AZD-3463
AZD-3463 is a potent ALK/IGF1R inhibitor with potential anticancer activity. AZD3463 inhibits neuroblastoma growth by overcoming crizotinib resistance and inducing apoptosis. AZD3463 effectively suppressed the proliferation of NB cell lines with wild type ALK (WT) as well as ALK activating mutations (F1174L and D1091N) by blocking the ALK-mediated PI3K/AKT/mTOR pathway and ultimately induced apoptosis and autophagy. In addition, AZD3463 enhanced the cytotoxic effects of doxorubicin on NB cells. AZD3463 also exhibited significant therapeutic efficacy on the growth of the NB tumors with WT and F1174L activating mutation ALK in orthotopic xenograft mouse models.
1: Wang Y, Wang L, Guan S, Cao W, Wang H, Chen Z, Zhao Y, Yu Y, Zhang H, Pang JC, Huang SL, Akiyama Y, Yang Y, Sun W, Xu X, Shi Y, Zhang H, Kim ES, Muscal JA, Lu F, Yang J. Novel ALK inhibitor AZD3463 inhibits neuroblastoma growth by overcoming crizotinib resistance and inducing apoptosis. Sci Rep. 2016 Jan 20;6:19423. doi: 10.1038/srep19423. PubMed PMID: 26786851; PubMed Central PMCID: PMC4726162.
2: Sampson VB, Vetter NS, Kamara DF, Collier AB, Gresh RC, Kolb EA. Vorinostat Enhances Cytotoxicity of SN-38 and Temozolomide in Ewing Sarcoma Cells and Activates STAT3/AKT/MAPK Pathways. PLoS One. 2015 Nov 16;10(11):e0142704. doi: 10.1371/journal.pone.0142704. PubMed PMID: 26571493; PubMed Central PMCID: PMC4646493.
2: Sampson VB, Vetter NS, Kamara DF, Collier AB, Gresh RC, Kolb EA. Vorinostat Enhances Cytotoxicity of SN-38 and Temozolomide in Ewing Sarcoma Cells and Activates STAT3/AKT/MAPK Pathways. PLoS One. 2015 Nov 16;10(11):e0142704. doi: 10.1371/journal.pone.0142704. PubMed PMID: 26571493; PubMed Central PMCID: PMC4646493.
| Chemical | |
|---|---|
| CAS Num | 1356962-20-3 |
| Chemical Formula | C24H25ClN6O |
| Molecular Weight | 448.95 |
| IUPAC Chemical Name | N-(4-(4-aminopiperidin-1-yl)-2-methoxyphenyl)-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine. |
| Exact Mass | 448.17784 |
| Elemental Analysis | C, 64.21; H, 5.61; Cl, 7.90; N, 18.72; O, 3.56 |
| Synonym | AZD3463; AZD 3463; AZD-3463. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | ClC1=CN=C(NC2=CC=C(N3CCC(N)CC3)C=C2OC)N=C1C4=CNC5=C4C=CC=C5 |
| Biological | |
| Targets and Effects | mTOR inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Light green to green solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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