中文名称:

3-氯-1-(3,4-二氯苯基)-4-(4-吗啉基)-1H-吡咯-2,5-二酮

中文同义词:

3-氯-1-(3,4-二氯苯基)-4-(4-吗啉基)-1H-吡咯-2,5-二酮;RAD51抑制剂(RI-1);13-氯-1-(3;4-二氯苯基)-4-(4-吗啉基)-1H-吡咯-2

英文名称:

RI-1

英文同义词:

RI-1;3-Chloro-1-(3,4-dichlorophenyl)-4-(4-morpholinyl)-1H-pyrrole-2,5-dione;RI-1, >=98%;RAD51 inhibitor RI-1;RAD51 inhibitor 1;3-Chloro-1-(3,4-dichlorophenyl)-4-Morpholino-1H-pyrrole-2,5-dione;1H-Pyrrole-2,5-dione, 3-chloro-1-(3,4-dichlorophenyl)-4-(4-morpholinyl)-;RI1;RI-1

CAS号:

415713-60-9

分子式:

C14H11Cl3N2O3

分子量:

361.61

EINECS号:

相关类别:

小分子抑制剂;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors

Mol文件:

415713-60-9.mol

沸点 

483.0±45.0 °C(Predicted)

密度 

1.61

储存条件 

2-8°C

溶解度 

DMSO: soluble10mg/mL, clear

形态

powder

酸度系数(pKa)

-3.45±0.20(Predicted)

颜色

yellow to orange

生物活性

RI-1 (RAD51 inhibitor 1)是RAD51抑制剂，IC50为5至30 µM。

靶点

Target Value RAD51 <30 μM

Target

Value

RAD51

<30 μM

体外研究

RI-1通过直接和特异破坏HsRAD51和抑制RAD51，形成对单链DNA细丝的能力，提高细胞对DNA损伤的敏感性。此外，在所有三种癌细胞株（HeLa细胞，MCF-7和U2OS）中，RI-1单独产生单剂毒性，LD50值在20-40微米范围内。 RI-1减少了在G2期细胞的γ-H2AX灶，并导致在辐射6小时后未修复DNA双链断裂的升高。

体内研究

RI-1 (50 mg/kg; i.p. every 3 d for 30 d) significantly reduces triple negative breast cancer (TNBC) tumor growth in mice. Animal Model: Female BALB/c nude mice (6 weeks) bearing TNBC tumor Dosage: 50 mg/kg Administration: I.p. every 3 days for 30 days Result: Resulted in significant inhibition of tumor growth. Did not cause body weight loss significantly.

Animal Model:

Female BALB/c nude mice (6 weeks) bearing TNBC tumor

Dosage:

50 mg/kg

Administration:

I.p. every 3 days for 30 days

Result:

Resulted in significant inhibition of tumor growth. Did not cause body weight loss significantly.