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 |