Lorlatinib acetate
| CAS No. | 1924207-18-0 | Cat. No. | BCP23509 |
| Name | Lorlatinib acetate | ||
| Synonyms | PF 06463922 acetate; PF-06463922 acetate; PF06463922 acetate; | ||
| Formula | C23H23FN6O4 | M. Wt | 466.47 |
| Description | PF-06463922 demonstrates significant cell activity against ALK and a large set of ALK clinical mutations with IC50 ranging from 0.2 nM-77 nM. PF-06463922 exhibited subnanomolar cellular potency against oncogenic ROS1 fusions and inhibited the crizotinib-refractory ROS1(G2032R) mutation and the ROS1(G2026M) gatekeeper mutation. Compared with crizotinib and the second-generation ALK/ROS1 inhibitors ceritinib and alectinib, PF-06463922 showed significantly improved inhibitory activity against ROS1 kinase. in vivo: PF-06463922 showed marked antitumor activity in tumor models expressing FIG-ROS1, CD74-ROS1, and the CD74-ROS1(G2032R) mutation. Furthermore, PF-06463922 demonstrated antitumor activity in a genetically engineered mouse model of FIG-ROS1 glioblastoma. | ||
| Pathways | Angiogenesis/Protein Tyrosine Kinase | ||
| Targets | ALK | ||
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GSK3 inhibition circumvents and overcomes acquired lorlatinib resistance in ALK-rearranged non-small-cell lung cancer
Publications Citing of Biochempartner's Lorlatinib acetate(CAS:1924207-18-0) |
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Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer
Publications Citing of Biochempartner's Lorlatinib acetate(CAS:1924207-18-0) |
Structure
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