SNS-032 (BMS-387032)

SNS-032 (BMS-387032)最初被描述为选择性CDK2抑制剂,无细胞试验中IC50为48 nM,比作用于CDK1/CDK4选择性高10和20倍。它也对CDK7/9敏感,IC50为62 nM/4 nM,对CDK6几乎没有抑制效果。SNS-032 (BMS-387032)可诱导凋亡。

SNS-032 (BMS-387032) Chemical Structure

SNS-032 (BMS-387032) Chemical Structure

CAS: 345627-80-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1414.37 现货
5mg RMB 901.17 现货
50mg RMB 4675.34 现货
200mg RMB 13677.3 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

免费分装
免费预溶

相关CDK产品

客户使用Selleck的SNS-032 (BMS-387032)发表文献72篇:

产品质控

批次: 纯度: 99.75%
99.75

CDK抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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SJ-GBM2 MmrxdWhVWyCjc4PhfS=> MXPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTTk1ISk1{IHPlcIx{ MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 NUWxZoNOeUiWUzDhd5NigQ>? Mn7zdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRnQuOzdiY3XscJM> MojsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
TC32 MnG2dWhVWyCjc4PhfS=> NYTtV3kzeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? M3jVc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS NVv2cXZ2eUiWUzDhd5NigQ>? M1\CbJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHUuOiCRUzDj[Yxtew>? NFnrWm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 NXu0coF4eUiWUzDhd5NigQ>? NF\McWxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDRzIHPlcIx{ NF;FeJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD NI\WWlVyUFSVIHHzd4F6 NXzP[JNteUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhWkRiY3XscJM> MoPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 M1fQd5FJXFNiYYPzZZk> NFTJcItyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBU[W:|LUKgZ4VtdHN? NXPT[mkzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NX;1doF6eUiWUzDhd5NigQ>? MVjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDPTHMuPTBiY3XscJM> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH NE\Id21yUFSVIHHzd4F6 NEn1O5dyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLWPIJINmdGy| NFjQOWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
点击查看更多细胞系数据

生物活性

产品描述 SNS-032 (BMS-387032)最初被描述为选择性CDK2抑制剂,无细胞试验中IC50为48 nM,比作用于CDK1/CDK4选择性高10和20倍。它也对CDK7/9敏感,IC50为62 nM/4 nM,对CDK6几乎没有抑制效果。SNS-032 (BMS-387032)可诱导凋亡。
特性 SNS-032是新一代CDK抑制剂,具有更高的选择性和更弱的毒性。
靶点
CDK9/CyclinT [3]
(Cell-free assay)
CDK2/CyclinA [3]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
CDK7/CyclinH [3]
(Cell-free assay)
GSK-3α [3]
(Cell-free assay)
点击更多
4 nM 38 nM 48 nM 62 nM 230 nM
体外研究(In Vitro)
体外研究活性

SNS-032是新型有效的选择性Cdk抑制剂, 有效抑制Cdk2, Cdk7和Cdk9。体外,不管病情预断和治疗病史如何,SNS-032都可有效杀死慢性淋巴细胞性白血病细胞。与Flavopiridol和Roscovitine相比, 抑制RNA合成和诱导细胞凋亡时,SNS-032更有效。SNS-032是可逆的,使SNS-032重激活RNA聚合酶II失活, 导致Mcl-1再合成和细胞存活。[1]

SNS-032抑制内皮细胞的三维毛细管网形成。SNS-032作用于人脐静脉内皮细胞(HUVECs),完全抑制U87MG细胞调节的毛细管形成。此外, SNS-032明显抑制VEGF的产生,从而抑制血管生成。临床前期研究显示SNS-032跨多种细胞系诱导细胞周期停滞和细胞凋亡。[2]

SNS-032通过抑制 CDKs 2和7而阻断细胞周期, 通过抑制CDKs 7和9阻断转录。SNS-032的活性不受人类血清影响。[3]

SNS-032诱导膜联蛋白V染色增多和caspase-3激活,这种作用存在剂量依赖性。在分子水平, SNS-032诱导RNA多聚酶(RNA Pol) II 在serine 2和5位点去磷酸化。且抑制CDK2,CDK9。和去磷酸化的CDK7的表达。[4]

细胞实验 细胞系 HUVECs和U87MG细胞
浓度 0-0.5 mM
孵育时间 24, 48, 或72小时
方法

U87MG细胞和HUVECs (每孔2000个细胞)接种在96孔板上,终体积为100 ml。24小时后,用不同浓度SNS-032(0-0.5 mM)处理细胞24,48,或72小时。完全处理后, 每孔加入100 mL CTG溶液,室温下黑暗温育20分钟。50 mL溶解物转移到96孔板上,通过POLARstar OPTIMA测定荧光值。计算加入SNS-032后的细胞生长百分数。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-RNA PolII / RNA Pol II / CDK7 / CDK9 YAP / p-YAP / CTGF / CYR61 p-ROCK / ROCK / p-LIMK1/2 / LIMK1/2 / p-Cofilin / Cofilin Mcl-1 / Cyclin D1 / Bcl-2 / PARP 31526394
Growth inhibition assay Cell viability 20663900
体内研究(In Vivo)
体内研究活性

SNS-032作用于肿瘤共培养模型,阻断肿瘤细胞诱导的VEGF分泌。[2] SNS-032, 作用于实体瘤时具有更高选择性,且毒性较弱。[4]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00446342 Completed B-lymphoid Malignancies|Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma|Multiple Myeloma Sunesis Pharmaceuticals February 2007 Phase 1

化学信息&溶解度

分子量 380.53 分子式

C17H24N4O2S2

CAS号 345627-80-7 SDF Download SNS-032 (BMS-387032) SDF
Smiles CC(C)(C)C1=CN=C(O1)CSC2=CN=C(S2)NC(=O)C3CCNCC3
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 76 mg/mL ( 199.72 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 30 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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