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A-966492

 
Catalog No.
A4160
PARP-1/-2抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,000.00
现货
10mg
¥ 1,727.00
现货
50mg
¥ 5,363.00
现货
200mg
¥ 13,545.00
Ship with 10-15 days

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A

背景

A-966492是PARP-1的抑制剂,Ki值为1 nM[1]。

PARP-1属于聚(ADP-核糖)聚合酶(PARP)家族,有助于癌症治疗后抗药性的发生。A-966492是一种有效的PARP1和PARP2抑制剂(Ki为1.5 nM),在C41全细胞中有良好效果(EC50值为1 nM)。A-966492具有优异的药学特性,口服生物利用度达到34-72%,半衰期为1.7-1.9 h。此外,A-966492可穿过血脑屏障。A-966492在小鼠B16F10同系黑色素瘤模型和BRCA1缺陷的MX-1乳腺癌模型中有效。同时,该物质可提高TMZ和卡铂在这些模型中的效果[1]。

参考文献:
[1] Penning TD, Zhu GD, Gong J, Thomas S, Gandhi VB, Liu X, Shi Y, Klinghofer V, Johnson EF, Park CH, Fry EH, Donawho CK, Frost DJ, Buchanan FG, Bukofzer GT, Rodriguez LE, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL.  Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor. J Med Chem. 2010 Apr 22;53(8):3142-53.

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt324.35
Cas No.934162-61-5
FormulaC18H17FN4O
Solubility≥32.4 mg/mL in DMSO; ≥16.53 mg/mL in H2O with ultrasonic; ≥3.16 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name2-[2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl]-1H-benzimidazole-4-carboxamide
SDFDownload SDF
Canonical SMILESC1CC(NC1)C2=CC(=C(C=C2)C3=NC4=C(C=CC=C4N3)C(=O)N)F
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

生物活性

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
Targets PARP1 PARP2        
IC50 1 nM 1.5 nM        

质量控制