1945950-21-9
|
|
|
- CAS号:
- 1945950-21-9
- 英文名:
- PDD 00017273
- 英文别名:
- PDD17273;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-
- 中文名:
- 1945950-21-9
- 中文别名:
- 化合物 T5700;PDD 00017273,PARG抑制剂;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
- CBNumber:
- CB63386505
- 分子式:
- C23H26N6O4S2
- 分子量:
- 514.62
- MOL File:
- 1945950-21-9.mol
|
|
|
1945950-21-9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:
-
Store at -20°C
-
|
-
溶解度:
-
DMSO: 10 mg/ml
-
|
-
形态:
-
A solid
-
|
-
酸度系数(pKa):
-
11.67±0.20(Predicted)
-
|
1945950-21-9性质、用途与生产工艺
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。
| Target | Value |
PARG
(Cell-free assay)
|
26 nM
|
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.
1945950-21-9
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-108360 | 1945950-21-9
PDD 00017273 | 1945950-21-9 | 5mg | 1100元 |
| 2024/04/30 | HY-108360 | 1945950-21-9
PDD 00017273 | 1945950-21-9 | 10mM * 1mLin DMSO | 1245元 |
1945950-21-9, 1945950-21-9 相关搜索:
- 药靶配体
- C23H26N6O4S2
- PDD 00017273,PARG抑制剂
- 化合物 T5700
- 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
- 1945950-21-9
- PDD17273
- PDD00017273 >=98% (HPLC)
- 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-
- 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
- PDD 00017273