|(Z)-5-(喹啉-6-基亚甲基)-2-((噻吩-2-基甲基)氨基)噻唑-4(5H)-酮|CsnPharm

CAS No.: 872573-93-8

(Z)-5-(Quinolin-6-ylmethylene)-2-((thiophen-2-ylmethyl)amino)thiazol-4(5H)-one Catalog No. CSN16564

Synonyms: Ro-3306Ro-3306

Ro 3306 is a potent and selective inhibitor of CDK1 with Ki value of 35 nM for CDK1/cyclin B1, 10-fold selectivity relative to CDK2/cyclin E and > 50-fold relative to CDK4/cyclin D.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CDK1/cyclin B1

Ki:35nM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT02555787 - - Active, not recruiting March 2023 -

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02555787	-	-	Active, not recruiting	March 2023	-

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8454 mL
- 14.2270 mL
- 28.4539 mL
- 5 mM
- 0.5691 mL
- 2.8454 mL
- 5.6908 mL
- 10 mM
- 0.2845 mL
- 1.4227 mL
- 2.8454 mL

技术信息

CAS号

872573-93-8

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H13N3OS2

运输

蓝冰

分子量

351.45

别名

Ro-3306Ro-3306

溶解度

DMSO	50.0 mg/mL (142.3 mM) warming
Water	insoluble

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

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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
human 8-MG-BA cell	-	Growth inhibition assay	-	Inhibition of human 8-MG-BA cell growth in a cell viability assay， IC50=3.14049 μM	SANGER
human A172 cell	-	Growth inhibition assay	-	Inhibition of human A172 cell growth in a cell viability assay, IC50=5.9079 μM	SANGER
human A253 cell	-	Growth inhibition assay	-	Inhibition of human A253 cell growth in a cell viability assay, IC50=15.2834 μM	SANGER
human A4-Fuk cell	-	Growth inhibition assay	-	Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=2.05604 μM	SANGER
human A549 cell	-	Growth inhibition assay	-	Inhibition of human A549 cell growth in a cell viability assay, IC50=11.206 μM	SANGER
human ALL-PO cell	-	Growth inhibition assay	-	Inhibition of human ALL-PO cell growth in a cell viability assay， IC50=1.90813 μM	SANGER
human BPH-1 cell	-	Growth inhibition assay	-	Inhibition of human BPH-1 cell growth in a cell viability assay, IC50=2.97455 μM	SANGER
human CAL-39 cell	-	Growth inhibition assay	-	Inhibition of human CAL-39 cell growth in a cell viability assay, IC50=7.3524 μM	SANGER
human COR-L23 cell	-	Growth inhibition assay	-	Inhibition of human COR-L23 cell growth in a cell viability assay, IC50=6.3735 μM	SANGER
human COR-L88 cell	-	Growth inhibition assay	-	Inhibition of human COR-L88 cell growth in a cell viability assay, IC50=3.47583 μM	SANGER
human D-566MG cell	-	Growth inhibition assay	-	Inhibition of human D-566MG cell growth in a cell viability assay, IC50=6.78873 μM	SANGER
human DB cell	-	Growth inhibition assay	-	Inhibition of human DB cell growth in a cell viability assay, IC50=8.01131 μM	SANGER
human ES3 cell	-	Growth inhibition assay	-	Inhibition of human ES3 cell growth in a cell viability assay, IC50=9.12794 μM	SANGER
human GAMG cell	-	Growth inhibition assay	-	Inhibition of human GAMG cell growth in a cell viability assay, IC50=5.3715 μM	SANGER
human GCT cell	-	Growth inhibition assay	-	Inhibition of human GCT cell growth in a cell viability assay, IC50=5.85121 μM	SANGER
human H4 cell	-	Growth inhibition assay	-	Inhibition of human H4 cell growth in a cell viability assay, IC50=1.15875 μM	SANGER
human H460a cells	-	Proliferation assay	-	Antiproliferative activity against human H460a cells, IC50=1.04 μM	17303421
human HCT-116 cell	-	Growth inhibition assay	-	Inhibition of human PC-3 cell growth in a cell viability assay, IC50=18.0043 μM	SANGER
human HCT-116 cell	-	Growth inhibition assay	-	Inhibition of human HCT-116 cell growth in a cell viability assay, IC50=19.668 μM	SANGER
human HCT116 cells	-	Proliferation assay	-	Antiproliferative activity against human HCT116 cells, IC50=1.14 μM	17303421
human HCT116 cells	-	Cytotoxic assay	5 days	Cytotoxicity against human HCT116 cells after 5 days by MTS assay， IC50=3.2 μM	22326168
human HGC-27 cell	-	Growth inhibition assay	-	Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=5.73077 μM	SANGER
human HN cell	-	Growth inhibition assay	-	Inhibition of human HN cell growth in a cell viability assay, IC50=5.97097 μM	SANGER
human HO-1-N-1 cell	-	Growth inhibition assay	-	Inhibition of human HO-1-N-1 cell growth in a cell viability assay, IC50=5.95425 μM	SANGER
human Hs-578-T cell	-	Growth inhibition assay	-	Inhibition of human Hs-578-T cell growth in a cell viability assay, IC50=2.27799 μM	SANGER
human HSC-2 cell	-	Growth inhibition assay	-	Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=11,7842 μM	SANGER
human HuP-T4 cell	-	Growth inhibition assay	-	Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50=10.4271 μM	SANGER
human IST-MES1 cell	-	Growth inhibition assay	-	Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50=5.97521 μM	SANGER
human IST-SL1 cell	-	Growth inhibition assay	-	Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=7.43349 μM	SANGER
human KOSC-2 cell	-	Growth inhibition assay	-	Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=3.446662 μM	SANGER
human KP-4 cell	-	Growth inhibition assay	-	Inhibition of human KP-4 cell growth in a cell viability assay, IC50=5.69823 μM	SANGER
human KYSE-270 cell	-	Growth inhibition assay	-	Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=7.03872 μM	SANGER
human LB1047-RCC cell	-	Growth inhibition assay	-	Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=3.23501 μM	SANGER
human LOXIMVI cell	-	Growth inhibition assay	-	Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=8.63701 μM	SANGER
human LXF-289 cell	-	Growth inhibition assay	-	Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=4.2176 μM	SANGER
human MCF7 cell	-	Growth inhibition assay	-	Inhibition of human MCF7 cell growth in a cell viability assay, IC50=11.1849 μM	SANGER
human MDA435 cells	-	Proliferation assay	-	Antiproliferative activity against human MDA435 cells, IC50=1.14 μM	17303421
human ME-180 cell	-	Growth inhibition assay	-	Inhibition of human ME-180 cell growth in a cell viability assay, IC50=8.80395 μM	SANGER
human MN-60 cell	-	Growth inhibition assay	-	Inhibition of human MN-60 cell growth in a cell viability assay, IC50=4.37623 μM	SANGER
human NB10 cell	-	Growth inhibition assay	-	Inhibition of human NB10 cell growth in a cell viability assay, IC50=7.98758 μM	SANGER
human NB13 cell	-	Growth inhibition assay	-	Inhibition of human NB13 cell growth in a cell viability assay, IC50=5.32786 μM	SANGER
human NBsusSR cell	-	Growth inhibition assay	-	Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=10.2318 μM	SANGER
human NCI-H1792 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H1792 cell growth in a cell viability assay, IC50=5.47954 μM	SANGER
human NCI-H2405 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H2405 cell growth in a cell viability assay, IC50=4.74493 μM	SANGER
human NCI-H28 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H28 cell growth in a cell viability assay, IC50=8.59884 μM	SANGER
human NCI-H446 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H446 cell growth in a cell viability assay, IC50=7.0181 μM	SANGER
human NCI-SNU-1 cell	-	Growth inhibition assay	-	Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50=0.73095 μM	SANGER
human NEC8 cell	-	Growth inhibition assay	-	Inhibition of human NEC8 cell growth in a cell viability assay, IC50=4.47076 μM	SANGER
human PA-1 cell	-	Growth inhibition assay	-	Inhibition of human PA-1 cell growth in a cell viability assay, IC50=1.22654 μM	SANGER
human PFSK-1 cell	-	Growth inhibition assay	-	Inhibition of human PFSK-1 cell growth in a cell viability assay, IC50=5.86168 μM	SANGER
human PSN1 cell	-	Growth inhibition assay	-	Inhibition of human PSN1 cell growth in a cell viability assay, IC50=4.10805 μM	SANGER
human RKO cells	-	Proliferation assay	-	Antiproliferative activity against human RKO cells, IC50=2 μM	17303421
human SF539 cell	-	Growth inhibition assay	-	Inhibition of human SF539 cell growth in a cell viability assay, IC50=7.55197 μM	SANGER
human SJSA1 cells	-	Proliferation assay	-	Antiproliferative activity against human SJSA1 cells, IC50=4.55 μM	17303421
human SKG-IIIa cell	-	Growth inhibition assay	-	Inhibition of human SKG-IIIa cell growth in a cell viability assay, IC50=6.85572 μM	SANGER
human SK-MEL-2 cell	-	Growth inhibition assay	-	Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50=5.09632 Μm	SANGER
human SK-N-DZ cell	-	Growth inhibition assay	-	Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=2.01876 μM	SANGER
human SK-N-FI cell	-	Growth inhibition assay	-	Inhibition of human SK-N-FI cell growth in a cell viability assay, IC50=9.41699 μM	SANGER
human SW1710 cell	-	Growth inhibition assay	-	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=1.61408 μM	SANGER
human SW480 cells	-	Proliferation assay	-	Antiproliferative activity against human SW480 cells, IC50=2.2 μM	17303421
human T98G cell	-	Growth inhibition assay	-	Inhibition of human T98G cell growth in a cell viability assay, IC50=1.36812 μM	SANGER
human TE-1 cell	-	Growth inhibition assay	-	Inhibition of human TE-1 cell growth in a cell viability assay, IC50=7.89091 μM	SANGER
human TGW cell	-	Growth inhibition assay	-	Inhibition of human TGW cell growth in a cell viability assay, IC50=6.05682 μM	SANGER
human U251 cell	-	Growth inhibition assay	-	Inhibition of human U251 cell growth in a cell viability assay, IC50=1.63771 μM	SANGER
human UM-UC-3 cell	-	Growth inhibition assay	-	Inhibition of human UM-UC-3 cell growth in a cell viability assay， IC50=2.73936 μM	SANGER
human YH-13 cell	-	Growth inhibition assay	-	Inhibition of human YH-13 cell growth in a cell viability assay, IC50=4.75776 μM	SANGER

(Z)-5-(Quinolin-6-ylmethylene)-2-((thiophen-2-ylmethyl)amino)thiazol-4(5H)-one Catalog No. CSN16564

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