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

Mobocertinib mesylate  (Synonyms: 莫博替尼甲磺酸盐; TAK-788 mesylate; AP32788 mesylate)

目录号: HY-135815B
产品使用指南

摩尔计算器

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

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Mobocertinib mesylate Chemical Structure

Mobocertinib mesylate Chemical Structure

CAS No. : 2389149-85-1

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Mobocertinib mesylate 的其他形式现货产品:

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Mobocertinib mesylate 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

HER2

 

EGFR exon 20 insertion

 

EGFR (WT)

 

体外研究
(In Vitro)

Mobocertinib mesylate (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50 of 21 nM[1].
Mobocertinib mesylate (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 mesylate (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells[1].
Mobocertinib mesylate (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling[1].
Mobocertinib mesylate (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 mesylate 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 mesylate (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: 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

681.80

Formula

C33H43N7O7S
CAS 号
中文名称

莫博替尼甲磺酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Mobocertinib mesylate 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Mobocertinib2389149-85-1TAK-788AP32788莫博替尼甲磺酸盐TAK788TAK 788AP 32788AP-32788EGFREpidermal growth factor receptorErbB-1HER1NSCLCEGFRex20insLU0387A431HCC827HCC4011H1975CUTO14Inhibitorinhibitorinhibit

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