| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P407796-1ml |
1ml |
现货  |
|
| 英文别名 | N-(6,6-dimethyl-5-(1-methylpiperidine-4-carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-methylbutanamide |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | PHA-793887 |
| 生化机理 | PHA-793887 是一种新型的 CDK2、CDK5 和 CDK7 强效抑制剂，其 IC50 分别为 8 nM、5 nM 和 10 nM。它对 CDK2、5 和 7 的选择性是 CDK1、4 和 9 的 6 倍多。PHA-793887 可诱导细胞周期停滞和细胞凋亡。第一阶段 |
| 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 | 细胞周期蛋白依赖性激酶抑制剂 |
| 产品介绍 |
PHA-793887是一种新型有效的CDK2，CDK5和CDK7抑制剂，IC50分别为8 nM， 5 nM 和10 nM，作用于CDK2， 5，和7比作用于CDK1， 4，和9选择性高6倍以上。a novel pan-Cdk inhibitor inactive against 34 other kinases. Information PHA-793887 is a novel and potent inhibitor ofCDK2,CDK5andCDK7withIC50of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 induces cell-cycle arrest andapoptosis. Phase 1. PHA-793887 has low activity against CDK1, CDK4, CDK9 and GSK3β with IC50 of 60 nM, 62 nM, 138 nM and 79 nM, respectively. PHA-793887 inhibits cell proliferation of many tumor cell lines, including A2780, HCT-116, COLO-205, C-433, DU-145, A375, PC3, MCF-7, and BX-PC3, with IC50 of 88 nM–3.4 μM. PHA-793887 (1 μM) shows a decrease in the S phase, a subsequent increase of the G1 phase and a slight accumulation of G2/M phase in A2780 cells. PHA-793887 (3 μM) significantly increases G2/M phase and reduces DNA synthsis. PHA-793887 is cytotoxic for leukemic cell lines, including K562, KU812, KCL22, and TOM1, with IC50 of 0.3–7 μM, but it is not cytotoxic for normal unstimulated peripheral blood mononuclear cells or CD34+ hematopoietic stem cells. In colony assays, PHA-793887 shows very high activity against leukemia cell lines with IC50 less than 0.1 μM. PHA-793887 induces cell-cycle arrest, inhibits Rb and nucleophosmin phosphorylation, and modulates cyclin E and cdc6 expression at 0.2−1 μM and induces apoptosis at 5 μM. In vivo PHA-793887 (10–30 mg/kg) shows good efficacy in the human ovarian A2780, colon HCT-116, and pancreatic BX-PC3 carcinoma xenograft models. PHA-793887 (20 mg/kg) is effective in xenograft models of K562 and HL60 cells, primary leukemic disseminated model, and a high-burden disseminated ALL-2 model derived from a relapsed Philadelphia-positive acute lymphoid leukemia patient. cell lines： Concentrations：0.1 nM-1 μM, dissolved in DMSO Incubation Time：72 hours Powder Purity:≥95% |
| ALogP | 1 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC(C)CC(=O)NC1=NNC2=C1CN(C2(C)C)C(=O)C3CCN(CC3)C |
| 分子量 | 361.48 |
| Reaxy-Rn | 12049504 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12049504&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 63 mg/mL (199.76 mM); Ethanol: 6 mg/mL (19.02 mM); Water: Insoluble; |
|---|
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