生物活性
Triciribine phosphate (NSC-280594) is a novel potent, small-molecule Akt inhibitor. Triciribine phosphate (NSC-280594) prevents the phosphorylation of Akt. Triciribine phosphate (NSC-280594) disrupts a specific signaling pathway associated with chemoresistance and cancer cell survival in ovarian cancer. Triciribine phosphate (NSC-280594)?in combination with trastuzumab was shown to inhibit cell growth and induce cell death in breast cancer cells that were previously trastuzumab resistant. Triciribine phosphate (NSC-280594) has been demonstrated anti-tumor activity against a wide spectrum of cancers in preclinical and clinical studies. Triciribine phosphate (NSC-280594) is a nucleotide derivative first synthesized by Schram and Townsend.
化学数据
| 分子量 | 400.28 |
| 分子式 | C13H17N6O7P |
| CAS号 | 61966-08-3 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 10 mM |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | CEM-SS cells |
| 方法 | Evaluate Ttriciribine for cytotoxicity by seeding CEM-SS cells at a density of 1 × 104cells/well in growth medium, using a 96-well flat-bottom plate. Serial fivefold dilutions of Triciribine are prepared in growth medium and added to the wells as a second overlay. After a 48-hours incubation at 37 °C, the cells are pulse labeled with [3H]dThd (1 μCi per well, specific activity 20 Ci/mmol) for 6 hours and the cells are harvested to measure total DNA synthesis. |
| 浓度 | 0-500 μM |
| 处理时间 | 48 hours |
| 动物实验 |
|---|
| 动物模型 | OVCAR3, OVCAR8, PANC1, OVCAR5 and COLO357 tumor cells are injected s.c. into 80week-old female nude mice. |
| 配制 | Triciribine is dissolved in 20% DMSO. |
| 剂量 | 1 mg/kg/day |
| 给药处理 | Triciribine is administrated through i.p. injection once a day. |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 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。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4983 mL | 12.4913 mL | 24.9825 mL |
| 5 mM | 0.4997 mL | 2.4983 mL | 4.9965 mL |
| 10 mM | 0.2498 mL | 1.2491 mL | 2.4983 mL |
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