CCT128930是一种有效的,ATP竞争性的,选择性的Akt2抑制剂,IC50为6 nM,作用于Akt2比作用于紧密相关的PKA激酶选择性高28倍。
CCT128930是一种有效的,ATP竞争性的,选择性的Akt2抑制剂,IC50为6 nM,作用于Akt2比作用于紧密相关的PKA激酶选择性高28倍。CCT128930 作用于AKT2比作用于紧密相关的PKA激酶选择性高28倍,比作用于 p70S6K 选择性高20倍。CCT128930作用于PTEN缺乏的人类肿瘤细胞系,包括U87MG人类恶性胶质瘤细胞,LNCaP人类前列腺癌细胞和PC3人类前列腺癌细胞,具有显著的抗增殖活性,GI50分别为6.3 μM, 0.35 μM 和 1.9 μM。而且, CCT128930 作用于PTEN-null U87MG人类恶性胶质瘤细胞,使细胞周期停在G1期,且阻断AKT通路。
体外实验* | |
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细胞系 | U87MG, LNCaP and PC3 cells |
方法 | Cells are seeded in 96-well plates and allowed to attach for 36 hours to ensure exponential growth prior to treatment. In vitro antiproliferative activity is determined using a 96-hour SRB assay. TCA-fixed cells are stained for 30 minutes with 0.4% (wt/vol) SRB dissolved in 1% acetic acid. At the end of the staining period, SRB is removed and cultures are quickly rinsed four times with 1% acetic acid to remove unbound dye. The acetic acid is poured directly into the culture wells from a beaker. This procedure permits rinsing to be performed quickly so that desorption of protein-bound dye does not occur. Residual wash solution is removed by sharply flicking plates over a sink, which ensures the complete removal of rinsing solution. Because of the strong capillary action in 96-well plates, draining by gravity alone often fails to remove the rinse solution when plates are simply inverted. After being rinsed, the cultures are air dried until no standing moisture is visible. Bound dye is solubilized with 10 mM unbuffered Tris base (pH 10.5) for 5 minutes on a gyratory shaker. OD is read in either a UVmax microtiter plate reader or a Beckman DU-70 spectrophotometer. For maximum sensitivity, OD is measured at 564 nm. Because readings are linear with dye concentrations only below 1.8 OD units, however, suboptimal wavelengths are generally used, so that all samples in an experiment remains within the linear OD range. With most cell lines, wavelengths of approximately 490-530 nm works well for this purpose. |
浓度 | 0-18.9 μM |
处理时间 | 48 hours |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
体内实验* | |
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动物模型 | PTEN-null U87MG human glioblastoma cells are injected subcutaneously (s.c.) in the right flank of female CrTacNCr-Fox1nu mice. For HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts, cells are administered s.c. in medium supplemented with M |
配制 | CCT128930 is dissolved in 10% DMSO, 5% Tween 20, and 85% saline |
剂量 | ≤50 mg/kg |
给药处理 | Administered via i.p. |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
分子量 | 341.84 |
分子式 | C18H20ClN5 |
CAS号 | 885499-61-6 |
溶解性(25°C) | DMSO 60 mg/mL |
储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 2.9253 mL | 14.6267 mL | 29.2535 mL |
5 mM | 0.5851 mL | 2.9253 mL | 5.8507 mL |
10 mM | 0.2925 mL | 1.4627 mL | 2.9253 mL |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
[1] Ziyue Guan, et al. CCT128930 is a novel and potent antagonist of TRPM7 channel
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