2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Mobocertinib

Mobocertinib  (Synonyms: 莫博替尼; TAK-788; AP32788)

目录号: HY-135815 纯度: 99.60%
COA 产品使用指南

摩尔计算器

Mobocertinib (TAK-788) 是一种口服有效并且不可逆的 EGFR/HER2 抑制剂。Mobocertinib 能选择性地 (相较于野生型 EGFR) 抑制含有 EGFRex20ins 的致癌突变体。Mobocertinib 可用于 NSCLC 的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Mobocertinib Chemical Structure

Mobocertinib Chemical Structure

CAS No. : 1847461-43-1

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
1 mg ￥120
In-stock
5 mg ￥230
In-stock
10 mg ￥360
In-stock
25 mg ￥720
In-stock
50 mg ￥1150
In-stock
100 mg ￥1850
In-stock
500 mg ￥4850
In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Mobocertinib:

Mobocertinib 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research[1][2].

IC50 & Target[1]

EGFR (WT)

 

EGFR exon 20 insertion

 

HER2

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 EC50
1676 nM
Compound: 2
Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
[PMID: 37197473]
BaF3 EC50
1.1 nM
Compound: 2
Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
[PMID: 37197473]
BaF3 IC50
1.9 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
10.1 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
1062.9 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
1133.7 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
2168.1 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
27.1 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 EC50
2711 nM
Compound: 2
Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
[PMID: 37197473]
BaF3 IC50
3814.5 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
3946 nM
Compound: 21c; TAK-788
Anticancer activity against parental mouse BaF3 cells assessed as cell viability incubated for 3 days by Cell Titer-Glo assay
Anticancer activity against parental mouse BaF3 cells assessed as cell viability incubated for 3 days by Cell Titer-Glo assay
[PMID: 36423823]
BaF3 IC50
47.6 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
5 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
8.3 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
8.9 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
BaF3 IC50
9 nM
Compound: Mobocertinib
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
[PMID: 36384036]
体外研究
(In Vitro)

Mobocertinib (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50 of 21 nM[1].
Mobocertinib (2 h) potently inhibits EGFR with common activating mutations (HCC827 (D), HCC4011 (L)) or with a T790M mutation (H1975 (LT)) more potently than WT EGFR (A431 (WT))[1].
Mobocertinib (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells[1].
Mobocertinib (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling[1].
Mobocertinib (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells[2].

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

Mobocertinib 相关抗体:

Cell Viability Assay[1]

Cell Line: LU0387 (NPH) cells
Concentration: 1.5 nM-10 μM
Incubation Time: 7 days
Result: Showed good inhibition activity for LU0387 (NPH) cells with IC50 of 21 nM.

Cell Viability Assay[1]

Cell Line: A431 (WT), HCC827 (D), HCC4011 (L), H1975 (LT) cells
Concentration:
Incubation Time: 2 h
Result: Inhibited EGFR with common activating mutations of HCC827 (D), HCC4011 (L) cells and T790M mutation of H1975 (LT) with IC50s of 4, 1.3 and 9.8 nM respectively, which more potently than WT EGFR (A431 (WT); IC50 of 35 nM).

Western Blot Analysis[1]

Cell Line: CUTO14 (ASV) cells
Concentration: 0.1 nM-1 μM
Incubation Time: 6 h
Result: Robustly inhibited EGFR signaling, reaching 80% and 100% inhibition of phosphorylated EGFR (pEGFR) at concentrations of 100 nM and 1 μM, respectively.

Western Blot Analysis[1]

Cell Line: HCC827 (D), HCC4011 (L), H1975 (LT) cells
Concentration: 0.3 nM-1 μM
Incubation Time: 6 h
Result: Potently inhibited EGFR and downstream signaling in HCC827 (D), HCC4011 (L) and H1975 (LT) cells.

Western Blot Analysis[2]

Cell Line: H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells
Concentration: 0.01, 0.1 and 1 μM
Incubation Time: 6 h
Result: Inhibited HER2 signaling in H1781 and Ba/F3-HER2 exon 20YVMA mutant cells at 0.1 μM with significantly decreased phosphorylations of HER2, AKT, and ERK1/2 in a dose-dependent manner.
体内研究
(In Vivo)

Mobocertinib (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition[1].

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

Animal Model: Female Athymic Nude-Foxn1nu mice (human NSCLC H1975 LT tumor model)[1].
Dosage: 3, 10, 30 mg/kg
Administration: Oral; once daily for 20 days.
Result: Decreased the mean tumor volume by 44% and 92% when at 3 mg/kg and 10 mg/kg, respectively, relative to the tumor size of vehicle group.
Induced a 76% tumor regression relative to the pretreatment tumor size at 30 mg/kg.
Clinical Trial
分子量

585.70

Formula

C32H39N7O4
CAS 号
性状

固体

颜色

Off-white to light yellow

中文名称

莫博替尼
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 : 25 mg/mL (42.68 mM; 超声助溶 (<80°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 1.7074 mL 8.5368 mL 17.0736 mL
5 mM 0.3415 mL 1.7074 mL 3.4147 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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.27 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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% Corn Oil

    Solubility: ≥ 1.25 mg/mL (2.13 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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： 0.5% CMC/saline water

    Solubility: 25 mg/mL (42.68 mM); 悬浊液; 超声助溶

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: 99.60%

COA (202 KB) HNMR (338 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献

Mobocertinib 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 1.7074 mL 8.5368 mL 17.0736 mL 42.6840 mL
5 mM 0.3415 mL 1.7074 mL 3.4147 mL 8.5368 mL
10 mM 0.1707 mL 0.8537 mL 1.7074 mL 4.2684 mL
15 mM 0.1138 mL 0.5691 mL 1.1382 mL 2.8456 mL
20 mM 0.0854 mL 0.4268 mL 0.8537 mL 2.1342 mL
25 mM 0.0683 mL 0.3415 mL 0.6829 mL 1.7074 mL
30 mM 0.0569 mL 0.2846 mL 0.5691 mL 1.4228 mL
40 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0671 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:

Mobocertinib1847461-43-1TAK-788 AP32788莫博替尼TAK788TAK 788AP32788AP 32788AP-32788EGFREpidermal growth factor receptorErbB-1HER1NSCLCEGFRex20insLU0387A431HCC827HCC4011H1975CUTO14Inhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
Mobocertinib
目录号：
HY-135815
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z