CAS |
No.1448169-71-8 |
英文名称 |
Futibatinib |
分子式 |
C22H22N6O3 |
分子量 |
418.45 |
溶解性 |
Soluble in DMSO ≥3mg/mL(Need ultrasonic) |
纯度 |
≥98% |
外观(性状) |
White to yellow Soild |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
MDL |
MFCD29037352 |
靶点 |
FGFR |
通路 |
Angiogenesis; Protein Tyrosine Kinase/RTK |
背景说明 |
Futibatinib 是一种有效的 FGFR 抑制剂,具有抗肿瘤活性。 |
生物活性 |
Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9?nM; V5651=1-3?nM; N550H=3.6?nM; E566G=2.4?nM).[1-3] |
IC50 |
FGFR1 3.9 nM (IC50) FGFR2 1.3 nM (IC50) FGFR3 1.6 nM (IC50) FGFR4 8.3 nM (IC50) wild-type FGFR2 0.3 nM (IC50) FGFR2 V5651 1-3 nM (IC50) FGFR2 N550H 3.6 nM (IC50) FGFR2 E566G 2.4 nM (IC50)[1-3] |
In Vitro |
Futibatinib (TAS-120) 与 FGFR 的 ATP 口袋中高度保守的 P 环半胱氨酸残基共价结合[1]。 |
In Vivo |
Futibatinib (TAS-120) (3、30、100 mg/kg/天,口服) 在小鼠体内发挥抗肿瘤作用。Futibatinib (TAS-120) 通过中等间隔给药显示抗肿瘤作用,如隔日给药和每周2次间歇给药,减少持续升高和抑制体重的血磷水平,可作为抗肿瘤有效日常管理[1]。 |
动物实验 |
It is transplanted to the right chest of the anti-tumor effect human gastric cancer strain (OCUM-2MD3) the old 6-week-old male nude rats with intermittent administration schedule in Test Example 7 rat. Measuring the major axis of tumor (mm) and minor axis (mm) after tumor implantation, the tumor volume: After calculating the (tumor volume TV), allocates the mouse average TV each group to be equal in each group, the the days that are conducted grouped the (n=5) is the day 0. Futibatinib (TAS-120) 3 mg/kg/day, 30 mg/kg/day, is prepared so as to 100 mg/kg/day, 3 mg/kg/day is daily administered orally, 30 mg/kg/day is administered orally every other day, 100 mg/kg/day is performed oral administration of 2 time/week from day 1, provided with the evaluation period of 14 days, the final valuation date it is day 15. |
数据来源文献 |
[1]. Goyal L, et al. TAS-120 Overcomes Resistance to ATP-Competitive FGFR Inhibitors in Patients with FGFR2 Fusion-Positive Intrahepatic Cholangiocarcinoma. Cancer Discov. 2019 Aug;9(8):1064-1079. [2]. Kalyukina M, et al. TAS-120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure. ChemMedChem. 2019 Feb 19;14(4):494-500. [3]. Lamarca A, et al. Molecular targeted therapies: Ready for “prime time“ in biliary tract cancer [published online ahead of print, 2020 Mar 12]. J Hepatol. 2020;S0168-8278(20)30165-3. |
规格 |
1mg 5mg 10mg 25mg 50mg |
单位 |
瓶 |