| 化合物英文学名 |
Infigratinib |
化合物中文学名 |
Infigratinib |
| CAS号 |
872511-34-7 |
分子式 |
C26H31Cl2N7O3 |
| 分子量 |
560.475 |
精确质量 |
559.187 |
| LogP |
5.5033 |
PSA |
95.09 |
详细描述
产品描述:NVP-BGJ398(BGJ-398) is a novel selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively; >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes.
IC50 Value: 0.9 nM (FGFR1); 1.4 nM (FGFR2); 1 nM (FGFR2) [1]
Target: FGFR1/2/3
in vitro: NVP-BGJ398 is a novel and selective fibroblast growth factor receptor (FGFR) inhibitor. NVP-BGJ398 inhibit FGFR1, FGFR2, FGFR3 with IC50 of 0.9 nM, 1.4 nM and 1 nM. NVP-BGJ398 inhibited FGFR1, FGFR2, and FGFR3 with single digit nmol/L IC50 in biochemical and cellular autophosphorylation assays and FGFR4 with 38- to 60-fold lower potency. NVP-BGJ398 significantly inhibits proliferation of cancer cell lines bearing FGF/FGFR genetic alterations across various cancer types.Among the 35 cell lines selected from the high-throughput assays, 28 were confirmed as sensitive to NVP-BGJ398 with IC50s ranging from 0.001 to 500 nM. Cancer cell lines harboring FGF19 copy number gain at the 11q13 amplicon are sensitive to NVP-BGJ398 only when concomitant expression of beta-klotho occurs [1]. Cell lines with activating FGFR2 mutations (S252W, N550K) were more sensitive to dovitinib or NVP-BGJ398 when compared with their FGFR2 wild-type counterparts (P = 0.073 and P = 0.021, respectively). Both agents inhibited FGFR2 signaling, induced cell-cycle arrest, and significantly increased apoptosis in FGFR2-mutant lines. In vitro, dovitinib and NVP-BGJ398 were both potent at inhibiting cell growth of FGFR2-mutant endometrial cancer cells, but the activity of dovitinib was less restricted to FGFR2-mutant lines when compared with NVP-BGJ398 [2].
in vivo: In tumor tissues from primary tumor model GAM033 treated with 15 mg/kg NVP-BGJ398, NVP-BGJ398 shows inhibition to FGFR and ERK1/2 [1].NVP-BGJ398 significantly inhibited the growth of FGFR2-mutated endometrial cancer xenograft models [2].
产品链接:http://www.medchemexpress.com/Droxinostat.html
产品链接:http://www.medchemexpress.cn/nvp-bgj398.html
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