Roblitinib (FGF-401) 是一种口服有效的，高选择性的FGFR4抑制剂，IC50为 1.9 nM。Roblitinib 有抗癌活性。
| 生物活性 | Roblitinib (FGF-401) is an orally active and highly selectiveFGFR4inhibitor with anIC50of 1.9 nM[1]. Roblitinib has antitumor activity[2]. |
| IC50& Target[1][2] | FGFR4 1.9 nM (IC50) | FGFR1 >10 μM (IC50) | FGFR2 >10 μM (IC50) | FGFR3 >10 μM (IC50) | rat FGFR4 >10 μM (IC50) |
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体外研究
(In Vitro) | Roblitinib (FGF-401; Compound Example 83) is a highly selective and potentFGFR4inhibitor (IC50= 1.9 nM)[1].
Roblitinib shows no activity FGFR1, FGFR2, FGFR3, rat FGFR4, C552A FGFR4 (all IC50>10 uM)[1].
Roblitinib inhibits HUH7 (IC50=12 nM), Hep3B (IC50=9 nM), JHH7 (IC50=9 nM), HEPG2 (IC50>10 uM), JHH (IC50>10 uM)[1].
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体内研究
(In Vivo) | Roblitinib (gavage; 10-100 mg/kg; b.i.d.; for 10 days) with the 30 mg/kg has the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model[1].
Roblitinib causes blood concentrations dropped below the IC90 threshold level within 8 h of dosing, and controlles tumor growth to the level of stasis at the lowest dose of 10 mg/kg for 6 days[1].
Roblitinib (iv at 1 mg/kg; po at 3 mg/kg) has a T1/2of 1.4 hours, a CL of 28 mL/minokg, and a Vssof 2.3 L/kg for Male mice (C57BL/6)[1].
Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T1/2of 4.4 hours, a CL of 19 mL/minokg, and a Vssof 3.9 L/kg for male SD rats[1].
| Animal Model: | Male Wistar Hannover rats (Hep3B xenograft model)[1] | | Dosage: | 10, 30, 100 mg/kg | | Administration: | Gavage; for 10 days | | Result: | Caused blood concentrations dropped below the IC90 threshold between 8 and 12 h following dosing.
Had the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model. |
| Animal Model: | Male mice (C57BL/6)[1] | | Dosage: | 1 mg/kg or 3 mg/kg (Pharmacokinetic Analysis) | | Administration: | IV at 1 mg/kg; PO at 3 mg/kg | | Result: | Had a T1/2of 1.4 hours, a CL of 28 mL/minokg, and a Vssof 2.3 L/kg. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 5.2 mg/mL(10.27 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9741 mL | 9.8705 mL | 19.7410 mL | | 5 mM | 0.3948 mL | 1.9741 mL | 3.9482 mL | | 10 mM | 0.1974 mL | 0.9870 mL | 1.9741 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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