympathetic neuron axons innervating the developing cardiovascular system. It also promotes sensory neuron survival and likely plays a role in the development of the peripheral nervous system. Finally, it has been reported to reverse neuropathic pain due to nerve injury, and to help resolve morphological changes associated with nerve damage.
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TMPJ-01414 | GDF-15 Protein, Mouse, Recombinant (His & Flag) | Mouse | HEK293 Cells | ||
Growth Differentiation Factor 15 (GDF-15), also called Macrophage Inhibitory Cytokine 1 (MIC-1), is a divergent member of the TGF-beta superfamily. GDF15 can be secreted by a wide variety of cell types in response to a broad range of stressors. GDF-15 expression is dramatically upregulated during acute brain injury, cancer, cardiovascular disease, and inflammation, suggesting its potential value as a disease biomarker. GDF15 was shown to inhibit proliferation of primitive hematopoietic progenitors and introduced as a putative placental mediator of embryonic development. GDF15 has recently gained scientific and translational prominence with the discovery that its receptor is a GFRAL-RET heterodimer of which GFRAL is expressed solely in the hindbrain.
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TMPJ-00688 | Persephin Protein, Human, Recombinant | Human | E. coli | ||
Persephin is a secreted protein, belongs to the glial cell linederived neurotrophic factor (GDNF) family of the TGF-β superfamily. It shares 38-46% amino acid (aa) identity with family members GDNF, neurturin and artemin. It is expressed at very low levels in most tissues. Mature protein contains a signal sequence, a pro-domain and a 96 aa mature sequence with several cysteines that are conserved among family members. It circulates as an unglycosylated disulfide-linked homodimer. Like other GDNF family members, Persephin acts through engagement of GRFα4, a glycosylphosphatidylinositol (GPI)-linked GDNF receptor family Persephin is reported to promote both the survival and growth of central dopaminergic and motor neurons, and kidney development. These effects are correlated with the expression patterns of GFRα4, and RET.
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TMPY-01576 | Artemin Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 Cells | ||
Artemin (ARTN) is a member of glial cell line-derived neurotrophic factor (GDNF) family of ligands, and its signaling is mediated via a multi-component receptor complex including the glycosylphosphatidylinositol-anchored GDNF family receptors a (GFRa1, GFRa3) and RET receptor tyrosine kinase. The major mechanism of ARTN action is via binding to a non-signaling co-receptor. The major function of ARTN is to drive the molecule to induce migration and axonal projection from sympathetic neurons. It also promotes the survival, proliferation and neurite outgrowth of sympathetic neurons in vitro. ARTN triggers oncogenicity and metastasis by the activation of the AKT signaling pathway. Recent studies have reported that the expression of ARTN in hepatocellular carcinoma is associated with increased tumor size, quick relapse and shorter survival. Furthermore, ARTN promotes drug resistance such as antiestrogens, doxorubicin, fulvestrant, paclitaxel, tamoxifen and trastuzumab. Moreover, ARTN also stimulates the radio-therapeutic resistance. Hypoxia has been reported to regulate the cancer stem cell (CSC) population yet the underlying mechanism is poorly characterized. Artemin (ARTN) is a member of the glial cell derived neurotrophic factor family of ligands, is a hypoxia-responsive factor and is essential for hypoxia-induced CSC expansion in hepatocellular carcinoma (HCC). Clinically, elevated expression of ARTN in HCC was associated with larger tumor size, faster relapse and shorter survival. In vitro, HCC cells with forced expression of ARTN exhibited reduced apoptosis, increased proliferation, epithelial-mesenchymal transition (EMT) and enhanced motility. Additionally, ARTN dramatically increased xenograft tumor size and metastasis in vivo. Moreover, ARTN also enhanced tumorsphere formation and the tumor initiating capacity of HCC cells, consequent to expansion of the CD133+ CSC population. ARTN transcription was directly activated by hypoxia-induced factor-1α (HIF-1α) and hypoxia induced ARTN promoted EMT and increased the CSC population via AKT signaling.
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