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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
718630-59-2
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥716.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥361.0 |
| 规格： | 5 mg | 产品价格： | ￥900.0 |
| 规格： | 10 mg | 产品价格： | ￥1450.0 |
| 规格： | 25 mg | 产品价格： | ￥2813.0 |
| 规格： | 50 mg | 产品价格： | ￥4350.0 |
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PHA-793887
CAS No. : 718630-59-2
MCE 国际站：PHA-793887
产品活性：PHA-793887 是一种有效的，ATP 竞争性的 CDK 抑制剂，可抑制 Cdk2，Cdk1，Cdk4 和 Cdk9 的活性，IC50 值分别为 8 nM，60 nM，62 nM 和 138 nM，同时可抑制糖原合酶激酶 3β (GSK-3β)，IC50 值为 79 nM。
研究领域：Cell Cycle/DNA Damage | Apoptosis
In Vitro: PHA-793887 partially inhibits Rb phosphorylation at 1 μM and almost completely at 3 μM, in A2780 tumor cell line. PHA-793887 (1 μM) partially inhibits phosphorylation of the Cdk2 substrates Rb and NPM in A2780 tumor cell line. PHA-793887 (6 μM) significantly inhibits Rb and NPM phosphorylation in MCF7 cell line. PHA-793887 shows cytotoxic activities against leukemic cell lines in vitro, with IC50 ranging from 0.3 to 7 μM. In colony assays, PHA-793887 is highly cytotoxic for leukemia cell lines, with an IC50 <0.1 μM. PHA-793887 induces cell-cycle arrest, inhibits Rb and nucleophosmin phosphorylation, and modulates cyclin E and cdc6 expression at low doses of 0.2 to 1 μM and induces apoptosis at the highest dose of 5 μM. PHA-793887 is a novel inhibitor of several cdk, including cdk1, cdk2, cdk4, cdk5, cdk7, and cdk9 with IC50 in the 5 to 140 nM range.
In Vivo: PHA-793887 induces tumor growth inhibition in the range of 50% at dose of 15 mg/kg to 75% at dose of 30 mg/kg in CD-1 nude mice. PHA-793887 (30 mg/kg, i.v.) also induces significant downregulation of the 58-gene panel in the skin of CD-1 mice. PHA-793887 (20 mg/kg, i.v.) induces tumor regression in the HL60 model. In the K562 model, PHA-793887 significantly reduces tumor growth. Moreover, PHA-793887 (20 mg/kg, i.v.) inhibits human primary leukemia growth in engraftment setting in vivo.
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文献和实验频率。1.4 0.075 mol/L 氯化钾溶液5.59 g 氯化钾加蒸馏水至 1000 ml。 1.5 固定液甲醇: 冰醋酸为 3:1，临用前配制。1.6 姬姆萨 (Giemsa) 染液取姬姆萨染料 3.8 g ，置乳钵中，加少量甲醇研磨。逐渐加甲醇至 375 mL，待完全溶解后，再加 125 mL 甘油，放入 37° C 温箱中保温 48 h。保温期间振摇数次，使充分溶解。取出过滤，2 周后使用，作为姬姆萨染液原液。使用时, 取 1 份姬姆萨染液原液，与 9 份 1 / 15 mol
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