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D-I03
产品别名
688342-78-1
D-I03
N-[2-(Diethylamino)ethyl]-N′-[2-(4-ethyl-1-piperazinyl)-4-methyl-6-quinolinyl]-thiourea
1-(2-(Diethylamino)ethyl)-3-(2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl)thiourea
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C23H36N6S |
Molecular weight | 428.64 |
Biochem/physiol Actions【生化/生理作用】 | D-I03 is a selective RAD52 inhibitor (IC50 = 5 and 8 μM, respectively, by SSA and DNA pairing (D-loop formation) assay; <5% RAD51 inhibition at 80 μM) that blocks single-strand DNA (ssDNA) annealing (SSA)-, but not homology dependent recombination (HDR)-, mediated double-strand break (DSB) repair (5-30 μM using respective U2OS reporter cells) and reduces nuclear RAD52, but not RAD51, foci formation (2.5 μM) upon DNA damage by cisplatin. D-I03 selectively suppresses BRCA1-deficient over BRCA1-proficient cancer cells and exerts synergistic activity with PARP1 inhibitors against BRCA1-deficient cancer both in cultures (1 & 2.5 μM) and in mice (50 mg/kg/day i.p.) in vivo. |
产品性质
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | powder |
color【颜色】 | white to beige |
solubility【溶解性】 | DMSO: 2 mg/mL, clear |
storage temp.【储存温度】 | 2-8℃ |
SMILES string | S=C(NCCN(CC)CC)NC1=CC2=C(C=C1)N=C(N3CCN(CC)CC3)C=C2C |
安全信息
Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
WGK | WGK 3 |