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| CHEMICAL INFORMATION | |||
|---|---|---|---|
| Name | Lorlatinib (PF-06463922) | CAS No. | 1454846-35-5 |
| CAT No. | YD0001 | Storage | 3 years -20°C powder |
| Formula | C21H19FN6O2 | 2 years -80°C in solvent | |
| Molecular | 406.41 | Purity | 99% |
| Description | PF-06463922 is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. Phase 1. | ||
| In vitro | In rats, PF-06463922 displays low plasma clearance, a moderate volume of distribution, a reasonable half-life, low propensity for p-glycoprotein 1-mediated efflux and a bioavailability of 100%. [1] In vivo, PF-06463922 shows cytoreductive antitumor efficacy in the NIH3T3 xenograft models expressing human CD74-ROS1 and Fig-ROS1 via inhibition in ROS1 phosphorylation and the downstream signaling molecules, as well as inhibition of the cell cycle protein Cyclin D1 in tumors. [2] In vivo, PF-06463922 also demonstrates marked antitumor activity in mice bearing tumor xenografts expressing EML4-ALK, EML4-ALK-L1196M, EML4-ALK-G1269A, EML4-ALK-G1202R or NPM-ALK. [3] | ||
