RO-3306 | Ro-3306 | CDK | AmBeed-信号通路专用抑制剂

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RO-3306 {[allProObj[0].p_purity_real_show]}

货号：A138869

RO-3306是一种强效且选择性的 CDK1 抑制剂，对 CDK1/cyclin B1 的 Ki 值为 35 nM，选择性是 CDK2/cyclin E 和 CDK4/cyclin D 的 10 倍和 50 倍以上。

RO-3306 化学结构
CAS号：872573-93-8

RO-3306 3D分子结构
CAS号：872573-93-8

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RO-3306 纯度/质量文件产品仅供科研

货号：A138869 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

CDK 亚型比较

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											SGK,ERK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 dihydrochloride									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			99+%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

RO-3306 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]

RO-3306 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
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

RO-3306 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.

RO-3306 实验方案

计算器

存储液制备

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

RO-3306 技术信息

CAS号	872573-93-8
分子式	C₁₈H₁₃N₃OS₂
分子量	351.445

别名
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

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

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
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

RO-3306 {[allProObj[0].p_purity_real_show]}

RO-3306 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

RO-3306 质控信息

RO-3306 生物活性

RO-3306 细胞研究

RO-3306 参考文献

RO-3306 实验方案

RO-3306 技术信息

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RO-3306 {[allProObj[0].p_purity_real_show]}

RO-3306 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

RO-3306 质控信息

RO-3306 生物活性

RO-3306 细胞研究

RO-3306 参考文献

RO-3306 实验方案

RO-3306 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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RO-3306 纯度/质量文件产品仅供科研