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The cheapest Glumetinib (SCC244, CAS No.: 1642581-63-2) is for research use only. Significant discount for bulk order of Glumetinib (SCC244). Condition of sample preparation and optimal sample dilution should be determined experimentally by the investigator.
Price/availability/specifications subject to change without notice. Unless otherwise indicated, our catalog and customized products are for research use only and not intended for human or animal diagnostic or therapeutic use.
Phone: 1-617-401-8149
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A highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM.
CAS No.: 1642581-63-2
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
Molecular Formula: C21H17N9O2S
Molecular Weight: 459.5
Purity: >98% (or refer to the Certificate of Analysis)
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental Analysis Report
Solubility: Soluble in DMSO
Storage: Store at 0 °C (short term), -20 °C (long term), Desiccated
Note: Please contact us for COA, Spectra, and SDS information.
Background Information:
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity.
Target: c-Met kinase
IC50: 0.42 nM
In Vitro: Glumetinib (SCC244) (0-10 nM; 72 hours) elicits selective and profound effects against c-Met–driven cancer cell proliferation.[1]
Glumetinib (0-50 nM; 24 hours) induces G1–S phase cell-cycle arrest in c-Met–addicted human cancer cells.[1]
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.[1]
Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration.[1]
What is the solubility of Glumetinib (SCC244) in vitro?
41.67 mg/mL in DMSO (Need ultrasonic)
Reference:
[1]. Ai, J. 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. 2018, 17, 751-762.
[2]. Chen, H.-J. et al. “32O First-in-human (FIH) study of SCC244, a novel potent and highly selective c- MET inhibitor, in patients (pts) with advanced non-small cell lung cancer (NSCLC)”, Ann. Oncol. 2021, 32, S14.
[3]. Ma, Y. et al. “Design and Optimization of a Series of 1-Sulfonylpyrazolo[4,3-b]pyridines as Selective c-Met Inhibitors”, J. Med. Chem. 2015, 58, 2513-2529.
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