Glumetinib


Catalog No. Size PriceQuantity
M27851-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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.

Product information

CAS Number: 1642581-63-2

Molecular Weight: 459.48

Formula: C21H17N9O2S

Chemical Name: 1-methyl-4-(1-{[6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]sulfonyl}-1H-pyrazolo[4,3-b]pyridin-6-yl)-1H-pyrazole

Smiles: CN1C=C(C=N1)C1=CN=C2C=NN(C2=C1)S(=O)(=O)C1=CN=C2C=CC(=CN21)C1=CN(C)N=C1

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 41.67 mg/mL (90.69 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

Products are for research use only. Not for human use.

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