CAM833

CAM833

C650141-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a K d of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization. CAM833 increases the progression of G2/M-arrested cells into apoptosis In Vitro CAM833 (3.125-50 μM; 24 h) causes a concentration-dependent decrease in RAD51 foci and subsequent increase in DNA damage. CAM833 (25 μM) inhibits RAD51 molecular clustering at DNA damage sites and suppresses extended RAD51 filament assembly. CAM833 (0-50 μM) inhibits DNA repair by homologous recombination. CAM833 (20 μM; 0-72 h) potentiates radiation-induced cell-cycle arrest and increases apoptosis over time in HCT116 cells. CAM833 (0.1-100 μM; 96 h) causes a dose-dependent growth inhibition of multiple cancer-derived human cell lines that is enhanced when combined with ionizing radiation. CAM833 (20 μM; 96 h) potentiates the growth suppressive effect of PARP1 inhibition in BRCA2 wild-type cells. CAM833 (96 h) alone inhibits the growth of HCT116 colon carcinoma cells with a GI 50 (50% growth inhibition) of 38 μM, when combined with 3 Gy IR, CAM833 suppresses the growth of HCT116 cells with a GI 50 of 14 μM. The quinoline of CAM833 occupies a hotspot, the Phe-binding pocket on RAD51 and the methyl of the substituted α-methylbenzyl group occupies the Ala-binding pocket. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: HCT116 cells Concentration: 20 μM Incubation Time: 0-72 h Result: In the control the percentage of cells in the apoptotic subG1 fraction remains below 5% throughout, in the compound-treated cells this rises progressively to peak at 15% at 48 hours. Form:Solid IC50& Target:K d : 355 nM (ChimRAD51, measured by FP), 366 nM (ChimRAD51, measured by ITC)

CAM833 是 BRCA2 和 RAD51 之间相互作用的强效正交抑制剂，对 ChimRAD51 蛋白的 K d 值为 366 nM。CAM833 还能抑制 RAD51 的寡聚化。CAM833 可增加 G2/M 停滞细胞进入凋亡的进程

2758364-02-0

C26H26ClFN4O5

528.96 g/mol

C[C@@H](C1=C(C=C(C=C1)OC)Cl)NC([C@H]2N(C[C@@H](C2)O)C(CNC(C3=NC4=C(C=C(C=C4)F)C=C3)=O)=O)=O

DMSO : 125 mg/mL (236.31 mM; Need ultrasonic)