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Lorlatinib

CAS No. : 1454846-35-5

MCE 國際站：Lorlatinib

產(chǎn)品活性：Lorlatinib (PF-06463922) 是一種具有口服活性，選擇性,，腦滲透性和 ATP 競爭性的 ROS1/ALK 抑制劑,，具有抗癌活性。Lorlatinib 對于 ROS1,，野生型 ALK 和 ALK^L1196M 的 K_i 分別為 <0.025 nM,，<0.07 nM 和 0.7 nM,。Lorlatinib 靶向 EML-ALK，并抑制 ALK 磷酸化,，IC₅₀ 分別為 15-43 nM (ALK^L1196),，14-80 nM (ALK^G1269A)，38-50 nM (ALK^1151Tins),，77-113 nM (ALK^G1202R),。

研究領(lǐng)域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶點：Anaplastic lymphoma kinase (ALK)  |  ROS Kinase  |  Apoptosis

In Vitro: Lorlatinib (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. Lorlatinib significantly inhibits cell proliferation and induces cell apoptosis in the HCC78 human NSCLC cells harboring SLC34A2-ROS1 fusions and the BaF3-CD74-ROS1 cells expressing human CD74-ROS1. Lorlatinib also shows potent growth inhibitory activity and induces apoptosis in the NSCLC cells harboring either non-mutant ALK or mutant ALK fusions.

In Vivo: In rats, Lorlatinib (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%. In vivo, Lorlatinib 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. Lorlatinib 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.

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