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| | Ack1 inhibitor 1 Basic information |
| Product Name: | Ack1 inhibitor 1 | | Synonyms: | Ack1 inhibitor 1;Benzamide, N-[3-[2-[[2-ethoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-7,8-dihydro-7-oxo-8-[[(2R)-tetrahydro-2-furanyl]methyl]pyrido[2,3-d]pyrimidin-6-yl]phenyl]-3-(trifluoromethyl)- | | CAS: | 2924415-92-7 | | MF: | C39H40F3N7O4 | | MW: | 727.78 | | EINECS: | | | Product Categories: | | | Mol File: | 2924415-92-7.mol |  |
| | Ack1 inhibitor 1 Chemical Properties |
| density | 1.344±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | pka | 12.820±0.70(predicted) |
| | Ack1 inhibitor 1 Usage And Synthesis |
| Uses | Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity[1]. | | in vivo | Ack1 inhibitor 1 (Compound 10zi) (10 mg/kg; PO; single dose) improves AUC value of 1920.56 h ng/mL, Cmax of 119.52 μg/L, and an oral bioavailability of 19.80% in a single oral dose of 10 mg/kg in SD rats[1].
| | References | [1] Li Q, et al. Design, Synthesis, and Evaluation of (R)-8-((Tetrahydrofuran-2-yl)methyl)pyrido[2,3-d]pyrimidin-7-ones as Novel Selective ACK1 Inhibitors to Combat Acquired Resistance to the Third-Generation EGFR Inhibitor. J Med Chem. 2023 May 25;66(10):6905-6921. DOI:10.1021/acs.jmedchem.3c00319 |
| | Ack1 inhibitor 1 Preparation Products And Raw materials |
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