A potent c-Met inhibitor
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Glumetinib

Item No. 28952

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(1-methyl-1H-pyrazol-4-yl)-1-[[6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]sulfonyl]-1H-pyrazolo[4,3-b]pyridine
CAS Number
1642581-63-2
Synonyms
  • SCC244
Molecular Formula
C21H17N9O2S
Formula Weight
459.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50mg/mLDMF:PBS (pH 7.2) (1:1): 0.5mg/mLDMSO: 30mg/mL
λmax
264, 316 nm
SMILES
O=S(N1N=CC2=NC=C(C3=CN(C)N=C3)C=C21)(C4=CN=C5N4C=C(C6=CN(C)N=C6)C=C5)=O
InChi Code
InChI=1S/C21H17N9O2S/c1-27-11-16(7-24-27)14-3-4-20-23-10-21(29(20)13-14)33(31,32)30-19-5-15(6-22-18(19)9-26-30)17-8-25-28(2)12-17/h3-13H,1-2H3
InChi Key
RYBLECYFLJXEJX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Glumetinib is a potent inhibitor of c-Met (IC50 = 0.42 nM).1 It is greater than 2,400-fold selective for c-Met over a panel of 312 kinases. Glumetinib (0.001-1 μM) inhibits c-Met phosphorylation in and proliferation of MET-overexpressing EBC-1 lung and MKN45 gastric cancer cells. It inhibits NCI H441 cell motility and invasion induced by hepatocyte growth factor (HGF) when used at a concentration of 10 nM. Glumetinib (2.5-10 mg/kg) reduces tumor volume in MKN45, SNU-5, and EBC-1 mouse xenograft models. It also reduces tumor growth in MET amplification-containing non-small cell lung cancer (NSCLC) and hepatocellular carcinoma (HCC) patient-derived xenograft (PDX) mouse models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ai, J., Chen, Y., Peng, X., et al. Preclinical evaluation of SCC244 (glumetinib), a novel, potent, and highly selective inhibitor of c-Met in MET-dependent cancer models. Mol. Cancer Ther. 17(4), 751-762 (2017).