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KU-0060648

KU-0060648是DNA-PK和PI3Kα/β/δ雙重抑制劑，IC50分別為8.6 nM和4 nM/0.5 nM/0.1 nM，對(duì)PI3Kγ抑制作用稍弱，IC50為0.59 μM。

KU-0060648 Chemical Structure

KU-0060648 Chemical Structure

CAS: 881375-00-4

規(guī)格 價(jià)格 庫存 購買數(shù)量
2mg 1212.62 現(xiàn)貨
25mg 7115.45 現(xiàn)貨
100mg 13677.3 現(xiàn)貨
1g 51352.24 現(xiàn)貨
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KU-0060648相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

DNA-PK Signaling Pathways

DNA-PK信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
HeLa Function assay 1 uM 1 hr Inhibition of DNA-PK in human HeLa cells assessed as phosphorylation of gammaH2AX at 1 uM treated 1 hr before 5 Gy ionizing radiation measured within 30 mins by immunofluorescence assay 23855836
MO59J-Fus1 cells Function assay 1 μM Inhibition of human DNA-PK autophosphorylation at S2056 in MO59J-Fus1 cells at 1 uM 23855836
human HeLa cells Function assay Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells, EC50=0.136 μM 23855836
HeLa Function assay Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells, EC50 = 0.136 μM. 23855836
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 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
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
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
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生物活性

產(chǎn)品描述 KU-0060648是DNA-PK和PI3Kα/β/δ雙重抑制劑，IC50分別為8.6 nM和4 nM/0.5 nM/0.1 nM，對(duì)PI3Kγ抑制作用稍弱，IC50為0.59 μM。
靶點(diǎn)
PI3Kδ [1]
(Cell-free assay)		 PI3Kβ [1]
(Cell-free assay)		 PI3Kα [1]
(Cell-free assay)		 DNA-PK [1]
(Cell-free assay)		 PI3Kγ [1]
(Cell-free assay)
0.1 nM 0.5 nM 4 nM 5 nM 0.59 μM
體外研究(In Vitro)
體外研究活性

KU-0060648表現(xiàn)對(duì)生長的不同抑制效果，但并不是對(duì)一類人腫瘤細(xì)胞都有細(xì)胞毒性。在細(xì)胞實(shí)驗(yàn)中，KU-0060648抑制DNA-PK和PI-3K的效果在MCF7細(xì)胞中比在SW620細(xì)胞中強(qiáng)。1mM KU-0060648處理5天抑制95％以上MCF7細(xì)胞的增殖，而在SW620細(xì)胞中只有55％。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 MCF7, T47D, MDA-MB-231, LoVo和SW620
濃度 ~1 μM
孵育時(shí)間 5 天
方法

SRB檢測(cè)

化學(xué)信息&溶解度

分子量 582.71 分子式

C33H34N4O4S
CAS號(hào) 881375-00-4 SDF Download KU-0060648 SDF
Smiles CCN1CCN(CC1)CC(=O)NC2=C3C4=CC=CC=C4SC3=C(C=C2)C5=CC=CC6=C5OC(=CC6=O)N7CCOCC7
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 2 mg/mL ( (3.43 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)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(qǐng)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(jìn)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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常見問題及建議解決方法

問題 1:
On your product page the in vivo solubility for S8045 in 30% Propylene glycol, 5% Tween 80, 65% D5W is up to 20 mg/mL, but in the reference listed "Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K." they use Phosphoric Acid pH 5 to resuspend the drug. I am curious if you have any information on solubility in phosphoric acid pH 5 for KU0060648.

回答：
30% Propylene glycol, 5% Tween 80, 65% D5W to 20 mg/mL is the vehicle we tested in our lab, it's a suspension and can only be used as oral gavage. Phosphoric Acid pH 5 is from the reference, but we didn't test the solubility of our compound in it.

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