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CAS No. 1206799-15-6
Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.
Selleck's Merestinib (LY2801653) has been cited by 5 publications
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|Description||Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.|
LY2801653 demonstrates in vitro effects on MET pathway-dependent cell scattering and cell proliferation. It demonstrates more potent anti-proliferative activity in cell lines with MET gene amplification (MKN45, Hs746T and H1993) than the cell lines without MET gene amplification (U-87MG, KATO-III). LY2801653 also maintains potency against 13 MET variants, each bearing a single-point mutation. It is found to have potent activity against several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1/2 and against the serine/threonine kinases MKNK1/2. The mean IC50 value of 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.
LY2801653 shows in vivo 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. It is able to induce vessel normalization in xenograft tumors. Among the species studied, LY2801653 has the shortest elimination half life in mice of 2.9 h, compared with 14.3 h in non-human primate. LY2801653 is currently in phase 1 clinical testing in patients with advanced cancer.
|In vitro||DMSO||100 mg/mL (180.98 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03125239||Completed||Drug: Merestinib|Drug: LY2874455||Relapsed Adult Acute Myeloid Leukemia|Refractory Adult Acute Myeloid Leukemia||Jacqueline Garcia MD|Eli Lilly and Company|Dana-Farber Cancer Institute||August 10 2017||Phase 1|
|NCT03027284||Completed||Drug: Merestinib|Drug: Cisplatin|Drug: Gemcitabine||Advanced Cancer|Metastatic Cancer|Biliary Tract Carcinoma|Cholangiocarcinoma|Gall Bladder Carcinoma|Solid Tumor|Non-Hodgkin''s Lymphoma||Eli Lilly and Company||February 3 2017||Phase 1|
|NCT02745769||Completed||Drug: Ramucirumab|Drug: Merestinib|Drug: Abemaciclib||Advanced Cancer|Colorectal Cancer|Mantle Cell Lymphoma||Eli Lilly and Company||October 21 2016||Phase 1|
|NCT02779738||Completed||Drug: Merestinib||Healthy||Eli Lilly and Company||May 2016||Phase 1|
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