SAR 125844 |CAS:1116743-46-4 Probechem Biochemicals

Chemical Structure : SAR 125844

CAS No.: 1116743-46-4

SAR 125844 (SAR125844;SAR-125844)

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

SAR 125844 is a potent, highly selective, ATP-competitive MET receptor tyrosine kinase inhibitor with IC50 of 4.2 nM.

Packing	Price	Stock
1 mg (Free Sample)	$18	In stock
5 mg	$78	In stock
10 mg	$128	In stock
25 mg	$218	In stock
50 mg		Get quote
100 mg		Get quote

Get Quotation Now

* Please select Quantity before adding items.

or Bulk Inquiry

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Biological Activity

SAR 125844 is a potent, highly selective, ATP-competitive MET receptor tyrosine kinase inhibitor with IC50 of 4.2 nM.
SAR 125844 also inhibits H1094Y, Y1235D, M1250T, L1195V, and D1228H mutants with IC50 of 0.22, 1.7, 6.5, 65, and 81 nM, respectively.
SAR 125844 displays >100-fold selectivity over RON, and good selectivity in a panel of 275 human kinases.
SAR 125844 inhibits phosphorylation of wild-type MET, M1250T, Y1235D, and L1195V MET mutants with IC50 of 8.8, 30, 179, and 591 nM, respectively.
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.

SAR 125844 (SAR125844;SAR-125844)

Biological Activity

Physicochemical Properties

References

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

Get Quote

* Indicates a Required FieldYour information is safe with us.