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Merestinib

CAS No. : 1206799-15-6

MCE 站：Merestinib

产品活性：Merestinib (LY2801653) 是一种有效的口服生物可利用的具有抗肿瘤活性的 c-Met 抑制剂 (K_i=2 nM)。Merestinib (LY2801653) 对 MST1R (IC₅₀=11 nM)、FLT3 (IC₅₀=7 nM)、AXL (IC₅₀=2 nM)、MERTK (IC₅₀=10 nM)、TEK (IC₅₀=63 nM)、ROS1、DDR1/2 (IC₅₀=0.1/7 nM) 和 MKNK1/2 (IC₅₀=7 nM) 也有较强的活性。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：c-Met/HGFR  |  FLT3  |  ROS  |  Discoidin Domain Receptor

In Vitro: Merestinib (LY2801653) demonstrates effects on MET pathway-dependent cell scattering and cell proliferation. The mean IC₅₀ value (n=6 determinations) of Merestinib (LY2801653) for inhibition of MET auto-phosphorylation in HGF-stimulated H460 cells is 35.2±6.9 nM and the IC₅₀ for MET auto-phosphorylation in S114 cells is 59.2 nM. Merestinib (LY2801653) also inhibits MST1R (IC₅₀=11 nM), AXL (IC₅₀=2 nM), MERTK (IC₅₀=10 nM), TYRO3 (IC50=28 nM), ROS1, PDGFRA (IC50=41 nM), FLT3 (IC₅₀=7 nM), TEK (IC50=63 nM), DDR1/2 (IC₅₀=0.1/7 nM) and MKNK1/2 (IC₅₀=7 nM).
Transfection with the MET variants confers growth-factor independence and treatment with Merestinib (LY2801653) inhibits growth of these MET variant clones with an IC₅₀ ranging from 3-fold more potent (V1092I) to approximately 6-fold less potent (L1195V) compare with the growth inhibition of cells with the MET wild-type sequence. Merestinib (LY2801653) (2, 5, and 10 μM) reduces the number of viable TFK-1 and SZ-1 cells in a dose and time dependent manner, and significant inhibits wound healing for TFK-1 and SZ-1 cell lines. Merestinib (LY2801653) inhibits cell invasion in TFK-1 and SZ-1 cells in a concentration dependent manner.

In Vivo: Merestinib (LY2801653) demonstrates anti-tumor effects in MET amplified (MKN45), MET autocrine (U-87MG, and KP4) and MET over-expressed (H441) xenograft models; and in vivo vessel normalization effects. Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a pharmacodynamic residence time (K_off) of 0.00132 min^-1 and t_1/2 of 525 min. Merestinib (LY2801653) treatment inhibits MET phosphorylation with a composite TED50 (50 % target inhibition dose) of 1.2 mg/kg and a composite TED90 (90 % target inhibition dose) of 7.4 mg/kg. Merestinib (LY2801653) (20 mg/kg) reduces TFK-1 tumor growth significantly relative to vehicle control. Merestinib (LY2801653) inhibits the growth of intra- and extrahepatic CCC xenograft tumors.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Orally Active Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  AT9283  |  Gandotinib  |  KW-2449  |  Lestaurtinib  |  PHA-665752  |  2-Phospho-L-ascorbic acid trisodium  |  WRG-28  |  DDR1-IN-1  |  CG-806  |  β-Carotene  |  SU11274  |  AST 487  |  SRI 31215 TFA  |  VU6015929  |  c-Met inhibitor 1  |  JNJ-47117096 hydrochloride  |  BPR1J-097 Hydrochloride  |  Crotonoside  |  Tyrphostin AG1296  |  X-376  |  DDR Inhibitor  |  SKLB4771  |  Tyrosine kinase inhibitor  |  TCS 359  |  3-Hydroxy Midostaurin  |  Hypothemycin  |  Sorafenib (D3)  |  (R)-3-Hydroxy Midostaurin  |  (S)-3-Hydroxy Midostaurin  |  5'-Fluoroindirubinoxime

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