SNS-032 | BMS-387032 | CDK Inhibitor | AmBeed-信号通路专用抑制剂

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SNS-032 99%+

货号：A153280 同义名： BMS-387032

SNS-032 is a potent inhibitor of cyclin-dependent kinases (CDKs)9, 2 and 7 (IC50 values are 4, 38 and 62 nM respectively).

SNS-032 化学结构
CAS号：345627-80-7

SNS-032 3D分子结构
CAS号：345627-80-7

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SNS-032 纯度/质量文件产品仅供科研

货号：A153280 标准纯度： 99%+ 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: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 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/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 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	98%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 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/CyclinE, IC50: 8 nM CDK2/CyclinA, 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/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 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	98%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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				98+%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ 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												++ Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM		99%+
(E/Z)-TG003												+++ mCLK4, IC50: 15 nM mCLK1, IC50: 200 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。

SNS-032 生物活性

靶点	CDK5 CDK5/p35, IC50:340 nM CDK2 CDK2/CyclinE, IC50:48 nM CDK2/CyclinA, IC50:38 nM CDK9 CDK9/CyclinT, IC50:4 nM CDK7 CDK7/CyclinH, IC50:62 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. Thus, the molecular events that distinguish the activities of CDKs can be leveraged as pharmacodynamics biomarkers for activity of the CDKs. For example, CDK2 inhibition can be assessed by increased level of cyclin E, decreased level of Cdc6 or phosphorylation of Rb. Decreased phosphorylation of pSer5 and pSer2 of RNA pol II CTD would indicate inhibition of CDKs 7 and 9, respectively. SNS-032 (BMS-387032) is a selective inhibitor of CDK2/Cyclin A, CDK2/Cyclin E, CDK7/Cyclin H and CDK9/Cyclin T with IC50 values of 38, 48, 62 and 4 nM (measured by enzymatic activity assay), respectively, with modest inhibitory activity against CDK5/p35, CDK1/Cyclin B and CDK4/Cyclin D with IC50 values of 340, 480 and 925 nM. After exposure to 0.03 - 3 μM SNS-032, stabilization of cyclin E can be observed by 4h and persisted for at least 2h post-washout of SNS-032 in RPMI-8226 cells, accompanied with decrease in Cdc6 at 4h. Cellular IC50 values of 231 nM and 192 nM for SNS-032 for 16h were identified for inhibition of CDK7 and CDK9, which was read out by phosphorylation of Ser5 and Ser2 of RNA Pol II CTD, in RPMI-8226 MM cells. 300 nM SNS-032 for up to 6h showed both decrease of pSer2 RNA Pol II-CTD and increase in cleaved PARP. Treatment with 300 nM SNS-032 for 24h caused arrested cell cycle progression at G2/M in asynchronous HCT116 cells^[1]. Exposure with 0.3 μM SNS-032 for 6 hours can significant decrease the mRNA and protein level of Mcl-1 and XIAP, the antiapoptotic proteins, in CLL cells from the same set of 6 patients^[2]. Treatment with 15 mg/kg SNS-032 intraperitoneally every 2 days for about 2 weeks can inhibit the growth of xenografts, BaF3-T674I FIP1L1-PDGFRα or KBM5-T315I cells, in nude mice^[3]. Up to now, a phase 1 study of SNS-032 treatment for B-lymphoid malignancies, chronic lymphocytic leukemia, mantle cell lymphoma and multiple myeloma has been completed (see in https://www.clinicaltrials.gov/).
作用机制	SNS-032 can compete with ATP-binding pocket to CDK7 and 9.

SNS-032 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 A2780 cell line		Proliferation assay	72 h	Antiproliferative effect against human A2780 cell line was determined in a whole cell 72 hr cytotoxicity assay, IC50=95 nM	15027863
human HCT116 cells		Function assay		Inhibition of CDK9 in human HCT116 cells assessed as phosphor-ser2 level of RNA polymerase 2 after 16 hrs by high content cellular assay, IC50=458 nM	18842409
human HCT116 cells		Function assay	16 h	Inhibition of CDK9-mediated RNA pol 2 phosphorylation at ser2 in human HCT116 cells after 16 hrs by HCS assay, IC50=0.55 μM	18926699

SNS-032 动物研究

Dose

Mice^[4] (i.p.): min = 18 mg/kg, max = 48 mg/kg

Administration

i.p.

Pharmacokinetics

Animal	Mice^[4]	Rats^[4]	Dogs^[4]
Dose	24 μmol/kg	24 μmol/kg	1.2 μmol/kg
Administration	i.v. / p.o.	i.v. / p.o.	i.v. / p.o.
C_max	1.4 μM (p.o.)	0.52 μM (p.o.)	0.33 μM (p.o.)
T_1/2	4.8 h (i.v.)	5.3 h (i.v.)	7 h (i.v.)
F	1	0.31	0.28
T_max	2.0 h (p.o.)	4.7 h (p.o.)	0.4 h (p.o.)
AUC_tot	4.8 μM·h (i.v.)	6.3 μM·h (i.v.)	2.1 μM·h (i.v.)
Vss	14 L/kg (i.v.)	15 L/kg (i.v.)	3.6 L/kg (i.v.)
CL	81 ml/min/kg (i.v.)	64 ml/min/kg (i.v.)	9.4 ml/min/kg (i.v.)
MRT	2.8 h (i.v.)	3.7 h (i.v.)	6.3 h (i.v.)

SNS-032 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
NCT00292864	Tumors	Phase 1	Completed	-	United States, Arizona ... 展开 >> Premiere Oncology of Arizona Scottsdale, Arizona, United States, 85260 United States, California University of California Davis Medical Center Davis, California, United States, 95817 United States, Massachusetts Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 Massachusetts General Hospital Boston, Massachusetts, United States, 02215 United States, Pennsylvania Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 收起 <<
NCT00446342	B-lymphoid Malignancies ... 展开 >> Chronic Lymphocytic Leukemia Mantle Cell Lymphoma Multiple Myeloma 收起 <<	Phase 1	Completed	-	United States, California ... 展开 >> City of Hope Duarte, California, United States, 91010 Stanford Cancer Center Stanford, California, United States, 94305 United States, Georgia Winship Cancer Institute at Emory University Atlanta, Georgia, United States, 30322 United States, Maryland Greenebaum Cancer Center, University of Maryland Baltimore, Maryland, United States, 21201 United States, New Jersey Hackensack University Medical Center at the Cancer Center Hackensack, New Jersey, United States, 07601 United States, Texas MD Anderson Cancer Center, University of Texas Houston, Texas, United States, 77230 收起 <<

SNS-032 参考文献

[1]Conroy A, Stockett DE, et al. SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples. Cancer Chemother Pharmacol. 2009 Sep;64(4):723-32.

[2]Chen R, Wierda WG, et al. Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637-45.

[3]Wu Y, Chen C, et al. Cyclin-dependent kinase 7/9 inhibitor SNS-032 abrogates FIP1-like-1 platelet-derived growth factor receptor α and bcr-abl oncogene addiction in malignant hematologic cells. Clin Cancer Res. 2012 Apr 1;18(7):1966-78.

[4]Misra RN, Xiao HY, et al. N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent. J Med Chem. 2004 Mar 25;47(7):1719-28.

SNS-032 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.28mL

5.26mL

2.63mL

SNS-032 技术信息

CAS号	345627-80-7
分子式	C₁₇H₂₄N₄O₂S₂
分子量	380.528

别名	BMS-387032
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 60 mg/mL(157.68 mM)，配合低频超声，并水浴加热至45℃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

SNS-032 99%+

SNS-032 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

SNS-032 质控信息

SNS-032 生物活性

SNS-032 细胞研究

SNS-032 动物研究

SNS-032 临床研究

SNS-032 参考文献

SNS-032 实验方案

SNS-032 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

热门区域

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CDK5	CDK5/p35, IC50:340 nM
CDK2	CDK2/CyclinE, IC50:48 nM CDK2/CyclinA, IC50:38 nM
CDK9	CDK9/CyclinT, IC50:4 nM
CDK7	CDK7/CyclinH, IC50:62 nM

SNS-032 99%+

SNS-032 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

SNS-032 质控信息

SNS-032 生物活性

SNS-032 细胞研究

SNS-032 动物研究

SNS-032 临床研究

SNS-032 参考文献

SNS-032 实验方案

SNS-032 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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热门区域

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SNS-032 纯度/质量文件产品仅供科研