Free shipping on all orders over $ 500


Cat. No. M3515
MK-2461 Structure
Size Price Availability Quantity
5mg USD 195  USD195 In stock
10mg USD 350  USD350 In stock
50mg USD 1200  USD1200 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

MK-2461 is a potent inhibitor of c-Met, Ron, Flt1, Flt 3, PDGFRβ, and Mer with IC50 of 2.5 nM, 7 nM, 10 nM, 22 nM, 22 nM, and 24 nM, respectively. MK-2461 also exhibits significant activities toward several other kinases including FGFR1, FGFR2, FGFR3, KDR, TrkA, TrkB, and Flt4 with IC50 of 65 nM, 39 nM, 50 nM, 44 nM, 46 nM, 61 nM, and 78 nM, respectively. MK-2461 preferentially binds to the activated c-Met, and is slightly more potent against five naturally occurring oncogenic human c-Met mutants (N1100Y, Y1230C, Y1230H, Y1235D, and M1250T) compared with wild-type c-Met. MK-2461 significantly inhibits constitutive and ligand-induced phosphorylation of the juxtamembrane domain (Y1003) and the COOH-terminal docking site (Y1349/Y1365) of c-Met, as well as phosphorylation of AKT (S473) and ERK1/2 (T202/Y204), without affecting c-Met activation loop (Y1234/35) phosphorylation in GTL-16 cells. MK-2461 displays potent antiproliferative activity against a variety of tumor cell lines with IC50 of 0.1-30 μM. Orally administered MK-2461 inhibits c-Met phosphorylation in vivo, and tumor growth of GTL-16 xenografts, as well as the growth of NIH3T3 tumors harboring murine equivalents of human c-Met Y1230H and M1250T mutants.

Protocol (for reference only)
Cell Experiment
Cell lines SW480, HT29, SW620, Colo 205, HCT116, HCT15, Colo 201, SCC-9, H1993, H1048, GTL-16, SNU15, et al.
Preparation method Exposing cells to various concentrations of MK-2461 for 72 hours. Using the ViaLight PLUS kit to mearsure the viability of tumor cells .
Concentrations Dissolved in DMSO, final concentrations ~100 μM
Incubation time 72 hours
Animal Experiment
Animal models Female nude CD-1 nu/nu mice inoculated s.c. with GTL-16 cells or c-Met mutant-transformed NIH3T3 cells
Formulation Dissolved in DMSO, and diluted in saline
Dosages ~134 mg/kg
Administration Orally once or twice daily
Chemical Information
Molecular Weight 495.55
Formula C24H25N5O5S
CAS Number 917879-39-1
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Sadaf Ghanaatgar-Kasbi, et al. Targeting the C-MET/HGF Signaling Pathway in Pancreatic Ductal Adenocarcinoma

[2] Jing-Fang Wu, et al. Design and synthesis of novel substituted naphthyridines as potential c-Met kinase inhibitors based on MK-2461

[3] Jason D Katz, et al. Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer

[4] Bo-Sheng Pan, et al. MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor

[5] A Tomillero, et al. Gateways to clinical trials

Related c-Met Products
SU 5616

SU 5616 is an organic compound.


MET/PDGFRA-IN-2 is a MET and PDGFRA protein inhibitor.


MET/PDGFRA-IN-1 is a MET and PDGFRA protein inhibitor (IC50: 36 μM for MET).


Canlitinib is a tyrosine kinase inhibitor, extracted from patent WO2018072614 (IV-2).

Norleual TFA

Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM.

Abmole Inhibitor Catalog

Keywords: MK-2461 supplier, c-Met, inhibitors, activators

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.