Glumetinib

SKU: orb1226003

Description

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.

Key Properties

• CAS Number: 1642581-63-2
• MW: 459.488
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₇N₉O₂S
• SMILES: O=S(N1N=CC2=NC=C(C3=CN(C)N=C3)C=C21)(C4=CN=C5C=CC(C6=CN(C)N=C6)=CN54)=O
• Target: c-Met/HGFR
• Solubility: 10 mM in DMSO

Bioactivity

• 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. 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.
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• 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. 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 Analysis Cell line: EBC-1 and MKN-45 cells. Concentration: 0-50 nM. Incubation time: 24 hours. Result: Consistently induced G1-S cell-cycle arrest.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SCC244 | SCC 244

Quick Database Links

Gene Symbol

c-Met/HGFR