| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C409110-1ml |
1ml |
现货  |
|
| 英文别名 | 4-(4-chlorobenzyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amine |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | CCT128930 |
| 生化机理 | CCT128930 是一种强效、ATP 竞争性和选择性 Akt2 抑制剂，在无细胞试验中的 IC50 为 6 nM，对 Akt2 的选择性是与之密切相关的 PKA 激酶的 28 倍。CCT128930 可诱导细胞周期停滞、DNA 损伤和自噬，与 Akt 抑制无关。高剂量的 CCT128930 会引发 HepG2 细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
CCT128930 是一种 ATP 竞争性地且选择性的 AKT 抑制剂 (对AKT2 的 IC50 为 6 nM )。CCT128930 通过靶向 AKT 的 Met282 (PKA-AKT嵌合体的 Met173)，对 PKA 激酶 (IC50=168 nM) 具有 28 倍的选择性，对 p70S6K (IC50=120 nM) 具有 20 倍的选择性。具有抗肿瘤活性。 Information CCT128930 is a potent, ATP-competitive and selective inhibitor ofAkt2withIC50of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase. CCT128930 induces cell cycle arrest, DNA damage, andautophagyindependent o CCT128930 exhibits marked antiproliferative activity against PTEN-deficient human tumor cell lines including U87MG human glioblastoma cells, LNCaP human prostate cancer cells and PC3 human prostate cancer cells with GI50 of 6.3 μM, 0.35 μM and 1.9 μM, respectively. Furthermore, CCT128930 causes a G1 arrest in PTEN- U87MG human glioblastoma cells and Akt pathway blockade. In vivo CCT128930 at 25 mg/kg i.p. shows a marked antitumor effect in established PTEN- U87MG human glioblastoma xenografts with a treated:control (T/C) ratio of 48% on day 12. In HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts, CCT128930 at 40 mg/kg also produces a profound antitumor effect with complete growth arrest and a T/C ratio of 29% on day 22. CCT128930 administrated via i.v. reaches a peak concentration of 6.4 μM in plasma and is eliminated with a relatively short half-life, high volume of distribution, and rapid clearance, giving an area under the curve AUC0-∞ of 4.6 μM h. CCT128930 administrated via i.p. leads to the peak plasma drug concentration of 1.3 μM and the corresponding AUC0-∞ of 1.3 μM·h. Oral CCT128930 administration leads to the peak plasma concentration of only 0.43 μM and a correspondingly low AUC0-∞ of 0.4 μM·h. cell lines： Concentrations：0-18.9 μM Incubation Time：48 hours Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C1CN(CCC1(CC2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4 |
| 分子量 | 341.84 |
| Reaxy-Rn | 12598617 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12598617&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 56 mg/mL (198.88 mM); Water: 19 mg/mL (67.47 mM); Ethanol: 4 mg/mL (14.2 mM); |
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