SNS-032 (BMS-387032)

目录号：S1145 Purity: 99.75%

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

规格	价格	库存
10mM (1mL in DMSO)	1414.37	现货
5mg	901.17	现货
50mg	4675.34	现货
200mg	13677.3	现货
1g	24488.1	现货
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产品质控

批次：纯度： 99.75%

99.75

SNS-032 (BMS-387032)相关产品

相关靶点	CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK9 CLK Cdc CDK8 CDK12 CDK13 CDK19 CDK11 CDK/cyclin complexes	点击展开
相关产品	Ro-3306 Dinaciclib Roscovitine Flavopiridol (Alvocidib) Flavopiridol (Alvocidib) HCl AT7519 LDC000067 PHA-767491 HCl THZ1 2HCl XL413 JNJ-7706621 AZD5438 Purvalanol A Milciclib BS-181 HCl K03861 (AUZ454) PHA-793887 BMS-265246 AT7519 HCl AZD4573 MSC2530818 R547 Riviciclib hydrochloride (P276-00) (E/Z)-TG003 Kenpaullone CVT-313 Atuveciclib (BAY-1143572) YKL-5-124 LDC4297 Enitociclib (BAY 1251152) SU9516 Wogonin SEL120 (SEL120-34A) hydrochloride THZ531 PF-06873600 ON123300 LY2857785 Senexin A Samuraciclib (ICEC0942) hydrochloride NU6027 ML167 NU2058 MC180295 NSC95397 CDK2-IN-73 (CDK2-IN-4) BRD6989 HLM006474 AS2863619 Simurosertib CDKI-73	点击展开
相关化合物库	激酶抑制剂库 PI3K/Akt 抑制剂库 MAPK抑制剂库 DNA损伤/ DNA修复化合物库细胞周期化合物库	点击展开

细胞实验数据示例

细胞系	实验类型	孵育时间	活性描述	文献信息(PMID)
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

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	点击更多

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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00446342	Completed	B-lymphoid Malignancies\|Chronic Lymphocytic Leukemia\|Mantle Cell Lymphoma\|Multiple Myeloma	Sunesis Pharmaceuticals	February 2007	Phase 1

参考文献
https://pubmed.ncbi.nlm.nih.gov/19234140/ https://pubmed.ncbi.nlm.nih.gov/17534442/ https://pubmed.ncbi.nlm.nih.gov/19169685/ https://pubmed.ncbi.nlm.nih.gov/21212792/ https://pubmed.ncbi.nlm.nih.gov/22447844/ + 展开

参考文献

https://pubmed.ncbi.nlm.nih.gov/19234140/
https://pubmed.ncbi.nlm.nih.gov/17534442/
https://pubmed.ncbi.nlm.nih.gov/19169685/

https://pubmed.ncbi.nlm.nih.gov/21212792/
https://pubmed.ncbi.nlm.nih.gov/22447844/

+ 展开

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

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 (78.83 mM)

Water : Insoluble

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)

Water : Insoluble

Ethanol : Insoluble

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)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方批次：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
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	30%PEG400 1 0.5%Tween80 2 5%propylene glycol 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	30.000mg/ml (78.84mM)	以 1 mL 工作液为例，取300μL100mg/ml的澄清PEG400储备液加到5μLTween80中，混合均匀使其澄清；向上述体系中加入50μL Propylene glycol，混合均匀使其澄清；然后继续加入645μL ddH2O定容至 1 mL。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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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* 必填项

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

SNS-032 (BMS-387032)

产品质控

SNS-032 (BMS-387032)相关产品

相关信号通路图

细胞实验数据示例

生物活性

化学信息&溶解度

实验计算

技术支持