RI-1

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Chemical Structure| 415713-60-9 同义名 : -
CAS号 : 415713-60-9
货号 : A194418
分子式 : C14H11Cl3N2O3
纯度 : 98%
分子量 : 361.608
MDL号 : MFCD00814248
存储条件:

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 35 mg/mL(96.79 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 RAD51 protein is highly expressed in many human cancers, and overexpression of RAD51 may improve homologous recombination function and enhance cellular resistance to DNA damage. RI-1 is a small molecule inhibitor of RAD51 with an IC50 of 5–30µM[3]. The IC50 value of RI-1 on RAD51 binding to single-stranded DNA is 6.82±0.81µM and the LD50 value of RI-1 is 16.62±1.1µM[4]. In a mouse xnograft model of MDA-MB-157 breast cancer, i.p. injection of RI-1 at a dose of 50mg/kg every 3 days for 30 days resulted in significant inhibition of tumor growth[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.83mL

2.77mL

1.38mL

27.65mL

5.53mL

2.77mL

参考文献

[1]Bee L, Fabris S, et al. The efficiency of homologous recombination and non-homologous end joining systems in repairing double-strand breaks during cell cycle progression. PLoS One. 2013 Jul 11;8(7):e69061.

[2]Budke B, Logan HL, et al. RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells. Nucleic Acids Res. 2012 Aug;40(15):7347-57.

[3]Budke B, Logan HL, Kalin JH, et al. RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells. Nucleic Acids Res. 2012;40(15):7347-7357. doi:10.1093/nar/gks353.

[4]Budke B, Kalin JH, Pawlowski M, et al. An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity. J Med Chem. 2013;56(1):254-263. doi:10.1021/jm301565b.

[5]Shi Y, Jin J, Wang X, Ji W, Guan X. DAXX, as a Tumor Suppressor, Impacts DNA Damage Repair and Sensitizes BRCA-Proficient TNBC Cells to PARP Inhibitors. Neoplasia. 2019;21(6):533-544. doi:10.1016/j.neo.2019.04.001.