SAR125844

For research use only. Not for therapeutic Use.

  • CAT Number: I009283
  • CAS Number: 1116743-46-4
  • Molecular Formula: C25H23FN8O2S2
  • Molecular Weight: 550.63
  • Purity: ≥95%
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SAR125844(Cat No.:I009283)is a highly selective small-molecule inhibitor of c-MET, a receptor tyrosine kinase involved in cell proliferation, survival, and metastasis. By inhibiting c-MET signaling, SAR125844 disrupts tumor growth and the spread of cancer, particularly in cancers with MET gene amplification or overexpression. Preclinical studies have shown its efficacy in reducing tumor cell viability and inducing apoptosis in MET-dependent cancers, such as non-small cell lung cancer (NSCLC) and gastric cancer. SAR125844 is being explored in clinical trials for its potential to improve outcomes in MET-driven malignancies.


Catalog Number I009283
CAS Number 1116743-46-4
Synonyms

SAR125844; SAR 125844; SAR-125844;1-(6-((6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)thio)benzo[d]thiazol-2-yl)-3-(2-morpholinoethyl)urea

Molecular Formula C25H23FN8O2S2
Purity ≥95%
Target PI3K/Akt/mTOR
Solubility Soluble in DMSO, not in water
Storage 0 - 4 °C for short term, or -20 °C for long term
Overview of Clinical Research

Originator: Sanofi<br />
Class: Antineoplastics<br />
Mechanism of Action: Proto oncogene protein c met inhibitors<br />
Orphan Drug Status: No<br />
New Molecular Entity: Yes<br />

IUPAC Name 1-[6-[[6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl]-1,3-benzothiazol-2-yl]-3-(2-morpholin-4-ylethyl)urea
InChI InChI=1S/C25H23FN8O2S2/c26-17-3-1-16(2-4-17)19-7-8-22-30-31-25(34(22)32-19)37-18-5-6-20-21(15-18)38-24(28-20)29-23(35)27-9-10-33-11-13-36-14-12-33/h1-8,15H,9-14H2,(H2,27,28,29,35)
InChIKey ODIUNTQOXRXOIV-UHFFFAOYSA-N
SMILES C1COCCN1CCNC(=O)NC2=NC3=C(S2)C=C(C=C3)SC4=NN=C5N4N=C(C=C5)C6=CC=C(C=C6)F
Reference

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1: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). Ugolini A, Kenigsberg M, Rak A, Vallée F, Houtmann J, Lowinski M, Capdevila C, Khider J, Albert E, Martinet N, Nemecek C, Grapinet S, Bacqué E, Roesner M, Delaisi C, Calvet L, Bonche F, Semiond D, Egile C, Goulaouic H, Schio L.J Med Chem. 2016 Aug 11;59(15):7066-74. doi: 10.1021/acs.jmedchem.6b00280. Epub 2016 Jul 13. PMID: 27355974 <br />
2:The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer. Egile C, Kenigsberg M, Delaisi C, Bégassat F, Do-Vale V, Mestadier J, Bonche F, Bénard T, Nicolas JP, Valence S, Lefranc C, Francesconi E, Castell C, Lefebvre AM, Nemecek C, Calvet L, Goulaouic H.Mol Cancer Ther. 2015 Feb;14(2):384-94. doi: 10.1158/1535-7163.MCT-14-0428. Epub 2014 Dec 10. PMID: 25504634 Free Article

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