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Mobocertinib

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Chemical Structure| 1847461-43-1 同义名 : TAK-788;AP32788;​TAK-788
CAS号 : 1847461-43-1
货号 : A1263841
分子式 : C32H39N7O4
纯度 : 98%
分子量 : 585.7
MDL号 : MFCD32669806
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(42.68 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • EGFR/ErbB1
描述 EGFR is a member of the ErbB family of structurally related RTKs (receptor tyrosine kinases), consisting of the EGFR (ErbB1), as well as human epidermal growth factor receptor 2 (ErbB2; HER2), ErbB3 (HER3) and ErbB4 (HER4). Aberrant ErbB family signaling is implicated in the development and progression of many human cancers, including NSCLC (non-small cell lung cancer)[1]. Mobocertinib is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions. It inhibits wide-type EGFR with an IC50 value of 35 nM and all 14 mutant variants of EGFR with IC50s ranging from 2.4 to 22 nM, and all 6 mutant variants of HER2 with IC50s ranging from 2.4 to 26 nM. 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, mobocertinib (once daily oral dosing at 30 - 100 mg/kg) induced regression of tumors[2]. In a phaseI/II study of the EGFR/HER2 TKI, mobocertinib, in patients with advanced NSCLC refractory to standard therapy, the partial response (PR) rate was 21%, with 64% disease control rate[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.71mL

0.34mL

0.17mL

8.54mL

1.71mL

0.85mL

17.07mL

3.41mL

1.71mL
参考文献

[1]Masood A, Kancha RK, Subramanian J. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in non-small cell lung cancer harboring uncommon EGFR mutations: Focus on afatinib. Semin Oncol. 2019;46(3):271-283

[2]AP32788, a potent, selective inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, in preclinical models