Futibatinib-TAS-120-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFutibatinibCat. No.: HY-100818CAS No.: 1448169-71-8Synonyms: TAS-120分式: CHNO分量: 418.45作靶点: FGFR作通路: Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 29 mg/mL (69.3

2、0 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3898 mL 11.9489 mL 23.8977 mL5 mM 0.4780 mL 2.3898 mL 4.7795 mL10 mM 0.2390 mL 1.1949 mL 2.3898 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性

3、，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.97 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.97 mM); Clear solution1/2 Master of Small Molecules 您边的抑

4、制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.97 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Futibatinib (TAS-120)种有效的 FGFR 抑制剂，具有抗肿瘤的功效。IC50 & Target FGFR体内研究 Futibatinib (TAS-120) (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor effect in mice. Futibatinib (TAS-120)show

5、s anti-tumor effect by administering at moderate intervals, such as intermittent administration of everyother day dosing and 2 times/week, and reducing the sustained elevation and weight suppression bloodphosphorus level, and take a antitumor effective as daily administration 1.PROTOCOLAnimal It is

6、transplanted to the right chest of the anti-tumor effect human gastric cancer strain (OCUM-2MD3) the oldAdministration 1 6-week-old male nude rats with intermittent administration schedule in Test Example 7 rat. Measuring themajor axis of tumor (mm) and minor axis (mm) after tumor implantation, the

7、tumor volume: After calculatingthe (tumor volume TV), allocates the mouse average TV each group to be equal in each group, the the daysthat are conducted grouped the (n=5) is the day 0. Futibatinib (TAS-120) 3 mg/kg/day, 30 mg/kg/day, isprepared so as to 100 mg/kg/day, 3 mg/kg/day is daily administe

8、red orally, 30 mg/kg/day is administeredorally every other day, 100 mg/kg/day is performed oral administration of 2 time/week from day 1, providedwith the evaluation period of 14 days, the final valuation date it is day 15.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Hiroaki OCHIIWA, et al. Antitumor drug for intermittent administration of fgfr inhibitor. WO 2015008839 A1.McePdfHeightCaution: Product has not been fully validated for medical appli