Glumetinib | SCC244 | CAS#1642581-63-2 | c-MET inhibitor

MedKoo Cat#: 206935 | Name: Glumetinib

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Glumetinib, also known as SCC244, is a novel, potent and highly selective inhibitor of c-Met in MET-dependent cancer models. SCC244 showed subnanomolar potency against c-Met kinase activity and high selectivity versus 312 other tested protein kinases, making it one of the most selective c-Met inhibitors described to date. Moreover, this inhibitor profoundly and specifically inhibits c-Met signal transduction and thereby suppresses the c-Met-dependent neoplastic phenotype of tumor and endothelial cells.

Chemical Structure

Glumetinib

CAS#1642581-63-2

Theoretical Analysis

MedKoo Cat#: 206935

Name: Glumetinib

CAS#: 1642581-63-2

Chemical Formula: C21H17N9O2S

Exact Mass: 459.1226

Molecular Weight: 459.49

Elemental Analysis: C, 54.89; H, 3.73; N, 27.44; O, 6.96; S, 6.98

Price and Availability

Size	Price	Availability
25mg	USD 250.00	2 Weeks
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,650.00	2 Weeks
1g	USD 3,650.00	2 Weeks

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Synonym

Glumetinib; Gumarontinib; SCC244; SC-C244; SCC 244;

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

InChi Key

RYBLECYFLJXEJX-UHFFFAOYSA-N

InChi Code

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

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

In xenografts of human tumor cell lines or non-small-cell lung cancer and hepatocellular carcinoma patient-derived tumor tissue driven by MET aberration, SCC244 administration exhibits robust antitumor activity at the well-tolerated doses. Additionally, the in vivo antitumor activity of SCC244 involves the inhibition of c-Met downstream signaling via a mechanism of combined anti-proliferation and antiangiogenic effects. The results of the current study provide a strong foundation for the clinical investigation of SCC244 in patients with tumors harboring c-Met pathway alterations.

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM.

In vitro activity:

SCC244 was preferentially efficacious against EBC-1, MKN-45, SNU-5, cancer cell lines (Fig. 2A; Supplementary Table S3). The growth of these cells lines is driven by MET amplification, and they have been reported to be extremely sensitive to c-Met inhibition. SCC244 also significantly inhibited the proliferation of BaF3/ TPR-Met cells (Fig. 2A, Supplementary Table S3), which also feature c-Met–addicted cell growth. Reference: Mol Cancer Ther. 2018 Apr;17(4):751-762. https://pubmed.ncbi.nlm.nih.gov/29237805/

In vivo activity:

Thus, this study studied the antitumor efficacy of SCC244 by interrogating a panel of 4 human NSCLC tumor models and 5 HCC tumor models known to harbor MET-driven mutation [gene amplification or/and Exon 14 skipping mutation (MET ex14)] or c-Met overexpression (Table 1).This study found that SCC244 showed robust antitumor efficiency in all these 9 mouse models, with the tumor growth–inhibitory rate from 87.7% to 115.8% at the optimal dose of 10 mg/kg (Fig. 5; Table 1). Reference: Mol Cancer Ther. 2018 Apr;17(4):751-762. https://pubmed.ncbi.nlm.nih.gov/29237805/

	Solvent	mg/mL	mM
Solubility
	DMF	50.0	108.82
	DMF:PBS (pH 7.2) (1:1)	0.5	1.09
	DMSO	27.6	59.97

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 459.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Ai J, Chen Y, Peng X, Ji Y, Xi Y, Shen Y, Yang X, Su Y, Sun Y, Gao Y, Ma Y, Xiong B, Shen J, Ding J, Geng M. Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models. Mol Cancer Ther. 2018 Apr;17(4):751-762. doi: 10.1158/1535-7163.MCT-17-0368. Epub 2017 Dec 13. PMID: 29237805.

In vitro protocol:

In vivo protocol:

1: Ai J, Chen Y, Peng X, Ji Y, Xi Y, Shen Y, Yang X, Su Y, Sun YM, Gao Y, Ma Y, Xiong B, Shen J, Ding J, Geng M. Preclinical evaluation of SCC244 (Glumetinib), a novel, potent and highly selective inhibitor of c-Met in MET-dependent cancer models. Mol Cancer Ther. 2017 Dec 13. pii: molcanther.0368.2017. doi: 10.1158/1535-7163.MCT-17-0368. [Epub ahead of print] PubMed PMID: 29237805.