MobocertinibMobocertinib
MedChemExpress (MCE)
HY-135815
1847461-43-1
TAK-788
AP32788
99.60%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
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.
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].
Mobocertinib (3, 10, 30 mg/kg
p.o.
once daily for 20 days) significantly induces tumor growth inhibition[1].
EGFR (WT) EGFR exon 20 insertion HER2
| | | |
| | | | | |
[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. [Content Brief]
[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. [Content Brief]