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。

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.

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EGFR (WT) EGFR exon 20 insertion

Mobocertinib (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50 of 21 nM.
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)).
Mobocertinib (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells.
Mobocertinib (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling.
Mobocertinib (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20), Ba/F3 (HER2 exon 20) cells. has not independently confirmed the accuracy of these methods. They are for reference only.

Mobocertinib (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Athymic Nude-Foxn1 m

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Gonzalvez F, et al. Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer. Cancer Discov. 2021 Jul;11(7):1672-1687.
[2]. Han H, et al. Targeting HER2 Exon 20 Insertion-Mutant Lung Adenocarcinoma with a Novel Tyrosine Kinase Inhibitor Mobocertinib. Cancer Res. 2021 Oct 15;81(20):5311-5324.

In Vitro: DMSO : 25 mg/mL (42.68 mM; ultrasonic and warming and heat to 80°C)配制储备液