Mobocertinib(Synonyms: TAK-788; AP32788)

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Mobocertinib (Synonyms: TAK-788; AP32788) 纯度: 99.60%

Mobocertinib (TAK-788) 是一种有效的的，具有口服活性的 EGFR 和 HER2 突变的抑制剂，包括外显子 20 的插入，并且选择性高于 WT EGFR。具有抗肿瘤活性。

Mobocertinib(Synonyms: TAK-788; AP32788)

Mobocertinib Chemical Structure

CAS No. : 1847461-43-1

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生物活性

Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity[1][2].

IC50 & Target[1]

EGFR exon 20 insertion

 

HER2

 

EGFR (WT)

35 nM (IC50)

体外研究
(In Vitro)

Mobocertinib (TAK-788) inhibits all 14 mutant variants of EGFR (IC50s=2.4-22 nM), and all 6 mutant variants of HER2 (IC50s=2.4-26 nM), more potently than it inhibited WT EGFR (IC50=35 nM), including all 8 variants with exon 20 activating insertions[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In mice implanted with a patient-derived tumor containing an EGFR exon 20 activating insertion, or with engineered Ba/F3 cells containing a HER2 exon 20 activating insertion, once daily oral dosing of Mobocertinib induced regression of tumors at doses that were well tolerated (30-100 mg/kg)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

585.70

Formula

C32H39N7O4
CAS 号

1847461-43-1
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (42.68 mM; ultrasonic and warming and heat to 80°C)

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
10 mM 0.1707 mL 0.8537 mL 1.7074 mL

*

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, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

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

  • 1.

    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); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.27 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (2.13 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.13 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Francois Gonzalvez, et al. Abstract 2644: AP32788, a potent, selective inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, in preclinical models. April 16-20, 2016; New Orleans, LA.

    [2]. Masood A, et al. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in non-small cell lung cancer harboring uncommon EGFR mutations: Focus on BIBW 2992. Semin Oncol. 2019 Jun;46(3):271-283.

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