CAS NO: | 1070790-89-4 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor ofCDK2/CDK9kinases[1]withIC50s of 5 and 26 nM, respectively[2]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Fadraciclib blocks cells in the G1 phase of the cell cycle and inhibits cell growth specifically in cyclin E1 (CCNE1)-overexpressing uterine serous carcinomas (USCs). USC cell lines expressing high CCNE1 mRNA and protein levels to be significantly more sensitive to treatment with Fadraciclib in vitro when compared with low CCNE1-expressing cell lines (IC50: mean±s.d.=124.1±57.8 nM in CCNE1-overexpressing USC cell lines vs 415±117.5 nM in CCNE1 low expressors, respectively; P=0.0003). Importantly, low concentrations of Fadraciclib (i.e., 100 nM) causes an arrest in the G1 phase of the cell cycle only in the CCNE1-overexpressing USC cell lines (i.e., USC-ARK-2, USC-ARK-7)[1]. | ||||||||||||||||
体内研究 (In Vivo) | To evaluate the therapeutic potential of Fadraciclib as a single agent, USC-ARK-2-derived xenografts are treated daily with Fadraciclib (22.5 mg/kg) for a 3-week period. Tumor size and mouse weight are recorded two times a week. The daily administration of Fadraciclib results in a significant reduction of tumor growth compared with the vehicle-treated mice (P=0.012 starting at day 9 of the treatment). No significant weight loss is reported during the entire treatment period[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 397.52 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H31N7O | ||||||||||||||||
CAS 号 | 1070790-89-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(251.56 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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