Glumetinib

Product NameGlumetinib
CAS1642581-63-2
MFC21H17N9O2S
MW459.48
EINECS
MOL File1642581-63-2.mol

Chemical Properties

Density	1.61±0.1 g/cm3(Predicted)
storage temp.	-20°C
solubility	Soluble in DMSO (>25 mg/ml)
form	solid
pka	0.09±0.10(Predicted)
color	Beige
Stability	Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

Usage And Synthesis

Description

Glumetinib (1642581-63-2) is a highly selective (2400-fold selectivity against a panel of 312 kinases) and potent (IC50 = 0.42 nM) inhibitor of c-Met kinase. It induced tumor regression in MET-driven CDX (MKN-45, SNU-5, EBC-1) and PDX (4 NSCLC, 5 HCC) tumor models.

Uses

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[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].

Animal Model:	Female nude mice (4-6 weeks old) (MKN-45 model)^[1]
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.

References

[1] JING AI. Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models.[J]. Molecular Cancer Therapeutics, 2018, 17 4: 751-762. DOI:10.1158/1535-7163.mct-17-0368