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Chemical Structure : Mobocertinib
CAS No.: 1847461-43-1
Catalog No.: PC-73153Not For Human Use, Lab Use Only.
Mobocertinib (TAK-788) is a potent, mutant-selective, irreversible inhibitor of EGFR ex20ins mutations with IC50 of 2.7 to 22.5 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg (Free Sample) | $28 | In stock | |
| 50 mg | $98 | In stock | |
| 100 mg | $148 | In stock | |
| 500 mg | $298 | In stock | |
| 1 g | Get quote |
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Mobocertinib (TAK-788) is a potent, mutant-selective, irreversible inhibitor of EGFR ex20ins mutations with IC50 of 2.7 to 22.5 nM.
Mobocertinib (TAK-788) displays selectivity over WT EGFR (IC50=34.5 nM).
Mobocertinib (TAK-788) inhibited all five variants of EGFR ex20ins mutations with IC50 of 4.3 nM for NPG, 10.9 nM for ASV, 11.8 nM for A763_Y764insFQEA (FQEA), 18.1 nM for N771_H773dupNPH (NPH), and 22.5nM for S768_D770dupSVD.
Mobocertinib (TAK-788) inhibited viability of various EGFRex20ins-driven cell lines more potently (CUTO14 cell viability assay, IC50=33 nM) than approved EGFR TKIs and demonstrated in vivo antitumor efficacy in patient-derived xenografts and murine orthotopic models.
| M.Wt | 585.709 | |
| Formula | C32H39N7O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO (5.85 mg/mL) |
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| Chemical Name/SMILES |
Isopropyl 2-((5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenyl)amino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate |
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1. Han H, et al. Cancer Res. 2021 Oct 15;81(20):5311-5324.
2. Zhang SS, et al. Lung Cancer (Auckl). 2021 Jul 12;12:61-65.
3. Gonzalvez F, et al. Cancer Discov. 2021 Jul;11(7):1672-1687.
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