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CAS No.: 1310746-10-1

Infigratinib phosphate Catalog No. CSN17679

Synonyms: BGJ-398 phosphate;NVP-BGJ398 phosphate;Infigratinib Phosphate

BGJ398 Phosphate is a selective and potent inhibitor of FGFRs with IC50 values of 1nM for FGFR11-3 and 60nM for FGFR4, as well as 4.9nM for FGFR3-K650E mutant.

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技术信息

生物活性

描述The FGFR (fibroblast growth factor receptor) family, comprising four members, FGFR1, FGFR2, FGFR3 and FGFR4, belongs to the RTKs which serve as high affinity receptors for FGFs controlling cell proliferation, migration, apoptosis and differentiation. BGJ398 is a selective and potent inhibitor of FGFRs with IC50 values of 1nM for FGFR11-3 and 60nM for FGFR4, as well as 4.9nM for FGFR3-K650E mutant (measured by purified recombinant enzymes). Treatment with BGJ398 in cell lysate from HEK293 cells transfected with FGFRs resulted in inhibition on autophosphorylation on specific tyrosine residues of FGFR 1-3 with IC50 values below 5nM. Consistent with the in vitro study, BGJ398 inhibited the proliferation of the FGFR1-, FGFR2-, and FGFR3-dependent BaF3 cells with IC50 values ranged from 0.7-52.2nM depended by different FGFR isoforms. Daily oral treatment with BGJ398 at dose of 10 or 30mg/kg for 12 consecutive days induced tumor growth inhibition in the orthotopic xenograft bladder cancer model. Similarly, nearly complete tumor stasis was achieved by oral treatment of BGJ398 at dose of 5, 10 and 15mg/kg in RT112 human bladder cancer xenografted rats.^[1]
作用机制BGJ398 Phosphate binds with ATP-binding pocket of FGFR3.^[1]
参考文献

[1] Guagnano V, Furet P, 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-methyl-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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5187 mL
- 7.5934 mL
- 15.1867 mL
- 5 mM
- 0.3037 mL
- 1.5187 mL
- 3.0373 mL
- 10 mM
- 0.1519 mL
- 0.7593 mL
- 1.5187 mL

技术信息

CAS号	1310746-10-1	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C26H34Cl2N7O7P	运输	蓝冰
分子量	658.47	别名	BGJ-398 phosphate;NVP-BGJ398 phosphate;Infigratinib Phosphate;NVPBGJ-398;BGJ-398;Infigratinib

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