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PHA-848125

目录号 M3519 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


Milciclib (PHA-848125)是一种有效的,ATP竞争性CDK抑制剂,作用于CDK2,IC50为45 nM,作用于CDK2比作用于CDK1, 2, 4, 5和7选择性高3倍以上。

PHA-848125结构式

别名:Milciclib

包装 价格 库存状态
5mg 原价 ¥ 1890
促销价 ¥ 1795.5
中国库存现货
10mg 原价 ¥ 2880
促销价 ¥ 2736
中国库存现货
50mg 原价 ¥ 7920
促销价 ¥ 7524
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
  • 当前批次:
  • 纯度 >98%
  • COA
  • MSDS
生物活性

Milciclib (PHA-848125)是一种有效的,ATP竞争性CDK抑制剂,作用于CDK2,IC50为45 nM,作用于CDK2比作用于CDK1, 2, 4, 5和7选择性高3倍以上。PHA-848125有效抑制细胞周期蛋白(cyclin)A/CDK2, IC50为45 nM,PHA-84812为ATP竞争性抑制剂。PHA-848125也抑制cyclin H/CDK7,cyclin D1/CDK4,p35/CDK5,cyclin E/CDK2,及cyclin B/CDK1活性,IC50 分别为of 0.15, 0.16, 0.265, 0.363, 0.398 μM。PHA-848125作用于大部分对PHA-848125敏感的细胞系时,诱导细胞周期停在G1期,这种抑制存在浓度依赖性。

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 Melanoma cells
方法 Suspending melanoma cells in culture media at a concentration of 2 × 104 cells/mL, dispensing in 50 μL aliquots into flat-bottom 96-well plates and allowed to adhere overnight at 37 °C. Then adding Graded amounts of PHA-848125 or TMZ to the wells (4 wells per point) in 50 μL of CM and incubating the plates at 37 °C in a 5% CO2 humidified atmosphere for 5 days. The cytotoxic effects of TMZ are also evaluated in combination with the MGMT inhibitor BG. To this end, adding 10 μM BG to the plates 2 hours before TMZ and left in culture for the entire period of cell exposure to the drug. ContS1017rol groups are represented by untreated cells and cells treated with BG or DMSO alone. The growth of the cells treated with BG or DMSO alone does not differ from that of untreated cells. MGMT activity of BG-treated cells is undetectable 2 hours after the addition of the inhibitor PHA-848125 and remained essentially undetectable up to the end of the assay. Normal melanocytes are suspended in MGM at the concentration of 1.6 × 105 cells/mL, plated (50 μL/well) and exposed to TMZ + BG or to PHA-848125 as described for melanoma cells. At the end of the incubation period, using the MTT assay to evaluate cell growth . Briefly, 0.1 mg of MTT (in 20 μL of PBS) is added to each well and cells are incubated at 37 °C for 4 hours. Cells are then lysed with a buffer (0.1 mL/well) containing 20% SDS and 50% N,N-dimethylformamide, pH 4.7. After overnight incubation, the absorbance is read at 595 nm using a 3550-UV microplate reader. Cell sensitivity to drug treatment is expressed in terms of IC50 (drug concentration producing 50% inhibition of cell growth, calculated on the regression line in which absorbance values at 595 nm are plotted against the logarithm of drug concentration).
浓度 5.7 mg/mL
处理时间 2 hours
动物实验
动物模型 K-Ras(G12D)LA2 mice
配制 5% dextrose solution
剂量 40 mg/kg twice daily for 10 days
给药处理 Oral administration
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 豚鼠 仓鼠
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,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据
分子量 460.57
分子式 C25H32N8O
CAS号 802539-81-7
纯度 >98%
溶解性(25°C) DMSO 90 mg/mL
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
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 2.1712 mL 10.8561 mL 21.7122 mL
5 mM 0.4342 mL 2.1712 mL 4.3424 mL
10 mM 0.2171 mL 1.0856 mL 2.1712 mL
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关键词:PHA-848125, Milciclib, PHA-848125供应商, CDK抑制剂, 购买PHA-848125, PHA-848125结构式

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