货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S82791-5mg	≥96%	￥410.00 S82791-5mg ￥410.00 3-5天	0 货期：3-5天	-	-	-	-
S82791-10mg	≥96%	￥490.00 S82791-10mg ￥490.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S82791-5mg

≥96%

￥410.00

货期：3-5天

S82791-10mg

≥96%

￥490.00

货期：3-5天

产品描述：

Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) is a potent inhibitor of the FGFR family with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

靶点：

FGFR1:0.9 nM (IC50);FGFR2:1.4 nM (IC50);FGFR3:1 nM (IC50);FGFR4:60 nM (IC50);FGFR

体外研究：

Infigratinib phosphate inhibits FGFR1, FGFR2, and FGFR3 with IC50=~1 nM, FGFR3K650E with IC50=4.9 nM, and FGFR4 with 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 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. 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. Infigratinib (ranging between 1 nM and 10 μM) is potent at inhibiting cell growth of FGFR2-mutant endometrial cancer cells

体内研究：

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. The relevant pharmacokinetic (PK) parameters indicate that the oral bioavailability of Infigratinib in this study is 32%. After intravenous dosing, Infigratinib shows a rapid distribution from the vascular compartment into the peripheral tissues, translating into a high volume of distribution (26 L/kg). 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. Infigratinib (30 mg/kg) significantly inhibits the growth of FGFR2-mutated endometrial cancer xenograft models

参考文献：

1. Guagnano V, et al. Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-me thyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of receptor tyrosine kinase. J Med Chem. 2011 Oct 27;54(20):7066-83. 2. Konecny GE, et al. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Mol Cancer Ther. 2013 May;12(5):632-42.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.519 ml	7.593 ml	15.187 ml
5 mM	0.304 ml	1.519 ml	3.037 ml
10 mM	0.152 ml	0.759 ml	1.519 ml
50 mM	0.03 ml	0.152 ml	0.304 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

NVP-BGJ398 (phosphate)