FGFR-IN-9 (Compound 19) 是一种有效的、可逆的、具有口服活性的FGFR抑制剂，对 FGFR4WT、FGFR3、FGFR4V550L、FGFR2 和 FGFR1 的IC50分别为 17.1、29.6、30.7、46.7 和 64.3 nM。
| 生物活性 | FGFR-IN-9 (Compound 19) is a potent, reversible and orally activeFGFRinhibitor with anIC50of 17.1, 29.6, 30.7, 46.7 and 64.3 nM againstFGFR4WT,FGFR3,FGFR4V550L,FGFR2andFGFR1, respectively[1]. |
| IC50& Target[1] | FGFR4WT 17.1 nM (IC50) | FGFR3 29.6 nM (IC50) | FGFR4V550L 30.7 nM (IC50) | FGFR2 46.7 nM (IC50) | FGFR1 64.3 nM (IC50) |
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体外研究
(In Vitro) | FGFR-IN-9 (Compound 19) (0-2 mM; 72 h) 抑制 HUH7 细胞，IC50为 94.7±28.6 nM，抑制 Ba/F3 FGFR4WT和 Ba/F3 FGFR4V550L细胞增殖，IC50分别为 82.5 ± 19.2 nM 和 260.0 ± 50.2 nM[1]。
FGFR-IN-9 (0-400 nM; 4 h) 抑制 FGFR 信号通路[1]。
Western Blot Analysis[1] | Cell Line: | Ba/F3-TEL-FGFR4 cells | | Concentration: | 0, 50, 100, 200 and 400 nM | | Incubation Time: | 4 h | | Result: | Showed dose-dependent inhibition of the FGFR4 signal cassette, including the phosphorylation of FGFR4 and its downstream effectors FRS2 and PLCγ. |
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体内研究
(In Vivo) | FGFR-IN-9 (Compound 19) (30 and 45 mg/kg; i.g.; daily for 3 weeks) 在 HUH7 异种移植小鼠模型中显示出抗肿瘤活性[1]。
In Vivo Pharmacokinetic Profile Data for FGFR-IN-9 (Compound 19)[1]
| FGFR-IN-9 | i.v. 1 mg/kg | p.o. 10 mg/kg | | T1/2(h) | 1.3 | 2.37 | | Tmax(h) | / | 2 | | Cmax(ng/mL) | / | 202 | | AUCmax(h·ng/mL) | 175 | 965 | | AUCINF(h·ng/mL) | 177 | 1087 | | MRTinf(h) | 1.13 | 3.87 | | F (%) | / | 61.5 | | VSS(L/kg) | 6.37 | / | | CL (L/h/kg) | 5.65 | / |
| Animal Model: | Female BALB/c nude mice, HUH7 xenograft model[1] | | Dosage: | 30 and 45 mg/kg | | Administration: | Intragastric gavage; daily for 3 weeks | | Result: | Resulted in significant tumor growth inhibition with a TGI value of 81% and an IR value of 63% at a dose of 45 mg/kg. No significant body weight loss (<5%) was observed. |
| Animal Model: | Male CD-1 mice[1] | | Dosage: | 1 mg/kg and 10 mg/kg | | Administration: | i.v. and p.o. (Pharmacokinetic Analysis) | | Result: | Showed good in vivo pharmacokinetic profile. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
