现货,Rucaparib (AG-014699 , PF-01367338) ,CAS:459868-92-9,美国进口, 细胞周期(Cell Cycle / Checkpoint) , PARP , PARP 抑制剂和化合物,selleck,S1098

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> PARP >> PARP 抑制剂和化合物 >> Rucaparib (AG-014699 , PF-01367338)http://selleck.cn/ag-014699-S1098.html

技术数据:

分子量(MW): 421.36

化学式:

C19H18FN3O.H3PO4

 

溶解度: DMSO ≥84mg/mL Water ≥60mg/mL Ethanol ≥7mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 459868-92-9

生物活性

 

 

Rucaparib (AG-014699 , PF-01367338) is a PARP inhibitor (Ki, 1.4 nmol/L) with outstanding in vivo chemosensitization potency, which is greater chemosensitization of temozolomide at a dose of 1 mg/kg than could be achieved with AG14361 at 10 mg/kg. Even a 10-fold lower dose of AG14447 (0.1 mg/kg) resulted in a 50% increase in the temozolomide-induced tumor growth delay.

Rucaparib (AG-014699 , PF-01367338), the phosphate salt of AG14447, which has improved aqueous solubility, has been selected for clinical trial.

Rucaparib (AG-014699 , PF-01367338) is a tricyclic indole poly(ADP-Ribose) polymerase (PARP) inhibitor with potential antineoplastic activity. PARP-1 inhibitor Rucaparib (AG-014699 , PF-01367338) blocks base excision repair mediated by PARP 1 on single strand breaks and may be particularly efficacious in inducing apoptosis in breast cancer associated gene-1 and -2 (BRCA1/2) deficient tumor cells.

 

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