Merestinib (LY2801653)

Catalog No.S7014

Merestinib (LY2801653) Chemical Structure

Molecular Weight(MW): 552.53

LY2801653 is a type-II ATP competitive, slow-off inhibitor of 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.

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Biological Activity

Description LY2801653 is a type-II ATP competitive, slow-off inhibitor of 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.
Targets
Met [1]
(Cell-free assay)
2 nM(Ki)
In vitro

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[1].

In vivo 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[1].

Protocol

Cell Research:

[1]

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  • Cell lines: DU145 cells
  • Concentrations: 0.01-10 μM
  • Incubation Time: 48 h
  • Method:

    2×103 DU145 cells/well on poly-D-lysine 96-well black/clear plates are treated with LY2801653 (in 0.4 % DMSO), immediately followed by the addition of human HGF (20 ng/ml), and incubated for 48 h at 37 °C. 2 % formaldehyde fixed cells are stained with AlexaFluor 488 Phalloidin and counterstained with Propidium Iodide. Colony counts are quantified on Acumen Explorer™ laser-scanning fluorescence microplate cytometer. A colony is defined as≥4 cells.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Athymic nude mice and CD-1 nude mice
  • Formulation: 10% acacia
  • Dosages: 0.75 mg/kg to 100 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (180.98 mM)
Ethanol 100 mg/mL (180.98 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 552.53
Formula

C30H22F2N6O3

CAS No. 1206799-15-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03125239 Recruiting 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 Active not recruiting 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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c-Met Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID