SNS-032 (BMS-387032)

目錄號：S1145 Purity: 99.75%

SNS-032 (BMS-387032)最初被描述為選擇性CDK2抑制劑，無細胞試驗中IC50為48 nM，比作用于CDK1/CDK4選擇性高10和20倍。它也對CDK7/9敏感，IC50為62 nM/4 nM，對CDK6幾乎沒有抑制效果。SNS-032 (BMS-387032)可誘導凋亡。

SNS-032 (BMS-387032) Chemical Structure

CAS: 345627-80-7

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1414.37	現貨
5mg	901.17	現貨
50mg	4675.34	現貨
200mg	13677.3	現貨
1g	24488.1	現貨
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產品質控

批次：純度： 99.75%

99.75

SNS-032 (BMS-387032)相關產品

相關靶點	CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK9 CLK Cdc CDK8 CDK12 CDK13 CDK19 CDK11 CDK/cyclin complexes	點擊展開
相關產品	Ro-3306 Dinaciclib (SCH 727965) Flavopiridol (Alvocidib, HMR-1275) Roscovitine (Seliciclib) Flavopiridol (Alvocidib) HCl AT7519 PHA-767491 HCl LDC000067 THZ1 2HCl XL413 Hydrochloride (BMS-863233) JNJ-7706621 AZD5438 BS-181 HCl Milciclib Purvalanol A K03861 (AUZ454) PHA-793887 BMS-265246 AT7519 HCl AZD4573 MSC2530818 LDC4297 Atuveciclib (BAY-1143572) Riviciclib hydrochloride (P276-00) CVT-313 YKL-5-124 (E/Z)-TG003 THZ531 Enitociclib (BAY 1251152) Cyclin D1 Antibody [L2G10] R547 Kenpaullone Senexin A SEL120 (SEL120-34A) hydrochloride NU6027 SU9516 LY2857785 PF-06873600 (Ebvaciclib) ML167 ON123300 Wogonin Samuraciclib (ICEC0942) hydrochloride G1T38 BI-1347 BRD6989 HLM006474 CGP60474 Cdc25C Antibody [K18P10] p21 Rabbit Recombinant mAb NU2058 MC180295 Indirubin-3'-monoxime NSC95397 CDK2-IN-73 (CDK2-IN-4) SR-4835 Simurosertib Fadraciclib (CYC065) Tagtociclib (PF-07104091) Cdk2 Antibody [L3P20] CDK4 Antibody [K10B14] CDK6 Antibody [F14F18] Phospho-Rb (Ser807/811) Antibody [P5B14] Cyclin B1 Antibody [F4L11] Cyclin E2 Antibody [C5M18] Bohemine NG 52 Alsterpaullone AS2863619 NVP-2 THAL-SNS-032 CDKI-73 Phospho-cdc2 (Tyr15) Antibody [P12H8]	點擊展開
相關化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫 MAPK抑制劑庫 DNA損傷/ DNA修復化合物庫細胞周期化合物庫	點擊展開

細胞實驗數據示例

細胞系	實驗類型	孵育時間	活性描述	文獻信息(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
點擊查看更多細胞系數據

生物活性

產品描述

特性

SNS-032是新一代CDK抑制劑,具有更高的選擇性和更弱的毒性。

靶點

CDK9/CyclinT (Cell-free assay)	CDK2/CyclinA (Cell-free assay)	CDK2/CyclinE (Cell-free assay)	CDK7/CyclinH (Cell-free assay)	GSK-3α (Cell-free assay)	點擊更多
4 nM	38 nM	48 nM	62 nM	230 nM	點擊更多

體外研究(In Vitro)
體外研究活性	SNS-032是新型有效的選擇性Cdk抑制劑, 有效抑制Cdk2, Cdk7和Cdk9。體外，不管病情預斷和治療病史如何，SNS-032都可有效殺死慢性淋巴細胞性白血病細胞。與Flavopiridol和Roscovitine相比, 抑制RNA合成和誘導細胞凋亡時，SNS-032更有效。SNS-032是可逆的，使SNS-032重激活RNA聚合酶II失活, 導致Mcl-1再合成和細胞存活。 SNS-032抑制內皮細胞的三維毛細管網形成。SNS-032作用于人臍靜脈內皮細胞(HUVECs),完全抑制U87MG細胞調節(jié)的毛細管形成。此外, SNS-032明顯抑制VEGF的產生,從而抑制血管生成。臨床前期研究顯示SNS-032跨多種細胞系誘導細胞周期停滯和細胞凋亡。 SNS-032通過抑制 CDKs 2和7而阻斷細胞周期, 通過抑制CDKs 7和9阻斷轉錄。SNS-032的活性不受人類血清影響。 SNS-032誘導膜聯蛋白V染色增多和caspase-3激活，這種作用存在劑量依賴性。在分子水平, SNS-032誘導RNA多聚酶(RNA Pol) II 在serine 2和5位點去磷酸化。且抑制CDK2，CDK9。和去磷酸化的CDK7的表達。
細胞實驗	細胞系	HUVECs和U87MG細胞
	濃度	0-0.5 mM
	孵育時間	24, 48, 或72小時
	方法	U87MG細胞和HUVECs (每孔2000個細胞)接種在96孔板上，終體積為100 ml。24小時后,用不同濃度SNS-032(0-0.5 mM)處理細胞24,48,或72小時。完全處理后, 每孔加入100 mL CTG溶液，室溫下黑暗溫育20分鐘。50 mL溶解物轉移到96孔板上，通過POLARstar OPTIMA測定熒光值。計算加入SNS-032后的細胞生長百分數。
實驗圖片	檢測方法	檢測指標	實驗圖片	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

體內研究(In Vivo)
體內研究活性	SNS-032作用于腫瘤共培養(yǎng)模型，阻斷腫瘤細胞誘導的VEGF分泌。 SNS-032, 作用于實體瘤時具有更高選擇性，且毒性較弱。

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (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

參考文獻
[1]https://pubmed.ncbi.nlm.nih.gov/19234140/ [2]https://pubmed.ncbi.nlm.nih.gov/17534442/ [3]https://pubmed.ncbi.nlm.nih.gov/19169685/ [4]https://pubmed.ncbi.nlm.nih.gov/21212792/ [5]https://pubmed.ncbi.nlm.nih.gov/22447844/ + 展開

參考文獻

[1]https://pubmed.ncbi.nlm.nih.gov/19234140/
[2]https://pubmed.ncbi.nlm.nih.gov/17534442/
[3]https://pubmed.ncbi.nlm.nih.gov/19169685/

[4]https://pubmed.ncbi.nlm.nih.gov/21212792/
[5]https://pubmed.ncbi.nlm.nih.gov/22447844/

+ 展開

化學信息&溶解度

分子量	380.53	分子式	C₁₇H₂₄N₄O₂S₂
CAS號	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
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 76 mg/mL ( (199.72 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 30 mg/mL (78.83 mM)

Water : Insoluble

DMSO : 76 mg/mL ( (199.72 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 76 mg/mL ( (199.72 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內溶解配方批次：現配現用，請按從左到右的順序依次添加，澄清后再加入下一溶劑				動物體內配方計算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	30%PEG400 1 0.5%Tween80 2 5%propylene glycol 該配方已經過Selleck實驗室實測。如果上述溶解方案不能滿足您的需求，可聯系Selleck銷售提供定制化測試。	30.000mg/ml (78.84mM)	以 1 mL 工作液為例，取300μL100mg/ml的澄清PEG400儲備液加到5μLTween80中，混合均勻使其澄清；向上述體系中加入50μL Propylene glycol，混合均勻使其澄清；然后繼續(xù)加入645μL ddH2O定容至 1 mL。工作液請現配現用！

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數量只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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C8=C7/X	C8:	LOG(C8):

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SNS-032 (BMS-387032)

產品質控

SNS-032 (BMS-387032)相關產品

相關信號通路圖

細胞實驗數據示例

生物活性

化學信息&溶解度

實驗計算

技術支持