SAR125844

SKU: orb1689883

Description

SAR125844 is a potent and selective small molecule inhibitor of the MET receptor tyrosine kinase, exhibiting an IC50 of 4.2 nM. It is utilized in preclinical research to investigate MET-driven oncogenesis and has demonstrated antitumor activity in both cellular assays and in vivo xenograft models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1116743-46-4
• MW: 550.63
• Purity: 98.73% (May vary between batches)
• Formula: C₂₅H₂₃FN₈O₂S₂
• SMILES: Fc1ccc(cc1)-c1ccc2nnc(Sc3ccc4nc(NC(=O)NCCN5CCOCC5)sc4c3)n2n1
• Target: PI3K,MEK,Akt,c-Met/HGFR,Apoptosis
• Solubility: DMSO:45 mg/mL (81.72 mM);10% DMSO+90% Corn Oil:2 mg/mL (3.63 mM)

Bioactivity

• Target IC50:
  MET RTK:4.2 nM
• In Vitro:
  SAR125844 inhibits MET autophosphorylation in cell-based assays in the nanomolar range, and promotes low nanomolar proapoptotic and antiproliferative activities selectively in cell lines with MET gene amplification or pathway addiction.
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• Cell Research:
  MKN-45, Hs 746T, and SNU-5 cells were seeded in poly d-lysine 96-well plates in complete medium. Plates were incubated with increasing SAR125844 concentrations for 1 hour, cell lysates were generated using standard procedures and pMETY1230/1234/1235 level evaluated. IC50 values were calculated using the Biost@t-SPEED internal software and a 4-parameter logistic model
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• Animal Research:
  Long duration of MET kinase inhibition up to 7 days was achieved with a nanosuspension formulation of SAR125844. Daily or every-2-days intravenous treatment of SAR125844 promoted a dose-dependent tumor regression in MET-amplified human gastric cancer models at tolerated doses without treatment-related body weight loss.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, MET RTK, HGFR, Apoptosis, c-Met, cMet/HGFR, cMet, c-Met/HGFR, SAR125844, SAR-125844, SAR125884, SAR-125884, SAR 125844, SAR 125884

Compound Identifiers

PubChem CID

25182860