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Roblitinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Roblitinib图片
CAS NO:1708971-55-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
FGF-401
产品介绍
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)

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].

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.
Clinical Trial
分子量

506.56

性状

Solid

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM1.9741 mL9.8705 mL19.7410 mL
5 mM0.3948 mL1.9741 mL3.9482 mL
10 mM0.1974 mL0.9870 mL1.9741 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。