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SAR125844

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SAR125844 Basic information

Product Name:
SAR125844
Synonyms:
  • SAR125884
  • SAR125884 hydrochlorid (1116743-46-4(free base))
  • SAR125844; SAR 125844; SAR-125844
  • SAR125844
  • 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-yl)ethyl]urea
  • SAR125844 /SAR-125844
  • Urea, N-[6-[[6-(4-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]-2-benzothiazolyl]-N'-[2-(4-morpholinyl)ethyl]-
  • 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
CAS:
1116743-46-4
MF:
C25H23FN8O2S2
MW:
550.63
Mol File:
1116743-46-4.mol
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SAR125844 Chemical Properties

storage temp. 
Store at -20°C
solubility 
DMSO : 45 mg/mL (81.72 mM)
form 
Solid
color 
Light yellow to yellow
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SAR125844 Usage And Synthesis

Biological Activity

SAR125844 is a potent and highly selective Met (c-Met) kinase inhibitor with nanomolar activity against wild-type Met (c-Met) kinase (IC50=4.2 nM), against H1094Y, Y1235D, M1250T, The IC50s of the L1195V and D1228H mutants were 0.22, 1.7, 6.5, 65 and 81 nM, respectively.

in vitro

SAR125844 is an ATP-competitive and reversible inhibitor. SAR125844 has moderate activity against RON, a homolog that is structurally similar to MET, and SAR125844 inhibits RON with an IC50 of approximately 740 nM. SAR125844 is more than 100-fold more selective for MET kinase than for RON.

in vivo

In a pharmacokinetic study in mice, the oral bioavailability of SAR125844 was low, approximately 2%. Its Caco-2 permeability is moderate. In female SCID mice bearing xenograft tumors (inoculated with the MET-expanded Hs 746T human gastric tumor cell line), a single intravenous injection of 20 mg/kg of SAR125844 resulted in a plasma exposure of 6190 h ng/kg mL, clearance CL = 3.1 L/h/kg, large volume of distribution (Vss = 4.2 L/kg).

SAR125844Supplier

Shanghai Boyle Chemical Co., Ltd.
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sales@boylechem.com
Sichuan Wei Keqi Biological Technology Co., Ltd.
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028-81700200 18116577057
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3003855609@qq.com
Shanghai JiYi Biotechnology Co. Ltd.
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13621943973
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sales@shjiyipharmatech.com
Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696,15000506266 15000506266
SPIRO PHARMA
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eric_feng1954@126.com
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