| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A408500-1ml |
1ml |
现货  |
|
| 别名 | 亚利桑那州 3146 |
|---|---|
| 英文别名 | 9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | AZ 3146 |
| 生化机理 | AZ3146 是一种选择性 Mps1 抑制剂，IC50 约为 35 nM，有助于 CENP-E（驱动蛋白相关运动蛋白）的招募，对 FAK、JNK1、JNK2 和 Kit 的抑制作用较弱。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | TTK 蛋白激酶抑制剂 |
| 产品介绍 |
AZ3146是单极纺锤体1（Mps1）激酶抑制剂，IC50为35 nM，对FAK，JNK1，JNK2和Kit的抑制性较弱。A potent and selective monopolar spindle 1 (Mps1) kinase inhibitor Information AZ 3146 AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM, contributes to recruitment of CENP-E (kinesin-related motor protein), less potent to FAK, JNK1, JNK2, and Kit. AZ3146 also inhibits FAK, JNK1, JNK2 and Kit. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. Mitotic-specific phospho forms of aurora B and BubR1 are not affected by AZ3146. AZ3146 does not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells treated with nocodazole and 2 μM AZ3146 only delay mitosis briefly and then rereplicate their genomes, indicating that AZ3146 overrides the SAC. AZ3146 also inhibits an already established SAC signal, as after release from a nocodazole block, AZ3146 dramatically accelerates mitotic exit.During an otherwise unperturbed mitosis, AZ3146 reduces the time to complete mitosis from 90 minutes in controls to 32 minutes. Strikingly, ~90% of AZ3146-treated HeLa cells undergo abnormal mitoses, although ~50% enter anaphase without aligning all of their chromosomes, and ~30% exit mitosis without undergoing obvious chromosome segregation. AZ3146 has a dramatic effect on kinetochore localization of Mad2, reducing its levels to ~15%, but its effect on Mad1 is less pronounced, with levels remaining at ~60%. When Mps1 is inhibited by AZ3146 before mitotic entry, subsequent recruitment of Mad1 and Mad2 to kinetochores is abolished. However, if Mps1 is inhibited by AZ3146 after mitotic entry, the Mad1–C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core. In vivo
cell lines：Ba/F3, Molm-13, Molm-14, HL60, AML193, KG-1, KG-1a, THP-1, and RS4;11 Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 3.416 |
|---|---|
| hba_count | 5 |
| HBD Count | 1 |
| Rotatable Bond | 6 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=C(NC2=NC3=C(C=N2)N(C)C(=O)N3C4CCCC4)C=CC(=C1)OC5CCN(C)CC5 |
| 分子量 | 452.55 |
| Reaxy-Rn | 18988740 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18988740&ln= |
| DMSO(mg / mL) Max Solubility | 28 |
|---|---|
| DMSO(mM) Max Solubility | 61.87 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 18988740 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18988740&ln= |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(A408500) | Colorless to light pink liquid |
| Record the entire process by video | Conform |
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