Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Infigratinib phosphate (BGJ-398 phosphate) 是 FGFR 抑制剂,对 FGFR1,FGFR2 和 FGFR3 的 IC50 分别为0.9,1.4 和 1 nM,比对 FGFR4 和 VEGFR2 的抑制性高40倍,对 Abl,Fyn,Kit,Lck 和 Lyn 几乎无活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 185 | 现货 | ||
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 496 | 现货 | ||
25 mg | ¥ 733 | 现货 | ||
50 mg | ¥ 993 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 150 | 现货 |
产品描述 | Infigratinib phosphate (BGJ-398 phosphate) is an effective inhibitor of the FGFR family (IC50: 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively). |
靶点活性 | FGFR4:60 nM, FGFR3:1 nM, FGFR1:0.9 nM, FGFR2:1.4 nM |
体外活性 | Infigratinib inhibits the proliferation of the FGFR1-, FGFR2-, and FGFR3-dependent BaF3 cells with IC50 values which are in the low nanomolar range and comparable to those observed for the inhibition of the receptors kinase activity in the enzymatic assay. Infigratinib phosphate suppresses FGFR1, FGFR2, and FGFR3(IC50=~1 nM), FGFR3K650E(IC50=4.9 nM), and FGFR4(IC50=60 nM). IC50 values for all other kinases are in the μM range (FYN, LCK, YES, and ABL, IC50=1.9, 2.5, 1.1, and 2.3 μM, respectively) except for VEGFR2, KIT, and LYN, which are inhibited at submicromolar concentrations (IC50=0.18, 0.75, and 0.3 μM, respectively). Infigratinib (ranging between 1 nM and 10 μM) is effective at inhibiting cell growth of FGFR2-mutant endometrial cancer cells. For the remaining cells, all IC50 values are greater than 1.5 μM except for VEGFR2 (IC50 1449 and 938 nM), for which there is at least a 400-fold selectivity versus FGFR1, FGFR2, and FGFR3[1][2]. |
体内活性 | Infigratinib (30 mg/kg) significantly suppresses the growth of FGFR2-mutated endometrial cancer xenograft models. Infigratinib is administered to athymic nude mice implanted subcutaneously with RT112/luc1 tumors: either as a 5 mg/kg intravenous bolus in NMP/PEG200 (1:9, v/v) or orally by gavage as a suspension in PEG300/D5W (2:1, v/v) at a 20 mg/kg dose. Infigratinib shows a rapid distribution from the vascular compartment into the peripheral tissues after intravenous dosing, translating into a high volume of distribution (26 L/kg). The relevant pharmacokinetic (PK) parameters indicate that the oral bioavailability of Infigratinib in this study is 32%. The plasma clearance is high at 3.3 L/h/kg (61% of liver blood flow). The ratio of tumor to plasma after oral dosing based on AUC is determined to be 10 [1][2]. |
别名 | NVP-BGJ398 phosphate, BGJ-398 phosphate |
分子量 | 658.47 |
分子式 | C26H34Cl2N7O7P |
CAS No. | 1310746-10-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 11.7mg/mL (17.8mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.5187 mL | 7.5934 mL | 15.1867 mL | 37.9668 mL |
5 mM | 0.3037 mL | 1.5187 mL | 3.0373 mL | 7.5934 mL | |
10 mM | 0.1519 mL | 0.7593 mL | 1.5187 mL | 3.7967 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Infigratinib phosphate 1310746-10-1 Angiogenesis Tyrosine Kinase/Adaptors FGFR NVP-BGJ398 Phosphate BGJ-398 Phosphate Infigratinib Phosphate BGJ398 Phosphate NVP-BGJ398 phosphate BGJ-398 phosphate BGJ 398 Phosphate NVP-BGJ 398 Phosphate NVP-BGJ-398 Phosphate Inhibitor inhibitor inhibit