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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
CYC065
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1070790-89-4
- 规格：
25mg/10mg/5mg/1mg
| 规格： | 25mg | 产品价格： | ￥4878.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥2965.0 |
| 规格： | 5mg | 产品价格： | ￥2103.0 |
| 规格： | 1mg | 产品价格： | ￥860.0 |
是一种ATP竞争性的CDK2/5/9的抑制剂
| 基本信息 | |
| CAS | No.1070790-89-4 |
| 英文名称 | CYC065 |
| 别名 | Fadracicib |
| 分子式 | C21H31N7O |
| 分子量 | 397.52 |
| 溶解性 | Soluble in DMSO ≥10mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD31693062 |
| SMILES | C[C@@H](O)[C@@H](NC1=NC(NCC2=C(C)C=C(C)N=C2)=C3N=CN(C(C)C)C3=N1)CC |
| InChIKey | DLPIYBKBHMZCJI-WBVHZDCISA-N |
| InChI | InChI=1S/C21H31N7O/c1-7-17(15(6)29)25-21-26-19(18-20(27-21)28(11-24-18)12(2)3)23-10-16-9-22-14(5)8-13(16)4/h8-9,11-12,15,17,29H,7,10H2,1-6H3,(H2,23,25,26,27)/t15-,17+/m1/s1 |
| PubChem CID | 24983461 |
| 靶点 | CDK |
| 通路 | Cell Cycle |
| 背景说明 | CYC065是一种ATP竞争性的CDK2/5/9的抑制剂。 |
| 生物活性 | CYC065 is a second-generation， orally available ATP-competitive inhibitor of CDK2/CDK9 kinases[1] |
| In Vitro | CYC065 blocked cells in the G1 phase of the cell cycle and inhibited cell growth specifically in CCNE1-overexpressing USCs.[1] |
| 细胞实验 | Cyclin E1 knockdown conferred increased resistance to CYC065， whereas CYC065 treatment of xenografts derived from CCNE1-amplified USCs significantly reduced tumour growth.The combination of CYC065 and Taselisib demonstrated synergistic effect in vitro and was significantly more effective than single-agent treatment in decreasing tumour growth in xenografts of CCNE1-amplified/pik3ca-mutated USCs.[1] |
| 细胞实验 | The effect of CYC065 on the viability and IC50 of USC-ARK-1， USC-ARK-2， USC-ARK-7， USC-ARK-4 and USC-ARK-6 USC primary cell lines is determined in flow-cytometry assay. Briefly， tumour cells are plated in six-well plates and treated with a titration of CYC065 concentrations (i.e.， ranging from 100 to 500?nM). After 72?h， cells are harvested， washed and stained with propidium iodide (PI; 5?μg/mL) for flow cytometric counts. The percentage of viable cells is then normalised considering the vehicle-treated cells as 100% viable. Half-maximal inhibitory concentration values are determined using GraphPad Prism5 version 6. For drug combination studies， USC-ARK-1 and USC-ARK-2 cell lines are incubated with the combination of Taselisib and CYC065 at multiple paired concentrations including the IC50， the IC50/2 and the IC50*2 of each cell line to the corresponding drug (i.e.， 10?nM of Taselisib and 198?nM of CYC065 for USC-ARK-1 and 50?nM of Taselisib and 62.5?nM of CYC065 for USC-ARK-2). Synergism is assessed by the combination index (CI). CI values <1 define a synergistic activity of the combination treatment. The CI values are calculated using the CompuSyn software[1]. |
| 动物实验 | The in vivo efficacy of CYC065 used as a single agent is evaluated on xenograft mouse models derived from the CCNE1-amplified USC-ARK-2 USC cell line. Xenografts derived from the CCNE1-amplified， PIK3CA-mutated USC-ARK-1 cell line are used for evaluating the in vivo combination of CYC065 and Taselisib. Briefly， 5-7-week-old SCID mice are injected into the subcutaneous region with USC cells. A minimum of five animals per group are used. Treatments are administrated by oral gavage starting 1 week after tumor implantation when the size of the tumor is 0.125-0.150?cm3. Uterine serous carcinoma-ARK-2-derived xenografts are divided into two groups: one group of animal receive the vehicle， whereas the experimental group receive CYC065 (22.5?mg/kg daily for 3 weeks). Uterine serous carcinoma-ARK-1-derived xenografts are instead divided into four groups: one group receive the vehicle (0.5% methylcellulose-0.2% Tween-80)， one group receive CYC065 (22.5?mg/kg daily for 3 weeks)， one group receive Taselisib (10 mg/kg daily， 5 days per week per 3 weeks) and the last group receive the combination of CYC065 and Taselisib. The size of the tumor at the initiation of treatment is 0.125-0.150?cm3. Mouse weight and tumor size is recorded two times a week for the entire experimental period. Tumor volume is calculated.[1] |
| 数据来源文献 | [1]. Cocco E， et al. Dual CCNE1/PIK3CA targeting is synergistic in CCNE1-amplified/PIK3CA-mutated uterine serous carcinomas in vitro and in vivo. Br J Cancer. 2016 Jul 26;115(3):303-11. |
| 单位 | 支 |
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的DNA含量而分析细胞处于不同的时期的方法。确切的说结果中G1期的百分比实际上是G1+G0期细胞的百分比。 G2的百分比实际上是G2+M期细胞的百分比。 图上最高的峰代表了G1期(也称2倍体峰)，后面的代表G2期、S期(也称4倍体峰)。 1、细胞周期的概念 细胞由一次分裂结束到下一次分裂结束，都要经历相同的变化阶段(即G1→S→G2→M )周而复始地进行活动，细胞的这种生长、分裂循环即称为细胞周期(Cell cyc1e)。一个细胞周期
图上最高的峰代表了G1期（也称2倍体峰），后面的代表G2期、S期（也称4倍体峰）。 1、细胞周期的概念 细胞由一次分裂结束到下一次分裂结束，都要经历相同的变化阶段（即G1→S→G2→M ）周而复始地进行活动，细胞的这种生长、分裂循环即称为细胞周期（cell cyc1e）。一个细胞周期包括有丝分裂期（M）和分裂间期（G1、S、G2）。尽管在各种细胞中各期所占时间都不尽相同，但相对而言M期最短，S期却较长。
DMSO，在脱色摇床上振荡10分钟，然后测吸光值。一般要低于IC50，避免非调亡性杀伤的细胞太多，造成流式细胞仪检测碎片太多。我一般用1/2-1/3的IC50，作用时间为36h。一般肿瘤细胞系空白处理的调亡率应低于1%，用药后一般为5-10%（Annexin V），细胞周期的亚G0峰比较明显。
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IC1720 CYC065 细胞周期 索莱宝
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