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RO-3306

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Chemical Structure| 872573-93-8 同义名 : -
CAS号 : 872573-93-8
货号 : A138869
分子式 : C18H13N3OS2
纯度 : 98%
分子量 : 351.445
MDL号 : MFCD17392573
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(71.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 20 mg/mL suspension

生物活性
靶点

  • CDK1

    CDK1, Ki:20 nM
描述 The CDKs (cyclin dependent kinases), as direct regulators of specific phases of the cell cycle, can control cellular proliferation and transcription with their activating cyclin partners and subunit inhibitors. CDK1, through forming complex with Cyclin A or B can trigger S-G2 and G2 to M transitions and G2 progression. RO-3306 is a selective CDK1 inhibitor with Ki value of 20nM (by the IMAP assay). Ro 3306 can reversibly arrest human cells at the G2/M border of the cell cycle and allows for effective cell synchronization in early mitosis. Treatment with 9uM RO-3306 for 20h caused significant decreased protein level of Cyclin E after 8h release from the nocodazole block, as well as Cyclin A and Cyclin B1 after 12h release from the nocodazole block, in HeLa cells synchronized in mitosis by a shake-off after 14 h of incubation in 100nM nocodazole (Cell transition through the G1 and S phase), without significantly affect cellular CDK2 and CDK4 function. HeLa cells traversed normally through the S phase in the presence of 9uM RO-3306 and effectively accumulated in the G2/M phase. Inhibition of CDK1 activity by 9uM RO-3306 forced HeLa cells in prometaphase to exit mitosis without cell division as indicated by the rapid disappearance of phosphohistone-H3 and chromatin decondensation, as well as rapid transition of Mcm2 from the soluble fraction to chromatin. Compared with MCF10A and MCF12A cells, treatement with 9 uM RO-3306 induced larger proapoptotic fraction, which showed that RO-3306 appeared to be more proapoptotic in cancer cells and may have utility as anticancer agents[1]. Combinatorial treatment RO3306 4mg/kg plus sorafenib 30mg/kg could suppress the tumor growth in hepatocellular carcinoma PDX models[2].
作用机制 Ro 3306 is an ATP-competitive CDK1 inhibitor. [1]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human 5637 cell Growth inhibition assay Inhibition of human 5637 cell growth in a cell viability assay, IC50=3.08532 μM SANGER
human 639-V cell Growth inhibition assay Inhibition of human 639-V cell growth in a cell viability assay, IC50=2.27537 μM SANGER
human 8505C cell Growth inhibition assay Inhibition of human 8505C cell growth in a cell viability assay, IC50=7.99817 μM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.28mL

14.23mL

2.85mL

1.42mL

28.45mL

5.69mL

2.85mL
参考文献

[1]Vassilev LT, Tovar C, et al. Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1. Proc Natl Acad Sci U S A. 2006 Jul 11;103(28):10660-5. Epub 2006 Jul 3.

[2]Wu CX, Wang XQ, et al. Blocking CDK1/PDK1/β-Catenin signaling by CDK1 inhibitor RO3306 increased the efficacy of sorafenib treatment by targeting cancer stem cells in a preclinical model of hepatocellular carcinoma. Theranostics 2018; 8(14):3737-3750.