Glumetinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Glumetinib (SCC 244) 是一种新型有效且高选择性的 c-Met 激酶抑制剂，IC50 为 0.42 nM。

Glumetinib (SCC 244)?is a novel potent and highly selective inhibitor of c-Met kinase with IC50 of 0.42 nM; displays high selectivity versus 312 other tested protein kinases; profoundly and specifically inhibits c-Met signal transduction and suppresses the c-Met-dependent neoplastic phenotype of tumor and endothelial cells; exhibits robust in vivo antitumor activity in NSCLC and hepatocellular carcinoma models.Lung Cancer Preclinical(In Vitro):Glumetinib (SCC244) (0-10 nM; 72 hours) elicits selective and profound effects against c-Met–driven cancer cell proliferation.Glumetinib (0-50 nM; 24 hours) induces G1–S phase cell-cycle arrest in c-Met–addicted human cancer cells.(In Vivo):Glumetinib (2.5-10 mg/kg; p.o.; once daily for 2-3 weeks) significantly inhibits c-Met–driven tumor growth in cancer CDX models.Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration.

Glumetinib (SCC244) (0-10 nM; 72 hours) elicits selective and profound effects against c-Met–driven cancer cell proliferation.Glumetinib (0-50 nM; 24 hours) induces G1–S phase cell-cycle arrest in c-Met–addicted human cancer cells. Cell Proliferation Assay Cell Line:EBC-1, SNU-5, MKN-45, BaF3/TPR-Met cells Concentration:0-10 nM Incubation Time:72 hours Result:Specifically and potently inhibited proliferation of c-Met–addicted human cancer cells (IC50 ranging 0.5 to 2.45 nM for EBC-1, SNU-5, MKN-45, BaF3/TPR-Met cells ).Cell Cycle AnalysisCell Line:EBC-1 and MKN-45 cells Concentration:0-50 nM Incubation Time:24 hours Result:Consistently induced G1–S cell-cycle arrest.

Glumetinib (2.5-10 mg/kg; p.o.; once daily for 2-3 weeks) significantly inhibits c-Met–driven tumor growth in cancer CDX models.Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration. Animal Model:Female nude mice (4-6 weeks old) (MKN-45 model) Dosage:10, 5, 2.5 mg/kg Administration:P.o.; once daily for 2-3 weeks Result:Significantly inhibited tumor growth with inhibitory rates of 99.3%, 88.6%, and 63.6% at doses of 10, 5, and 2.5 mg/kg, respectively.

SCC244 | SCC 244

Angiogenesis

c-Met/HGFR

c-Met

Cancer

Lung Cancer

1642581-63-2

459.488

C21H17N9O2S

>98% (HPLC)

10 mM in DMSO

O=S(N1N=CC2=NC=C(C3=CN(C)N=C3)C=C21)(C4=CN=C5C=CC(C6=CN(C)N=C6)=CN54)=O

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

(-20℃)

With Ice Pack

≥ 2 years