SAR125844
- CAS NO.:1116743-46-4
- Empirical Formula: C25H23FN8O2S2
- Molecular Weight: 550.63
- MDL number: MFCD25976852
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:03
What is SAR125844?
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).
Properties of SAR125844
storage temp. | Store at -20°C |
solubility | DMSO : 45 mg/mL (81.72 mM) |
form | Solid |
color | Light yellow to yellow |
Safety information for SAR125844
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for SAR125844
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