化学性质:
规格 | 5mg 10mg 50mg 200mg |
CAS | 934162-61-5 |
别名 |
|
化学名 | 2-[2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl]-1H-benzimidazole-4-carboxamide |
分子式 | C18H17FN4O |
分子量 | 324.35 |
溶解度 | ≥ 32.4 mg/mL in DMSO, ≥ 3.16 mg/mL in EtOH with ultrasonic and warming, ≥ 16.53 mg/mL in H2O with ultrasonic |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
A-966492 is an inhibitor of PARP-1 with Ki value of 1nM [1].
PARP-1 belongs to the poly(ADP-ribose) polymerases (PARPs) family, it contributes to the resistance happened after cancer therapy. A-966492 is a potent inhibitor of both PARP-1 and PARP-2 (Ki value of 1.5nM) with good potency in C41 whole cells (EC50 value of 1nM). A-966492 shows excellent pharmaceutical properties with oral bioavailabilities of 34-72% and half-lives of 1.7-1.9 h. Additionally, A-966492 can crosses the blood-brain barrier. A-966492 is proved potent in a murine B16F10 syngeneic melanoma model and a BRCA1-deficient MX-1 breast carcinoma model. Meanwhile, it can enhance the efficacy of TMZ and carboplatin in these models [1].
特别提醒:
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。
2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。
标签:A-966492
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