Glumetinib (SCC244)
$120.00 – $800.00
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. Cheap Glumetinib on Market, Fast Shipping, >98% Purity.
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| Catalog No. | SYD-CHEM-S005 |
|---|---|
| Product Name | Glumetinib (SCC244) |
Description
APIM050403: Glumetinib (SCC244) is 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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