SAR125884

SKU: orb1220943

Description

SAR125844 a potent and highly selective inhibitor of the MET receptor tyrosine kinase (RTK) for intravenous administration. (IC50 value of 4.2 nmol/L).

Key Properties

• CAS Number: 1116743-46-4
• MW: 550.63
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₃FN₈O₂S₂
• SMILES: Fc1ccc(cc1)-c1ccc2nnc(Sc3ccc4nc(NC(=O)NCCN5CCOCC5)sc4c3)n2n1
• Target: c-Met/HGFR
• Solubility: DMSO:45 mg/mL (81.72 mM)

Bioactivity

• In Vivo:
  Animal model: SNU-5 and Hs 746T tumor-bearing mice. Dosage: 45 mg/kg. Administration: Intravenous injection (i. v.). Result: Resulted in complete and almost complete tumor regression in 3 of 8 mice and 5 of 8 mice, respectively. Animal model: MET-amplified gastric tumor model mice. Dosage: 5 mg/kg, 11 mg/kg, 21 mg/kg, 53 mg/kg, 106 mg/kg, 213 mg/kg. Administration: Intravenous injection (i. v.). Result: Resulted complete tumor regression in 7 of 8 of mice at 53, 106, and 213 mg/kg and partial regression at 11 and 21 mg/kg. Showed more than 80% MET inhibition at all doses and maintained for 96 hours at 213 mg/kg, 72 hours at. 106 mg/kg, and 48 hours at 53 mg/kg. Showed complete or near-complete regression (92%–99%) and maintained for 7 days at 106 mg/kg, and 48 hours at 53 mg/kg.
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• In Vitro:
  Cell Proliferation Assay Cell line: H-460 cells, HCT116 cells, H1993 cells, EBC-1 cells, SNU-5 cells, OE33 cells, Hs 746T cells and MKN-45 cells. Concentration: 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM, 10000 nM. Incubation time: 96 h. Result: Inhibited cell proliferation in all cell lines with MET gene amplification, with IC50 values in the nanomolar range (1-7 nM), with the exception of the lung cancer cell line NCI-H1573.Apoptosis Analysis Cell line: SNU-5 cells. Concentration: 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM. Incubation time: 24 h, 48 h, 72 h. Result: Induced massive apoptosis in SNU-5 cells at 48 and 72 hours, with a relative EC50 value of 6 nM and a plateau of 60% at 72 hours. Cell Migration Assay Cell line: H-460 cells, HCT116 cells, H1993 cells, EBC-1 cells, SNU-5 cells, OE33 cells, Hs 746T cells and MKN-45 cells. Concentration: 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM. Incubation time: 20 h. Result: Inhibited cell migration with an IC50 value of 26 nM。
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

c-Met/HGFR