AZD3463 is a novel inhibitor of ALK which overcomes multiple mechanisms of acquired resistance to crizotinib. AZD3463 inhibits ALK with a Ki value of 0.75 nM. AZD3463 dose-dependently inhibits pALK in tumor xenografts in vivo, resulting in stasis (H3122) or regression (DEL, H2228) in tumor volume. AZD3463 obtains equivalent potency to mutantL1196M and wild-type ALK in vivo.
|Source||Sci Rep (2016). Figure 2. AZD3463|
|Method||colony formation assay|
|Cell Lines||NB cells|
|Incubation Time||4 hrs|
|Results||Our data indicates that AZD3463 effectively blocks both anchorage-dependent and independent colony formation of NB cells.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mg/mL|
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LDK378 2Hcl (Ceritinib) is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.
Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2.
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Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
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