SAR125844 | c-Met inhibitor | Probechem Biochemicals

Chemical Structure : SAR125844

CAS No.: 1116743-46-4

SAR125844 (SAR 125844, SAR-125844)

Catalog No.: PC-60463Not For Human Use, Lab Use Only.

SAR125844 is a potent, highly selective, ATP-competitive MET receptor tyrosine kinase inhibitor with IC50 of 4.2 nM.

Packing	Price	Stock
5 mg	$78	In stock
10 mg	$128	In stock
25 mg	$218	In stock
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Biological Activity

SAR125844 is a potent, highly selective, ATP-competitive MET receptor tyrosine kinase inhibitor with IC50 of 4.2 nM.
SAR125844 also inhibits H1094Y, Y1235D, M1250T, L1195V, and D1228H mutants with IC50 of 0.22, 1.7, 6.5, 65, and 81 nM, respectively.
SAR125844 displays >100-fold selectivity over RON, and good selectivity in a panel of 275 human kinases.
SAR125844 inhibits phosphorylation of wild-type MET, M1250T, Y1235D, and L1195V MET mutants with IC50 of 8.8, 30, 179, and 591 nM, respectively.
SAR125844 selectively inhibits proliferation in cells with MET gene amplification, promotes apoptosis and inhibits HGF-mediated tumor cell migration; displays potent antitumor activity in vivo models.

Physicochemical Properties

M.Wt	550.631
Formula	C25H23FN8O2S2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea

References

1. Egile C, et al. Mol Cancer Ther. 2015 Feb;14(2):384-94.

2. Ugolini A, et al. J Med Chem. 2016 Aug 11;59(15):7066-74.

3. Shitara K, et al. Oncotarget. 2017 Jun 16;8(45):79546-79555.

SAR125844 (SAR 125844, SAR-125844)

Biological Activity

Physicochemical Properties

References

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