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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.
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Source | Sci Rep (2016). Figure 2. AZD3463 |
| Method | colony formation assay | |
| Cell Lines | NB cells | |
| Concentrations | 5 μM | |
| Incubation Time | 4 hrs | |
| Results | Our data indicates that AZD3463 effectively blocks both anchorage-dependent and independent colony formation of NB cells. |
| Molecular Weight | 448.95 |
| Formula | C24H25ClN6O |
| CAS Number | 1356962-20-3 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ALK Products |
|---|
| AP26113 (Brigatinib)
AP26113 (Brigatinib) is a highly potent ALK inhibitor with IC50 of 0.6 nM. |
| X-376
X-376 is a potent and highly specific ALK small molecule tyrosine kinase inhibitor with IC50 of 0.61 nM. |
| SB431542
SB-431542 is a potent and selective inhibitor of the transforming growth factor-β (TGF-β) type I receptor activin receptor-like kinase ALK5 (IC50 = 94 nM). |
| RepSox
RepSox (ALK5 Inhibitor II) is a potent and ATP-competitive inhibitor of the TGF-β type I receptor ALK5 (IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively). |
| LDN-193189
LDN-193189 is a highly potent small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3. |
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