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CAY10603
別名: BML-281
CAY10603 (BML-281)是一種強效的選擇性HDAC6抑制劑，IC50為2 pM，選擇性比其它HDACs高200多倍。
CAY10603 Chemical Structure
CAS: 1045792-66-2
產(chǎn)品質(zhì)控
批次：
S759601
DMSO]89 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false
純度：
99.85%
99.85
CAY10603相關產(chǎn)品
相關信號通路圖
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 SU.86.86 cells | Proliferation assay | 72 h | Antiproliferative activity against human SU.86.86 cells after 72 hrs by MTT assay, IC50=0.6 μM | 18642892 | |
| HPDE 6c7 cells | Cytotoxicity assay | 72 h | Cytotoxicity against HPDE 6c7 cells after 72 hrs by MTT assay, IC50=0.5 μM | 18642892 | |
| human HupT3 cells | Proliferation assay | 72 h | Antiproliferative activity against human HupT3 cells after 72 hrs by MTT assay, IC50=0.3 μM | 18642892 | |
| human MiaPaca2 cells | Proliferation assay | 72 h | Antiproliferative activity against human MiaPaca2 cells after 72 hrs by MTT assay, IC50=0.1 μM | 18642892 | |
| human Panc04.03 cells | Proliferation assay | 72 h | Antiproliferative activity against human Panc04.03 cells after 72 hrs by MTT assay, IC50=0.1 μM | 18642892 | |
| human BxPC3 cells | Proliferation assay | 72 h | Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay, IC50=1 μM | 18642892 | |
| HMEC | Cytotoxicity assay | 72 h | Cytotoxicity against HMEC after 72 hrs by MTT assay, IC50=1 μM | 18642892 | |
| sf9 | Function assay | 5 to 10 mins | Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins, IC50=0.0032μM. | 31414801 | |
| sf9 | Function assay | 5 to 10 mins | Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins, IC50=0.0138μM. | 31414801 | |
| HeLa | Function assay | 2 hrs | Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay, IC50=0.79433μM. | 30964290 | |
| MV4-11 | Function assay | 1 hr | Binding affinity to HDAC6 in human MV4-11 cells assessed as increase in cellular protein stabilization at 1 uL preincubated for 1 hr followed by heating at 52 degree C for 3.5 mins by CETSA | 32212730 | |
| 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 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS 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 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 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 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 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 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 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 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 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 | CAY10603 (BML-281)是一種強效的選擇性HDAC6抑制劑，IC50為2 pM，選擇性比其它HDACs高200多倍。 | ||
|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | CAY10603，通過抑制HDAC6，對胰腺癌細胞系表現(xiàn)出有效的抗增殖活性，IC50 <1 μM，其可以用作新的分子探針以探索HDAC的生物學性能。[1] | |||
|---|---|---|---|---|
| 激酶實驗 | HDAC 抑制試驗 | |||
| 純化的HDACs與1 mM羧基熒光素(FAM)-標記的乙?；嚯牡孜锖蜏y試化合物在HDAC試驗緩沖液中于25℃下培養(yǎng)17小時，試驗緩沖液包含100 mM HEPES (pH 7.5)，25 mM KCl，0.1% BSA，和0.01% Triton X-100。加入包含0.078% SDS的緩沖液(終SDS濃度為0.05%)終止反應。底物和產(chǎn)物使用Caliper LabChip 3000系統(tǒng)電泳分離，以藍色激光激發(fā)，綠色熒光檢測(CCD2)。底物和產(chǎn)品峰的熒光強度使用Well Analyzer軟件在Caliper系統(tǒng)中檢測。對每個樣品，反應重復進行兩次。IC50值使用Microsoft Excel 中IDBS XLFit版4.2.1 插件和XLFit 4參數(shù)Logistic模型: ((A+((B_A)/1+((C/x)D))))自動計算，公式中X是化合物濃度，A和B分別為估計的最小和最大抑制百分比，C是拐點，D是S形曲線的Hill斜率。IC50的標準差使用Microsoft Excel 中IDBS XLFit版4.2.1 插件和公式xf4_FitResultStdError自動計算。 | ||||
| 細胞實驗 | 細胞系 | BxPc-3，HupT3，Mia Paca-2，Panc 04.03，和 SU 86.86 細胞 | ||
| 濃度 | ~50 μM | |||
| 孵育時間 | 72小時 | |||
| 方法 | 胰腺癌細胞系BxPc-3，HupT3，Mia Paca-2，Panc 04.03，和SU 86.86在包含10%胎牛血清和左旋谷酰胺的培養(yǎng)基(DMEM或RPMI)中生長。胰腺癌細胞重復兩份接種在96孔板的6孔中。接種4小時后，各孔用稀釋劑(DMSO)或不同濃度的SAHA或指示的1 nM到50 mM濃度的HDACIs進行處理。細胞毒性在處理后 “0”，和 72 小時使用比色MTT法根據(jù)制造商的建議進行測量。IC50值使用XLfit計算。 | |||
化學信息&溶解度
| 分子量 | 446.5 | 分子式 | C22H30N4O6 |
| CAS號 | 1045792-66-2 | SDF | Download CAY10603 SDF |
| Smiles | CC(C)(C)OC(=O)NC1=CC=C(C=C1)C2=CC(=NO2)C(=O)NCCCCCCC(=O)NO | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 89 mg/mL ( (199.32 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 5 mg/mL (11.19 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。
技術支持
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常見問題及建議解決方法
問題 1:
I want to use CAY10603 and Tubastatin A via IP for mice. What can serve as the working solution instead of DMSO?
回答：
S7596 CAY10603 can be dissolved in 5% DMSO+50% PEG 300+ddH2O at 9mg/ml as a clear solution. The dissolving protocol is the same as S8049.
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