Home Protein Tyrosine Kinase c-Met inhibitor - FLT3 inhibitor - DDR inhibitor - ROS1 inhibitor - Mertk inhibitor - Axl inhibitor Merestinib (LY2801653) For research use only.

Merestinib (LY2801653)

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.

Merestinib (LY2801653) Chemical Structure

Merestinib (LY2801653) Chemical Structure

CAS No. 1206799-15-6

Purity & Quality Control

Batch: S701401 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.78%
99.78

Merestinib (LY2801653) Related Products

Signaling Pathway

c-Met Signaling Pathways

c-Met Signaling Pathway

Biological Activity

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.
Targets
DDR1 [2]
(Cell-based assay)		 AXL [2]
(Cell-based assay)		 Met [1]
(Cell-free assay)		 MKNK1/2 [2]
(Cell-based assay)		 FLT3 [2]
(Cell-based assay)		 Click to View More Targets
0.1 nM 2 nM 2 nM(Ki) 7 nM 7 nM
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Athymic nude mice and CD-1 nude mice
Dosages 0.75 mg/kg to 100 mg/kg
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03125239 Completed
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
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
Advanced Cancer|Colorectal Cancer|Mantle Cell Lymphoma
Eli Lilly and Company
 October 21 2016 Phase 1
NCT02779738 Completed
Healthy
Eli Lilly and Company
 May 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 552.53 Formula

C30H22F2N6O3
CAS No. 1206799-15-6 SDF Download Merestinib (LY2801653) SDF
Smiles CC1=CC=C(C(=O)N1C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C(C=C5C(=C4)C=NN5C)C6=CNN=C6)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (180.98 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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