AZ3146 is a novel and potent Mps1 inhibitor, which was used to probe the role of Mps1's catalytic activity during mitosis. AZ3146 also inhibits FAK, JNK1, JNK2, KSP and Kit. In in vitro kinase assays, AZ3146 inhibited human Mps1Cat with an IC50 (50% inhibitory concentration) of ~35 nM. AZ3146 also efficiently inhibited autophosphorylation of full-length Mps1 immunoprecipitated from human cells. 9-环戊基-2-[[2-甲氧基-4-[(1-甲基哌啶-4-基)氧基]-苯基]氨基]-7-甲基-7,9-二氢-8H-嘌呤-8-酮
CAS 1124329-14-1 MFCD224329141
化学结构图
SMILES: COc1cc(OC2CCN(C)CC2)ccc1Nc1ncc2c(n1)n(C1CCCC1)c(=O)n2C
化学属性
| Mol. Formula | C24H32N6O3 |
|---|---|
| Mol. Weight | 452.55 |
| Appearance | white to off-white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | AZ3146 is a novel and potent Mps1 inhibitor, which was used to probe the role of Mps1's catalytic activity during mitosis. AZ3146 also inhibits FAK, JNK1, JNK2, KSP and Kit. In in vitro kinase assays, AZ3146 inhibited human Mps1Cat with an IC50 (50% inhibitory concentration) of ~35 nM. AZ3146 also efficiently inhibited autophosphorylation of full-length Mps1 immunoprecipitated from human cells. |
|---|---|
| Chemical Name Translation | 9-环戊基-2-[[2-甲氧基-4-[(1-甲基哌啶-4-基)氧基]-苯基]氨基]-7-甲基-7,9-二氢-8H-嘌呤-8-酮 |
| Chemicalbook ID | CB52518786 |
| Formula | C24H32N6O3 |
| Synonym | AZ3146; AZ 3146; AZ-3146 |
| IUPAC Name | 9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one |
| InChIKey | YUKWVHPTFRQHMF-UHFFFAOYSA-N |
| InChI | InChI=1S/C24H32N6O3/c1-28-12-10-17(11-13-28)33-18-8-9-19(21(14-18)32-3)26-23-25-15-20-22(27-23)30(24(31)29(20)2)16-6-4-5-7-16/h8-9,14-17H,4-7,10-13H2,1-3H3,(H,25,26,27) |
| Canonical SMILES | O=C1N(C)C2=CN=C(NC3=CC=C(OC4CCN(C)CC4)C=C3OC)N=C2N1C5CCCC5 |
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- AZ3146 is a novel and potent Mps1 inhibitor, which was used to probe the role of Mps1's catalytic activity during mitosis. AZ3146 also inhibits FAK, JNK1, JNK2, KSP and Kit. In in vitro kinase assays, AZ3146 inhibited human Mps1Cat with an IC50 (50% inhibitory concentration) of ~35 nM. AZ3146 also efficiently inhibited autophosphorylation of full-length Mps1 immunoprecipitated from human cells.
相关文献及参考
- [2]. Liu X, et al. TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells. Oncotarget. 2015 Oct 27;6(33):34309-20.
- [3]. Gurden MD, et al. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer Res. 2015 Aug 15;75(16):3340-54.
- [1]. Hewitt L, et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J Cell Biol. 2010 Jul 12;190(1):25-34.
- [1]. Hewitt L, et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J Cell Biol. 2010 Jul 12;190(1):25-34.
- [2]. Liu X, et al. TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells. Oncotarget. 2015 Oct 27;6(33):34309-20.
- [3]. Gurden MD, et al. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer Res. 2015 Aug 15;75(16):3340-5
