SAR125844

SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer[1][2][3].

Product Specifications

CAS Number

[1116743-46-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Akt; Apoptosis; c-Met/HGFR; MEK; PI3K

Type

Reference compound

Related Pathways

Apoptosis; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/SAR125844.html

Purity

98.17

Solubility

DMSO : 45 mg/mL (ultrasonic)

Smiles

O=C(NCCN1CCOCC1)NC2=NC3=CC=C(SC4=NN=C5C=CC(C6=CC=C(F)C=C6)=NN54)C=C3S2

Molecular Formula

C25H23FN8O2S2

Molecular Weight

550.63

Precautions

H302, H315, H319, H335

References & Citations

[1]Egile C, et al. The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer. Mol Cancer Ther. 2015 Feb;14 (2) :384-94.|[2]Egile C, et al. The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer [J]. Molecular cancer therapeutics, 2015, 14 (2) : 384-394.|[3]Angevin E, et al. A first-in-human phase I study of SAR125844, a selective MET tyrosine kinase inhibitor, in patients with advanced solid tumours with MET amplification [J]. European Journal of Cancer, 2017, 87: 131-139.|[4]Ugolini A, et al. Discovery and pharmacokinetic and pharmacological properties of the potent and selective MET kinase inhibitor 1-{6-[6- (4-fluorophenyl) -[1, 2, 4] triazolo [4, 3-b] pyridazin-3-ylsulfanyl] benzothiazol-2-yl}-3- (2-morpholin-4-ylethyl) urea (SAR125844) [J]. 2016.