A c-MET inhibitor
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MK-2461

Item No. 32964

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N′-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-sulfamide
CAS Number
917879-39-1
Molecular Formula
C24H25N5O5S
Formula Weight
495.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/ml
λmax
262, 346 nm
SMILES
O=C1C2=CC(C3=CN(N=C3)C)=CN=C2C=CC4=CC=C(NS(N(C)C[C@@H]5COCCO5)(=O)=O)C=C41
InChi Code
InChI=1S/C24H25N5O5S/c1-28-13-18(12-26-28)17-9-22-23(25-11-17)6-4-16-3-5-19(10-21(16)24(22)30)27-35(31,32)29(2)14-20-15-33-7-8-34-20/h3-6,9-13,20,27H,7-8,14-15H2,1-2H3/t20-/m1/s1
InChi Key
JGEBLDKNWBUGRZ-HXUWFJFHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $202

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    5 mg

    $351

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    10 mg

    $599

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    Product Description

    MK-2461 is an inhibitor of wild-type and mutant forms of c-MET (IC50s = 0.4-2 nM).1 It is selective for c-MET over a panel of 13 additional kinases (IC50s = 22-7,800 nM) but does inhibit Ron and FLT1 (IC50s = 7 and 10 nM, respectively). MK-2461 also inhibits autophosphorylation of FGFR2 and PDGFRα in KATO III cells but not EGF-induced phosphorylation of EGFR in A549 lung cancer cells when used at a concentration of 2 µM.2 It reduces proliferation in a panel of cancer cell lines, including cells expressing constitutively active c-MET, FGFR2, or PDGFR (IC50s = ≤1 µM for all).2 MKT-2461 (10-200 mg/kg) reduces tumor growth in a GTL-16 gastric cancer mouse xenograft model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Katz, J.D., Jewell, J.P., Guerin, D.J., 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. J. Med. Chem. 54(12), 4092-4108 (2011).

    2. Pan, B.-S., Chan, G.K.Y., Chenard, M., et al. MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer. Res. 70(4), 1524-1533 (2010).