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

Futibatinib  (Synonyms: TAS-120)

目录号: HY-100818 纯度: 99.65%
COA 产品使用指南

摩尔计算器

Futibatinib (TAS-120) 是一种口服生物利用度高、选择性强、不可逆的 FGFR 抑制剂，对 FGFR 1-4 的 4 个亚型的 IC50 分别为 3.9、1.3、1.6 和 8.3 nM。Futibatinib 抑制突变型和野生型 FGFR2，且 IC50 相似 (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM)。

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Futibatinib Chemical Structure

Futibatinib Chemical Structure

CAS No. : 1448169-71-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1650
In-stock
1 mg ￥300
In-stock
5 mg ￥750
In-stock
10 mg ￥1200
In-stock
25 mg ￥2400
In-stock
50 mg ￥3840
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Futibatinib:

Futibatinib 相关抗体

Top Publications Citing Use of Products

查看 FGFR 亚型特异性产品:

查看所有亚型
FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM)[1][2][3].

IC50 & Target[3]

FGFR1

3.9 nM (IC50)

FGFR2

1.3 nM (IC50)

FGFR3

1.6 nM (IC50)

FGFR4

8.3 nM (IC50)

wild-type FGFR2

0.3 nM (IC50)

FGFR2 V5651

1-3 nM (IC50)

FGFR2 N550H

3.6 nM (IC50)

FGFR2 E566G

2.4 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Huh-7 IC50
> 10 μM
Compound: TAS-120
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
[PMID: 34129329]
NCI-H1581 IC50
0.007 μM
Compound: TAS-120
Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
[PMID: 34129329]
NCI-H460 IC50
> 10 μM
Compound: TAS-120
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
[PMID: 34129329]
SK-HEP1 IC50
0.152 μM
Compound: TAS-120
Antiproliferative activity against human SK-HEP1 cells expressing FGFR4 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
Antiproliferative activity against human SK-HEP1 cells expressing FGFR4 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
[PMID: 34129329]
SNU1 IC50
> 5000 nM
Compound: 5; TAS-120
Cytotoxicity against human SNU1 cells assessed as inhibition of cell growth measured after 72 hrs by cell titer glo assay
Cytotoxicity against human SNU1 cells assessed as inhibition of cell growth measured after 72 hrs by cell titer glo assay
[PMID: 37077386]
SNU-16 IC50
0.004 μM
Compound: TAS-120
Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
[PMID: 34129329]
SNU-16 IC50
3.7 nM
Compound: 5; TAS-120
Cytotoxicity against human SNU-16 cells assessed as inhibition of cell growth measured after 72 hrs by cell titer glo assay
Cytotoxicity against human SNU-16 cells assessed as inhibition of cell growth measured after 72 hrs by cell titer glo assay
[PMID: 37077386]
体外研究
(In Vitro)

Futibatinib (TAS-120) 与 FGFR 的 ATP 口袋中高度保守的 P 环半胱氨酸残基共价结合[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Futibatinib 相关抗体:
体内研究
(In Vivo)

Futibatinib (TAS-120) (3、30、100 mg/kg/天，口服) 在小鼠体内发挥抗肿瘤作用。Futibatinib (TAS-120) 通过中等间隔给药显示抗肿瘤作用，如隔日给药和每周2次间歇给药，减少持续升高和抑制体重的血磷水平，可作为抗肿瘤有效日常管理[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

418.45

Formula

C22H22N6O3
CAS 号
性状

固体

颜色

White to yellow

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 1 year
-20°C 6 months
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 29 mg/mL (69.30 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3898 mL 11.9489 mL 23.8977 mL
5 mM 0.4780 mL 2.3898 mL 4.7795 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.08 mg/mL (4.97 mM); 悬浊液; 超声助溶

    此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (4.97 mM); 悬浊液; 超声助溶

    此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
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

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.65%

COA (290 KB) HNMR (298 KB) LCMS (98 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

It is transplanted to the right chest of the anti-tumor effect human gastric cancer strain (OCUM-2MD3) the old 6-week-old male nude rats with intermittent administration schedule in Test Example 7 rat. Measuring the major axis of tumor (mm) and minor axis (mm) after tumor implantation, the tumor volume: After calculating the (tumor volume TV), allocates the mouse average TV each group to be equal in each group, the the days that are conducted grouped the (n=5) is the day 0. Futibatinib (TAS-120) 3 mg/kg/day, 30 mg/kg/day, is prepared so as to 100 mg/kg/day, 3 mg/kg/day is daily administered orally, 30 mg/kg/day is administered orally every other day, 100 mg/kg/day is performed oral administration of 2 time/week from day 1, provided with the evaluation period of 14 days, the final valuation date it is day 15.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Futibatinib 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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 2.3898 mL 11.9489 mL 23.8977 mL 59.7443 mL
5 mM 0.4780 mL 2.3898 mL 4.7795 mL 11.9489 mL
10 mM 0.2390 mL 1.1949 mL 2.3898 mL 5.9744 mL
15 mM 0.1593 mL 0.7966 mL 1.5932 mL 3.9830 mL
20 mM 0.1195 mL 0.5974 mL 1.1949 mL 2.9872 mL
25 mM 0.0956 mL 0.4780 mL 0.9559 mL 2.3898 mL
30 mM 0.0797 mL 0.3983 mL 0.7966 mL 1.9915 mL
40 mM 0.0597 mL 0.2987 mL 0.5974 mL 1.4936 mL
50 mM 0.0478 mL 0.2390 mL 0.4780 mL 1.1949 mL
60 mM 0.0398 mL 0.1991 mL 0.3983 mL 0.9957 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.

Keywords:

Futibatinib1448169-71-8TAS-120TAS120TAS 120FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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