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

Erdafitinib  (Synonyms: 厄達(dá)替尼; JNJ-42756493)

目錄號: HY-18708 純度: 99.66%
COA 產(chǎn)品使用指南 技術(shù)支持

Erdafitinib (JNJ-42756493)是有效的有口服活性的 FGFR 家族抑制劑；抑制FGFR1-4活性的 IC50 分別為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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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥688
In-stock
1 mg ￥310
In-stock
5 mg ￥700
In-stock
10 mg ￥990
In-stock
25 mg ￥1900
In-stock
50 mg ￥2950
In-stock
100 mg ￥4200
In-stock
500 mg 現(xiàn)貨 詢價(jià)
1 g   詢價(jià)  
5 g   詢價(jià)  

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Customer Review

Other Forms of Erdafitinib:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

細(xì)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]
體外研究
(In Vitro)

在時間分辨熒光分析中，Erdafitinib（JNJ-42756493）對 FGFR1-4 的酪氨酸激酶活性具有抑制作用，其 IC50 值分別為 1.2、2.5、3.0 和 5.7 nM。Erdafitinib 對與FGFR 密切相關(guān)的 VEGFR2 激酶的抑制作用較弱 (與 FGFR1 相比效力低 30 倍)，其 IC50 值為 36.8 nM。Erdafitinib 與 FGFR 1、3、4 和 2 的結(jié)合 Kd 值分別為 0.24、1.1、1.4 和 2.2 nM。與 VEGFR2 的結(jié)合 Kd 值較高，為 6.6 nM。Erdafitinib 對表達(dá) FGFR1、3 和 4 的細(xì)胞的增殖具有抑制作用，其 IC50 值分別為 22.1、13.2 和 25 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

在來自具有 FGFR 激活突變的人類腫瘤細(xì)胞系或患者來源的腫瘤組織的異種移植模型中，給予 Erdafitinib 會產(chǎn)生強(qiáng)效且劑量依賴性的抗腫瘤活性，并伴有腫瘤中磷酸化 FGFR 和磷酸化 ERK 的藥動學(xué)調(diào)節(jié)[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 號
性狀

固體

顏色

Light yellow to yellow

中文名稱

厄達(dá)替尼
運(yùn)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 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 62.5 mg/mL (139.97 mM; 超聲助溶; 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(zhì)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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)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

動物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

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

  • 方案 二

    請依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in Saline)

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

動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)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(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.66%

參考文獻(xiàn)
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.
參考文獻(xiàn)

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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
Erdafitinib
目錄號：
HY-18708
需求量：