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
CAS: 345627-80-7
产品质控
批次：
纯度：
99.75%
99.75
SNS-032 (BMS-387032)相关产品
相关信号通路图
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 |
|---|---|---|---|---|---|
| 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 | |
| HCT116 | Function assay | 16 hrs | 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=0.458μM | 18842409 | |
| HCT116 | Function assay | 16 hrs | Inhibition of CDK9-mediated RNA pol 2 phosphorylation at ser2 in human HCT116 cells after 16 hrs by HCS assay, IC50=0.55μM | 18926699 | |
| HCT116 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay, IC50=0.7μM | 30197029 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50=1μM | 30197029 | |
| Sf21 | Function assay | Inhibition of recombinant human full length C-terminal His6-tagged CDK9/cyclin T1 expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate, IC50=0.004μM | 27171036 | ||
| Sf21 | Function assay | Inhibition of human full length C-terminal His6-tagged CDK2/N-terminal GST-tagged cyclin A expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate, IC50=0.038μM | 27171036 | ||
| Sf21 | Function assay | Inhibition of recombinant human full length C-terminal His6-tagged CDK2/N-terminal GST-tagged cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate, IC50=0.048μM | 27171036 | ||
| Sf21 | Function assay | Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide, IC50=0.062μM | 27171036 | ||
| Sf21 | Function assay | Inhibition of recombinant human full length N-terminal His6-tagged CDK5/N-terminal GST-tagged p25 expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate, IC50=0.34μM | 27171036 | ||
| Sf21 | Function assay | Inhibition of human full length C-terminal His6-tagged CDK1/N-terminal GST-tagged cyclin B expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate, IC50=0.48μM | 27171036 | ||
| Sf cells | Function assay | Inhibition of recombinant human N-terminal GST-tagged CDK4/cyclin D1 expressed in baculovirus infected sf cells, IC50=0.925μM | 27171036 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| 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 |
|
| 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] |
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|---|---|---|---|---|
| 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。 |
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| 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) | |||
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体外溶解度 |
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 (78.83 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 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
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
只
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，注：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：取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：取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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