Glumetinib, also known as SCC244, is a novel, potent and highly selective inhibitor of c-Met in MET-dependent cancer models. SCC244 showed subnanomolar potency against c-Met kinase activity and high selectivity versus 312 other tested protein kinases, making it one of the most selective c-Met inhibitors described to date. Moreover, this inhibitor profoundly and specifically inhibits c-Met signal transduction and thereby suppresses the c-Met-dependent neoplastic phenotype of tumor and endothelial cells.
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Name | Glumetinib |
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Iupac Chemical 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 |
Synonyms | Glumetinib; SCC244; SC-C244; SCC 244. |
Molecular Formula | C21H17N9O2S |
Molecular Weight | 459.12 |
Smile | O=S(N1N=CC2=NC=C(C3=CN(C)N=C3)C=C21)(C4=CN=C5C=CC(C6=CN(C)N=C6)=CN54)=O |
InChiKey | RYBLECYFLJXEJX-UHFFFAOYSA-N |
InChi | 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 |
CAS Number | 1642581-63-2 |
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Formulation | crystalline solid |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Solubility | Soluble in DMSO, not in water |
Handling | |
Shipping Condition | Shipped under ambient temperature |
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Clinical study |
1: Ai J, Chen Y, Peng X, Ji Y, Xi Y, Shen Y, Yang X, Su Y, Sun YM, Gao Y, Ma Y,
Xiong B, Shen J, Ding J, Geng M. Preclinical evaluation of SCC244 (Glumetinib), a
novel, potent and highly selective inhibitor of c-Met in MET-dependent cancer
models. Mol Cancer Ther. 2017 Dec 13. pii: molcanther.0368.2017. doi:
10.1158/1535-7163.MCT-17-0368. [Epub ahead of print] PubMed PMID: 29237805.