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

Roblitinib  (Synonyms: FGF-401)

目錄號: HY-101568 純度: 99.74%
COA 產(chǎn)品使用指南 技術支持

Roblitinib (FGF-401) 是一種口服有效的，高選擇性的 FGFR4 抑制劑，IC50 為 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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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥491
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2 mg ￥690
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5 mg ￥1000
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10 mg ￥1650
In-stock
25 mg ￥3163
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50 mg ￥4800
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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
24 nM
Compound: 6; FGF401
Antiproliferative activity against mouse BaF3 cells transfected with FGFR4 V550M mutant assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against mouse BaF3 cells transfected with FGFR4 V550M mutant assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
[PMID: 36278929]
BaF3 IC50
3 nM
Compound: 6; FGF401
Antiproliferative activity against mouse BaF3 cells transfected with human FGFR4 assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against mouse BaF3 cells transfected with human FGFR4 assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
[PMID: 36278929]
BaF3 IC50
5 nM
Compound: 6; FGF401
Antiproliferative activity against mouse BaF3 cells transfected with FGFR4 V550L mutant assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against mouse BaF3 cells transfected with FGFR4 V550L mutant assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
[PMID: 36278929]
Hep 3B2 IC50
0.01 μM
Compound: 6; FGF401
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 5 days by SRB analysis
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 5 days by SRB analysis
[PMID: 36278929]
Hep 3B2 IC50
8.8 nM
Compound: FGF401
Antiproliferative activity against human Hep3B cells with high FGFR4 expression assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo method
Antiproliferative activity against human Hep3B cells with high FGFR4 expression assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo method
[PMID: 30987781]
Huh-7 IC50
0.026 μM
Compound: 6; FGF401
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 5 days by SRB analysis
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 5 days by SRB analysis
[PMID: 36278929]
Huh-7 IC50
16.3 nM
Compound: FGF401
Antiproliferative activity against human HuH7 cells with high FGFR4 expression assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo method
Antiproliferative activity against human HuH7 cells with high FGFR4 expression assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo method
[PMID: 30987781]
NCI-H1299 IC50
16.2 μM
Compound: 6; FGF401
Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 5 days by SRB analysis
Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 5 days by SRB analysis
[PMID: 36278929]
體外研究
(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.
體內(nèi)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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 5 mg/mL (9.87 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質量 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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.74%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質量 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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產(chǎn)品名稱：
Roblitinib
目錄號：
HY-101568
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