|4-((3-环丙基-1-乙基-1H-吡唑-5-基)氨基)-7-(3,5-二甲基异唑-4-基)-N-(5-(2-(2,6- 二氧代哌啶-3-基)-1-氧代异吲哚啉-4-基)戊基)-6-甲氧基-9H-嘧啶并[4,5-b]吲哚-2-甲酰胺|CsnPharm

CAS No.: 2093388-62-4

BETd-260 Catalog No. CSN21389

Synonyms: ZBC 260

PROTAC BET Degrader 23 is a highly potent and efficacious PROTAC targeting on BET with DC50 value of 30pM for degradation of BRD4 in RS4;11 leukemia cell line.

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400-920-2911

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靶点选择性

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实验方案

技术信息

生物活性

描述PROTAC BET Degrader 23 is a highly potent and efficacious PROTAC targeting on BET with DC50 value of 30pM for degradation of BRD4 in RS4;11 leukemia cell line. PROTAC BET Degrader 23 effectively degraded BRD2, 3 and 4 at concentration of 1nM post 3-hour treatment in RS4;11 cells. A dose-dependent downregulation of c-MYC, a BET target gene, could be observed accompanied with the decreased BET in RS4;11 cells post 24-hour treatment with PROTAC BET Degrader 23 at concentration ranging in 0.03-10nM. PROTAC BET Degrader 23 strongly induced cell cycle arrest in both RS4;11 cell line and MOLM-13 cell line as low as 0.3nM, as well as a robust apoptosis at 3−10 nM concentrations with a 24 h treatment. Administration of PROTAC BET Degrader 23 at dose of 5mg/kg, i.v., every other day, three times a week for 3 weeks, achieved rapid tumor regression with a maximum of >90% regression observed in the xenograft model of human RS4;11 tumor cells^[1].
动物研究
剂量
Mice: 5 mg/kg^[1] (i.v.)

给药途径
i.v.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[1] (i.v.)
给药途径	i.v.

[1] Zhou B, Hu J, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2517 mL
- 6.2587 mL
- 12.5174 mL
- 5 mM
- 0.2503 mL
- 1.2517 mL
- 2.5035 mL
- 10 mM
- 0.1252 mL
- 0.6259 mL
- 1.2517 mL

技术信息

CAS号	2093388-62-4	储存条件	粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C43H46N10O6	运输	蓝冰
分子量	798.89	别名	ZBC 260

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