SNS-032是CDK 9,2和7的抑制剂,IC50分别为4,38和62 nM。
SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. Phase 1.
0-0.5 mM
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,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Chen R, et al. Blood, 2009, 113(19): 4637-45.
[2] Vasiliou, S.; Castaner, R.; Bolos, J. SNS-032 - Cyclin-dependent kinase inhibitor oncolytic Drugs of the Future (2008), 33(11), 932-937.
[3] Jones, Clifford D. Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors Bioorganic & Medicinal Chemistry Letters (2008), 18(24), 6486-6489.
分子式 C17H24N4O2S2 |
分子量 380.53 |
CAS号 345627-80-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mM |
Water <1 mg/mL |
Ethanol 100 mM |
体内溶解度
NCT00446342 | B-lymphoid Malignancies|Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma|Multiple Myeloma | Drug: SNS-032 Injection | Sunesis Pharmaceuticals | Phase 1 | 2007-02-01 | 2012-06-05 |
NCT00292864 | Tumors | Drug: SNS-032 Injection | Sunesis Pharmaceuticals | Phase 1 | 2006-01-01 | 2012-06-05 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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