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SNS-032 (BMS-387032)
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(dǎo)凋亡。
SNS-032 (BMS-387032) Chemical Structure
CAS: 345627-80-7
產(chǎn)品質(zhì)控
批次：
純度：
99.75%
99.75
SNS-032 (BMS-387032)相關(guān)產(chǎn)品
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | 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(dǎo)凋亡。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 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 |
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| 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(yù)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(dǎo)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(dǎo)致Mcl-1再合成和細胞存活。[1] SNS-032抑制內(nèi)皮細胞的三維毛細管網(wǎng)形成。SNS-032作用于人臍靜脈內(nèi)皮細胞(HUVECs),完全抑制U87MG細胞調(diào)節(jié)的毛細管形成。此外, SNS-032明顯抑制VEGF的產(chǎn)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(dǎo)細胞周期停滯和細胞凋亡。[2] 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(zhuǎn)錄。SNS-032的活性不受人類血清影響。[3] SNS-032誘導(dǎo)膜聯(lián)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(dǎo)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。[4] |
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|---|---|---|---|---|
| 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(zhuǎn)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(shù)。 |
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| 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(nèi)研究(In Vivo) | ||
| 體內(nèi)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(dǎo)的VEGF分泌。[2] SNS-032, 作用于實體瘤時具有更高選擇性，且毒性較弱。[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 |
化學(xué)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) | |||
|
體外溶解度 |
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 |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)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(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)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）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)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(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)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(lián)系Selleck）；
體內(nèi)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(nèi)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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