SAR125884

Research use only, not for human use.

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

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

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 cellsConcentration:1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM, 10000 nMIncubation Time:96 hResult: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 nMIncubation Time:20 h Result:Inhibited cell migration with an IC50 value of 26 nM。

Animal Model:SNU-5 and Hs 746T tumor-bearing miceDosage: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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Angiogenesis

c-Met/HGFR

MET RTK

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1116743-46-4

550.63

C25H23FN8O2S2

>98% (HPLC)

DMSO:45 mg/mL (81.72 mM)

Fc1ccc(cc1)-c1ccc2nnc(Sc3ccc4nc(NC(=O)NCCN5CCOCC5)sc4c3)n2n1

1-(6-((6-(4-fluorophenyl)-[124]triazolo[43-b]pyridazin-3-yl)thio)benzo[d]thiazol-2-yl)-3-(2-morpholinoethyl)urea

(-20℃)

With Ice Pack

≥ 2 years