Roblitinib(Synonyms: FGF-401)

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Roblitinib (Synonyms: FGF-401) 纯度: 99.33%

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。

Roblitinib(Synonyms: FGF-401)

Roblitinib Chemical Structure

CAS No. : 1708971-55-4

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生物活性

Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 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)

体外研究
(In Vitro)

Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor (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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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 T1/2 of 1.4 hours, a CL of 28 mL/min•kg, and a Vss of 2.3 L/kg for Male mice (C57BL/6) [1].
Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T1/2 of 4.4 hours, a CL of 19 mL/min•kg, and a Vss of 3.9 L/kg for male SD rats[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 T1/2 of 1.4 hours, a CL of 28 mL/min•kg, and a Vss of 2.3 L/kg.

Clinical Trial

分子量

506.56

Formula

C25H30N8O4
CAS 号

1708971-55-4
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
溶解性数据
In Vitro: 

DMSO : 5.2 mg/mL (10.27 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Nicole Buschmann, et al. Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors. WO2015059668A1.

    [2]. Robin A Fairhurst, et al. Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. J Med Chem. 2020 Nov 12;63(21):12542-12573.

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