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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
Met
Available Sizes
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