13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 5mg 25mg |
| CAS | 1645286-75-4 |
| 別名 |
|
| 化學名 | 2-(4-(6-((3S,5R)-3,5-dimethylpiperazin-1-yl)-4-methylpyridin-3-yl)phenyl)-7-methyl-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one |
| 分子式 | C25H28N6O |
| 分子量 | 428.53 |
| 溶解度 | DMF: 15 mg/ml,DMF:PBS(pH7.2) (1:2): 0.3 mg/ml,DMSO: 10 mg/ml |
| 儲存條件 | 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 |
產品描述：
IC50: 1 and 3 nM for TNKS2 and TNKS1, respectively
AZ6102 is a TNKS1/2 inhibitor.
Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of the tankyrases (TNKS1 and TNKS2) is reported to inhibit the Wnt pathway by increasing stabilization of Axin. The canonical Wnt pathway plays a critical role in adult tissue homeostasis, embryonic development, as well as cancer.
In vitro: AZ6102 was identified as a potent TNKS1/2 inhibitor with 100-fold selectivity against other PARP family enzymes including PARPs 1, 2, and 6. In addition, AZ6102 showed a 5 nM IC50 against Wnt pathway in DLD-1 cells [1].
In vivo: In animal study, AZ6102 was intravenously dosed to nude mice at 25 mg/kg, and the results showed that AZ6102 had a clearance of 24 mL/min·kg and a half-life of 4 h. The bioavailability of AZ6102 in mouse and rat was only moderate at 12% and 18%, respectively. In addition, AZ6102 was used as an intravenous probe compound to evaluate the in vivo effects of TNKS1/2 inhibition on normal tissue and tumor xenografts, however, the results of such experiments have not be released so far [1].
Clinical trial: Up to now, AZ6102 is still in the preclinical development stage.
特別提醒：
1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區。
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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