(S)-1-(1-(imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine
Savolitinib
CAS: 1313725-88-0
Molecular Formula: C17H15N9
(S)-1-(1-(imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine - Names and Identifiers
(S)-1-(1-(imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine - Physico-chemical Properties
| Molecular Formula | C17H15N9 |
| Molar Mass | 345.36 |
| Density | 1.55±0.1 g/cm3(Predicted) |
| Melting Point | 205-207°C |
| Solubility | DMSO: ≥ 34 mg/mL |
| Appearance | Solid |
| Color | Pale Beige |
| pKa | 5.67±0.50(Predicted) |
| Storage Condition | -20°C Freezer |
| In vitro study | Volitinib has precise kinase selectivity and potency. In the gastric cancer cell line panel, Volitinib is highly selective and effectively inhibits cell growth in cell lines with dysregulated cMET (EC50 range of 0.6 nM/L-12.5 nM/L). Volitinib has good cell membrane permeability and no efflux transport in Caco-2 cell monolayers. In human liver microsomes, Volitinib had no significant reversible or mechanism-based CYP inhibition. In human liver cells, CYP1A2 and CYP3A4 were also not induced. |
| In vivo study | In a mouse pharmacokinetic study (ICR mice), the clearance of Volitinib was 4.28 L/(h kg) with a half-life of 1.7 hours. Although its oral bioavailability is only moderate (F = 27.2%), its total plasma exposure is high. Volitinib has a dose-dependent inhibition of tumor growth in a xenograft tumor model administered subcutaneously with U87MG. Its processing will lead to the adjustment of the pharmacodynamics of the c-MET signal, forming an effective tumor stasis in the 3/3 cMET-dysregulated GC PDX model. Volitinib has a moderate plasma protein binding rate, 60% to 60% in rats, dogs and humans, 40% in mice and 80% in monkeys, volitinib is widely distributed in different tissues and organs, with high exposure in liver and kidney, while the exposure in brain, spinal cord and testis is lower than that in plasma. In the pharmacokinetic study of mice, rats and dogs, Volitinib has a rapid oral absorption rate (Tmax<2.5 h) and high exposure, and the oral bioavailability is 27.2, 42.6, 86.3%, the in vivo clearance (CL) was 11.0, 11.8 and 3.5 mL/min/kg, respectively, and the volume of distribution (Vss) at steady state was 0.4, respectively, 1.4 and 1.4 L/kg. In rats Volitinib at doses of 1-25 mg/kg had a linear pharmacokinetic profile, whereas in dogs Volitinib at concentrations of 2-10 mg/kg had antecedent pharmacokinetics. Food intake has little effect on its pharmacokinetics in dogs. In monkeys, volitinib had a high extraction rate (CL = 17.2 mL/min/kg). In monkeys, the low oral bioavailability of volitinib may be due to excessive first-pass extraction. Overall, volitinib has good preclinical PK/ADME properties. |
(S)-1-(1-(imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.896 ml | 14.478 ml | 28.955 ml |
| 5 mM | 0.579 ml | 2.896 ml | 5.791 ml |
| 10 mM | 0.29 ml | 1.448 ml | 2.896 ml |
| 5 mM | 0.058 ml | 0.29 ml | 0.579 ml |
Last Update：2024-01-02 23:10:35
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CAS: 1313725-88-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Savolitinib Visit Supplier Webpage Request for quotationCAS: 1313725-88-0
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