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1945950-21-9

中文名称 1945950-21-9
英文名称 PDD 00017273
CAS 1945950-21-9
分子式 C23H26N6O4S2
分子量 514.62
MOL 文件 1945950-21-9.mol
更新日期 2024/07/31 18:34:59
1945950-21-9 结构式 1945950-21-9 结构式

基本信息

中文别名
1-[(1,3-二甲基-1H-吡唑-5-基)甲基]-1,2,3,4-四氢-N-(1-甲基环丙基)-3-[(2-甲基-5-噻唑基]甲基]-2,4-二氧代-6-喹唑啉磺酰胺
英文别名
PDD 00017273
PDD00017273 >=98% (HPLC)
1-[(1,3-Dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide
6-Quinazolinesulfonamide, 1-[(1,3-dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-

物理化学性质

沸点733.9±70.0 °C(Predicted)
密度1.52±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: 10 mg/ml
酸度系数(pKa)11.67±0.20(Predicted)
形态固体
颜色White to light yellow
1945950-21-9价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-1083601945950-21-9
PDD 00017273
1945950-21-95mg1100元
2024/04/30HY-1083601945950-21-9
PDD 00017273
1945950-21-910mM * 1mLin DMSO1245元
2024/04/30HY-1083601945950-21-9
PDD 00017273
1945950-21-910mg2100元

常见问题列表

生物活性
PDD00017273是有效的、选择性的poly (ADP ribose) glycohydrolase (PARG)抑制剂,IC50为26 nM. 它对PARG的选择性比对其他离子通道、酶和受体如PARP1和ARH3高350倍以上。
靶点
TargetValue
PARG
(Cell-free assay)
26 nM
体外研究

PDD 00017273 is a potent inhibitor of PARG, with an IC 50 of 26 nM, and a K D of 1.45 nM. PDD 00017273 (10 μM) does not inhibit five common Cytochrome P450 enzymes. PDD 00017273 (30 μM) modestly increasess phosphorylated H2AX (γH2AX) intensity, PDD 00017273 also decreases in NAD/H through PARG inhibition after DNA damage. PDD 00017273 suppresses the ZR-75-1 cells carring BRCA1 and BRCA2 wild type, and exhibits less potent activities against MDA-MB-436 cells carry the 5396 + 1G>A mutation in BRCA1. PDD 00017273 (0.3 μM) inhibits degradation of PAR polymers in MCF7 cells. PDD 00017273 (0.3 μM) also reduces the viability of BRCA1, BRCA2, PALB2, FAM175A, and BARD1 depleted cells. PDD 00017273 stalls replication forks and induces DNA damage that requires homologous recombination (HR) for repair.

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