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TAK-788
- Mobocertinib - AP32788
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C32H39N7O4
- MW: 585.7
Description
TAK-788 is a potent and selective dual EGFR/HER2 tyrosine kinase inhibitor. Specifically, TAK-788 inhibited all 14 mutant variants of EGFR (IC50 values between 2.4 and 22 nM), and all 6 mutant variants of HER2 (IC50 values between 2.4 and 26 nM), more potently than it inhibited WT EGFR (IC50 value of 35 nM), including all 8 variants with exon 20 activating insertions.
More Information
| Parent CAS No. | 1847461-43-1 |
|---|---|
| Chemical Name | Isopropyl 2-(5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenylamino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate |
| SMILES | C1(OC)C(NC2N=CC(C(=O)OC(C)C)=C(C3C4C=CC=CC=4N(C)C=3)N=2)=CC(NC(=O)C=C)=C(N(C)CCN(C)C)C=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C32H39N7O4/c1-9-29(40)34-24-16-25(28(42-8)17-27(24)38(6)15-14-37(4)5)35-32-33-18-22(31(41)43-20(2)3)30(36-32)23-19-39(7)26-13-11-10-12-21(23)26/h9-13,16-20H,1,14-15H2,2-8H3,(H,34,40)(H,33,35,36) |
| InChiKey | AZSRSNUQCUDCGG-UHFFFAOYSA-N |
| CID | 118607832 |
| Short Description | EGFR/HER2 inhibitor |
References
- G Gonzalvez et al. Abstract 2644: AP32788, a potent, selective inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, in preclinical models. Proceedings: AACR 107th Annual Meeting 2016; April 16-20, 2016; New Orleans, LA.
- A Masood et al. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in non-small cell lung cancer harboring uncommon EGFR mutations: Focus on afatinib. Semin Oncol. 2019 Jun;46(3):271-283.
- RW Madison et al. Urothelial cancer harbours EGFR and HER2 amplifications and exon 20 insertions. BJU Int. 2020 May;125(5):739-746.
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