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 100mg |
CAS | 1883429-22-8 |
別名 |
|
化學名 | 4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one |
分子式 | C20H23N3O3 |
分子量 | 353.41 |
溶解度 | DMF: 5 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 5 mg/ml,Ethanol: 2 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: 75 nM and 3.4 μM for BRD9 and BRD7 bromodomains, respectively
BI-9564 is a BRD9/7 specific inhibitor.
BRD7 and BRD9 are two important members of the bromodomain family protein. Both BRD7 and BRD9 have been implicated in chromatin remodeling.
In vitro: BI-9564 was identified as a BRD9/7 specific inhibitor via fragment-based screening and structure-guided design. BI-9564 was found to be bind to BRD9 with a higher affinity than to BRD7, and was negative on BET family proteins. In addition, BI-9564 demonstrated in vitro off-target selectivity to CECR2, but not in cells [1].
In vivo: In animal study, BomTac:NMRIFoxn1nu mice were given two oral doses daily and the concentration of BI-9564 in plasma was measured. Dose-dependent AUCs were obtained for BI-9564, achieving exposures that were higher compared to the EC50 level for EOL-1 cells. Moreover, when the oral treatment with BI-9564 at 180 mg/kg was initiated on day 5 and applied daily with an interruption at day 18 and 19, a significant reduction in tumour growth compared to controls was found on day 18 leading to a median tumour growth inhibition value of 52% [1].
Clinical trial: Up to now, BI-9564 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