N-(4-(4-Aminopiperidin-1-yl)-2-methoxyphenyl)-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine N-(4-(4-氨基哌啶-1-基)-2-甲氧基苯基)-5-氯-4-(1H-吲哚-3-基)嘧啶-2-胺
CAS 1356962-20-3 MFCD456962203
化学结构图
SMILES: COc1cc(N2CCC(N)CC2)ccc1Nc1ncc(Cl)c(-c2c[nH]c3ccccc23)n1
化学属性
| Mol. Weight | 448.95 |
|---|---|
| Appearance | Light green to green solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name Translation | N-(4-(4-氨基哌啶-1-基)-2-甲氧基苯基)-5-氯-4-(1H-吲哚-3-基)嘧啶-2-胺 |
|---|---|
| Chemical Name | N-(4-(4-Aminopiperidin-1-yl)-2-methoxyphenyl)-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine |
| Formula | C24H25ClN6O |
| Synonym | AZD3463; AZD 3463; AZD-3463. |
| IUPAC Name | N-(4-(4-aminopiperidin-1-yl)-2-methoxyphenyl)-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine. |
| InChIKey | GCYIGMXOIWJGBU-UHFFFAOYSA-N |
| InChI | InChI=1S/C24H25ClN6O/c1-32-22-12-16(31-10-8-15(26)9-11-31)6-7-21(22)29-24-28-14-19(25)23(30-24)18-13-27-20-5-3-2-4-17(18)20/h2-7,12-15,27H,8-11,26H2,1H3,(H,28,29,30) |
| Canonical SMILES | ClC1=CN=C(NC2=CC=C(N3CCC(N)CC3)C=C2OC)N=C1C4=CNC5=C4C=CC=C5 |
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产品应用
- 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.
