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Merestinib (LY2801653) c-Met inhibitor

Name: Merestinib (LY2801653)
Brand: Selleck Chemicals
SKU: S7014
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S7014

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. This compound 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.

Chemical Structure

Molecular Weight: 552.53

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.78

Related Targets	EGFR VEGFR PDGFR FGFR Src MEK CSF-1R FLT3 HER2 c-Kit
Other c-Met Products	Tepotinib Dihexa SGX-523 Foretinib PHA-665752 SU11274 BMS-777607 JNJ-38877605 Tivantinib PF-04217903

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (180.98 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	552.53	Formula	C₃₀H₂₂F₂N₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1206799-15-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	DDR1 (Cell-based assay) 0.1 nM AXL (Cell-based assay) 2 nM Met (Cell-free assay) 2 nM(Ki) MKNK1/2 (Cell-based assay) 7 nM FLT3 (Cell-based assay) 7 nM DDR2 (Cell-based assay) 7 nM MERTK (Cell-based assay) 10 nM MST1R (Cell-based assay) 11 nM ROS1 (Cell-based assay) 23 nM
In vitro	Merestinib (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). This compound 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 this chemical 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.
In vivo	Merestinib (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, this compound has the shortest elimination half life in mice of 2.9 h, compared with 14.3 h in non-human primate. It is currently in phase 1 clinical testing in patients with advanced cancer.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23275061/ [2] https://pubmed.ncbi.nlm.nih.gov/23275061/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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