E7090 是一种有效的，具有口服活性的选择性FGFR抑制剂，对FGFR1/FGFR2/FGFR3/FGFR4的IC50值分别为 0.71 nM、0.50 nM、1.2 nM 和120 nM。
| 生物活性 | E7090 is an orally available, potent, and selectiveFGFRinhibitor withIC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM forFGFR1/FGFR2/FGFR3/FGFR4, respectively[1]. |
| IC50& Target[2] | FGFR1 0.71 nM (IC50) | FGFR2 0.50 nM (IC50) | FGFR3 1.2 nM (IC50) | FGFR4 120 nM (IC50) |
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体外研究
(In Vitro) | E7090 inhibits the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC50value of 3 nM[1].
E7090 inhibits SNU-16 cell proliferation with an IC50value of 5.7 nM[2].
E7090 inhibits proliferation of human cancer cell lines harboring various types of FGFRs gene abnormalities such as amplification, mutation, or translocation in vitro, which are confirmed by the inhibition of FGFR signaling[1].
E7090 has interaction kinetics with FGFR1 kinases intermediate between those of the two representative inhibitors, and the residence time of E7090 succinate is 19 minutes[1].
Western Blot Analysis[1] | Cell Line: | SNU-16 cells | | Concentration: | 0.4-100 nM | | Incubation Time: | 4 hours | | Result: | Inhibited FGFR phosphorylation with an IC50value of 1.2 nM.
Inhibited the phosphorylation of FRS2a, ERK1/2, and AKT, molecules downstream of FGFRs, in a dose-dependent manner. |
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体内研究
(In Vivo) | Pharmacodynamics analysis reveals that E7090 inhibits phosphorylation of FGFRs in SNU-16 xenograft tumors in a dose-dependent manner[1].
E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model[2].
| Animal Model: | Mouse xenograft model of SNU-16 human gastric cancer[2] | | Dosage: | 6.25 to 50 mg/kg | | Administration: | Orally, once daily for 14 days | | Result: | Inhibited tumor growth in a dose-dependent manner. |
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| Clinical Trial | |
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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. |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(170.16 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.7016 mL | 8.5082 mL | 17.0164 mL | | 5 mM | 0.3403 mL | 1.7016 mL | 3.4033 mL | | 10 mM | 0.1702 mL | 0.8508 mL | 1.7016 mL |
In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.25 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.25 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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