CAS 881375-00-4; ku-0060648

CAS:

881375-00-4

分子式:

C₃₃H₃₄N₄O₄S

分子量:

582.71

英文名称:

ku-0060648

4-ethyl-n-[4-[2-(4-morpholinyl)-4-oxo-4h-1-benzopyran-8-yl]-1-dibenzothienyl]-1-piperazineacetamide

ku 0060648

用途:

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]

推荐供应商

货号

品牌

产品名称

规格

包装、参考价格

K872692

MACKLIN

KU-0060648

99%

1307元/5mg;

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储存：-20℃
状态：粉末

SML1257

Sigma-Aldrich

KU-0060648

≥98% (HPLC)

2102.31元/5 MG; 6765.81元/25 MG;

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产品说明

包装

5, 25 mg in glass bottle

生化/生理作用

KU-0060648 is a very potent dual inhibitor of DNA-PK and PI3K. The IC₅₀ values for inhibition of DNA-PK in MCF7 and SW620 cells are 19 and 170 nM, respectively. The compound KU-0060648 inhibits MCF7 PI3K activity with an IC₅₀ of 39 nM, but is inactive against PI3K in SW620, suggesting a cell-dependent mechanism of inhibition. KU-0060648 increases sensitivity to DNA damaging cytotoxic drugs such as etoposide and doxorubicin in tumor cell lines expressing DNA-PK. KU-0060648 stimulates Cas9 (CRISPR associated protein 9) mediated genome editing by enhancing the rate of homology directed-repair (HDR) and decreasing the rate of NHEJ (non-homologous end-joining).
KU-0060648 is observed to inhibit proliferation and initiate apoptosis in hepatocellular carcinoma. KU-0060648 is useful in chemotherapy as it increases the efficiency of double stranded breaks initiated by anticancer drugs.

基本信息

经验(实验)分子式	C₃₃H₃₄N₄O₄S
分子量	582.71
MDL编号	MFCD17214218
PubChem化学物质编号	329825749
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
颜色	white to light brown
溶解性	DMSO: 1 mg/mL, clear (warmed)
储存温度	−20℃
SMILES string	O=C(CN1CCN(CC)CC1)NC2=CC=C(C3=CC=CC4=C3OC(N5CCOCC5)=CC4=O)C6=C2C(C=CC=C7)=C7S6
InChI	1S/C33H34N4O4S/c1-2-35-12-14-36(15-13-35)21-29(39)34-26-11-10-23(33-31(26)25-6-3-4-9-28(25)42-33)22-7-5-8-24-27(38)20-30(41-32(22)24)37-16-18-40-19-17-37/h3-11,20H,2,12-19,21H2,1H3,(H,34,39)
InChI key	AATCBLYHOUOCTO-UHFFFAOYSA-N

安全信息

象形图
警示用语：	Danger
危险声明	H301
预防措施声明	P264 - P270 - P301 + P310 + P330 - P405 - P501
危险分类	Acute Tox. 3 Oral
储存分类代码	6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable