KU-0060648
KU-0060648是DNA-PK和PI3Kα/β/δ双重抑制剂，IC50分别为8.6 nM和4 nM/0.5 nM/0.1 nM，对PI3Kγ抑制作用稍弱，IC50为0.59 μM。
KU-0060648 Chemical Structure
CAS: 881375-00-4
客户使用Selleck的KU-0060648发表文献11篇
客户使用该产品的2个实验数据
产品质控
KU-0060648相关产品
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 凋亡分子化合物库 细胞周期化合物库 NF-κB信号通路库 | 点击展开 |
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相关信号通路图
DNA-PK抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | KU-0060648是DNA-PK和PI3Kα/β/δ双重抑制剂，IC50分别为8.6 nM和4 nM/0.5 nM/0.1 nM，对PI3Kγ抑制作用稍弱，IC50为0.59 μM。 | ||||||||||
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | KU-0060648表现对生长的不同抑制效果，但并不是对一类人肿瘤细胞都有细胞毒性。在细胞实验中，KU-0060648抑制DNA-PK和PI-3K的效果在MCF7细胞中比在SW620细胞中强。1mM KU-0060648处理5天抑制95％以上MCF7细胞的增殖，而在SW620细胞中只有55％。在克隆生存测定法中，KU-0060648增加了etoposide和doxorubicin对富含DNA-PKcs细胞的细胞毒性作用，而对DNA-PKcs缺陷的细胞作用不强，这证实了拓扑异构酶和doxorubicin增强的细胞毒作用是由于DNA-PK的抑制作用。[1] | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | MCF7, T47D, MDA-MB-231, LoVo和SW620 | ||
| 浓度 | ~1 μM | |||
| 孵育时间 | 5 天 | |||
| 方法 | SRB检测 | |||
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在MCF7和SW620异种移植物模型中，KU-0060648提高etoposide的抗肿瘤活性，并且在MCF7异种移植模型中具有单一试剂的活性。[1] | |
|---|---|---|
| 动物实验 | Animal Models | 人类肿瘤SW620或MCF7异种移植模型 |
| Dosages | 10 毫克/千克, 每天2次 | |
| Administration | 腹腔注射 | |
化学信息&溶解度
| 分子量 | 582.71 | 分子式 | C33H34N4O4S |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 2 mg/mL ( (3.43 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 |
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体内溶解度 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 | ||||
实验计算
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）
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）
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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常见问题及建议解决方法
问题 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.
