1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. Roblitinib

Roblitinib  (Synonyms: FGF-401)

目录号: HY-101568 纯度: 99.74%
COA 产品使用指南

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。

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Roblitinib Chemical Structure

Roblitinib Chemical Structure

CAS No. : 1708971-55-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1839
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2 mg ¥690
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5 mg ¥1000
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10 mg ¥1650
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50 mg ¥4800
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100 mg ¥7450
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查看 FGFR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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].

MCE 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
性状

固体

颜色

White to off-white

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 中的溶解度 : 5 mg/mL (9.87 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.74%

参考文献

Roblitinib 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9741 mL 9.8705 mL 19.7410 mL 49.3525 mL
5 mM 0.3948 mL 1.9741 mL 3.9482 mL 9.8705 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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目录号:
HY-101568
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