2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FGFR Apoptosis
  4. Erdafitinib

Erdafitinib  (Synonyms: 厄达替尼; JNJ-42756493)

目录号: HY-18708 纯度: 99.66%
COA 产品使用指南

摩尔计算器

Erdafitinib (JNJ-42756493)是有效的有口服活性的 FGFR 家族抑制剂；抑制FGFR1-4活性的 IC50 分别为1.2, 2.5, 3.0和5.7 nM。

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Erdafitinib Chemical Structure

Erdafitinib Chemical Structure

CAS No. : 1346242-81-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥825
In-stock
5 mg ￥700
In-stock
10 mg ￥990
In-stock
50 mg ￥2950
In-stock
100 mg ￥4200
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Erdafitinib:

Erdafitinib 相关抗体

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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

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

IC50 & Target[1]

FGFR1

1.2 nM (IC50)

FGFR2

2.5 nM (IC50)

FGFR3

3.0 nM (IC50)

FGFR4

5.7 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 IC50
0.02 μM
Compound: 1; JNJ-42756493
Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
AN3-CA GI50
0.048 μM
Compound: 2
Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
BaF3 GI50
> 5 μM
Compound: 2
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
BaF3 GI50
> 5 μM
Compound: 2
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
BaF3 GI50
0.005 μM
Compound: 2
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
BaF3 GI50
0.761 μM
Compound: 2
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
BaF3 GI50
4.011 μM
Compound: 2
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
HCT-116 IC50
4.24 μM
Compound: 1; JNJ-42756493
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
J82 GI50
3.796 μM
Compound: 2
Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
Jurkat IC50
6.81 μM
Compound: 1; JNJ-42756493
Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
K562 IC50
3.02 μM
Compound: 1; JNJ-42756493
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
KATO III stomach cancer cell line IC50
0.004 μM
Compound: 1; JNJ-42756493
Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
KMS-11 GI50
0.39 μM
Compound: 2
Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
Sf21 IC50
3 nM
Compound: JNJ-42756493
Inhibition of human recombinant N-terminal His6 tagged FGFR3 (447 to 761 residues) expressed in Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins in presence of ATP by time resolved f
Inhibition of human recombinant N-terminal His6 tagged FGFR3 (447 to 761 residues) expressed in Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins in presence of ATP by time resolved f
[PMID: 32278710]
Sf21 IC50
36.8 nM
Compound: JNJ-42756493
Inhibition of human N-terminal His6-tagged VEGFR2 (790 to end residues) expressed in baculovirus infected Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition in presence of ATP by time resolved fluorescence a
Inhibition of human N-terminal His6-tagged VEGFR2 (790 to end residues) expressed in baculovirus infected Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition in presence of ATP by time resolved fluorescence a
[PMID: 32278710]
Sf9 IC50
0.003 μM
Compound: 5
Inhibition of wild type His-tagged human FGFR3 (455 to 763 residues) expressed in Sf9 insect cells by ELISA
Inhibition of wild type His-tagged human FGFR3 (455 to 763 residues) expressed in Sf9 insect cells by ELISA
10.1039/C9MD90044F
SNU-16 IC50
0.0007 μM
Compound: 1; JNJ-42756493
Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36449947]
体外研究
(In Vitro)

在时间分辨荧光分析中，Erdafitinib（JNJ-42756493）对 FGFR1-4 的酪氨酸激酶活性具有抑制作用，其 IC50 值分别为 1.2、2.5、3.0 和 5.7 nM。Erdafitinib 对与FGFR 密切相关的 VEGFR2 激酶的抑制作用较弱 (与 FGFR1 相比效力低 30 倍)，其 IC50 值为 36.8 nM。Erdafitinib 与 FGFR 1、3、4 和 2 的结合 Kd 值分别为 0.24、1.1、1.4 和 2.2 nM。与 VEGFR2 的结合 Kd 值较高，为 6.6 nM。Erdafitinib 对表达 FGFR1、3 和 4 的细胞的增殖具有抑制作用，其 IC50 值分别为 22.1、13.2 和 25 nM[1]。

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

Erdafitinib 相关抗体:
体内研究
(In Vivo)

在来自具有 FGFR 激活突变的人类肿瘤细胞系或患者来源的肿瘤组织的异种移植模型中，给予 Erdafitinib 会产生强效且剂量依赖性的抗肿瘤活性，并伴有肿瘤中磷酸化 FGFR 和磷酸化 ERK 的药动学调节[1]。

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

446.54

Formula

C25H30N6O2
CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

厄达替尼
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 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 62.5 mg/mL (139.97 mM; 超声助溶; 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 2.2394 mL 11.1972 mL 22.3944 mL
5 mM 0.4479 mL 2.2394 mL 4.4789 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.75 mg/mL (6.16 mM); 澄清溶液

  • 方案 二

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (6.16 mM); 澄清溶液

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: 99.66%

COA (290 KB) HNMR (227 KB) LCMS (120 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

Erdafitinib is dissolved in DMSO. KATO III, RT-112, A-204, RT-4, DMS-114, A-427 and MDA-MB-453 cells are treated with erdafitinib (from 10 μM to 0.01 nM in 2% DMSO, final concentration). Following 4-day incubation, cell viability is determined using MTT reagent. The optical density is determined at 540 nm[1].

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

Mice: Mice bearing SNU-16 human gastric carcinoma (FGFR2 amplified) xenograft tumors are dosed orally with 0, 3, 10 or 30 mg/kg Erdafitinib. Tumor tissue and mouse plasma (3 mice per time point) are harvested at 0.5, 1, 3, 7, 16 and 24h post-dosing[1].

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

Erdafitinib 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2394 mL 11.1972 mL 22.3944 mL 55.9860 mL
5 mM 0.4479 mL 2.2394 mL 4.4789 mL 11.1972 mL
10 mM 0.2239 mL 1.1197 mL 2.2394 mL 5.5986 mL
15 mM 0.1493 mL 0.7465 mL 1.4930 mL 3.7324 mL
20 mM 0.1120 mL 0.5599 mL 1.1197 mL 2.7993 mL
25 mM 0.0896 mL 0.4479 mL 0.8958 mL 2.2394 mL
30 mM 0.0746 mL 0.3732 mL 0.7465 mL 1.8662 mL
40 mM 0.0560 mL 0.2799 mL 0.5599 mL 1.3997 mL
50 mM 0.0448 mL 0.2239 mL 0.4479 mL 1.1197 mL
60 mM 0.0373 mL 0.1866 mL 0.3732 mL 0.9331 mL
80 mM 0.0280 mL 0.1400 mL 0.2799 mL 0.6998 mL
100 mM 0.0224 mL 0.1120 mL 0.2239 mL 0.5599 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:

Erdafitinib1346242-81-6JNJ-42756493厄达替尼JNJ42756493JNJ 42756493FGFRApoptosisFibroblast growth factor receptorInhibitorinhibitorinhibit

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