|2-((S)-4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-f][1,2,4]三唑并[4,3-a][1,4]二氮杂卓-6-基)-N-(4-(2-((2-(2,6-二氧代哌啶-3-基)-1,3-二氧代异吲哚啉-4-基)氧基)乙酰氨基)丁基)乙酰胺|CsnPharm

CAS No.: 1799711-21-9

dBET1 Catalog No. CSN22286

Synonyms: JQ1-Thalidomide conjugate

dBET1 is a PROTAC, consisting of a BRD4-ligand JQ-1 linkerd to a cereblon E3 ligase ligand, targeting on BET bromodomain BRD4

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述dBET1 is a PROTAC, consisting of a BRD4-ligand JQ-1 linkerd to a cereblon E3 ligase ligand, targeting on BET bromodomain BRD4 with DC50 values of < 100nM and 140nM for degradation of BRD4 protein in MV4-11 cells post 18-hour treatment and in H661 cells post 4-hour treatment. dBET1 exhibited a bell-shaped dose−response curve in the cereblon/PROTAC/BRD4 proximity assay^[1]. Treatment with dBET1 resulted a depletion of BRD4 in MV4;11 cells at concentration ranging in 0.1-10μM post 18h and a downregulation of BRD4 by 95 at concentration of 100nM post 2h. Similarly, a dose-dependent degradation of BRD4 could be observed in MM1S cells exposure to dBET1 at concentration ranging in 0.5-10μM post 18-hour treatment. The degradation of BRD4 by treatment with 250nM dBET1 for 2h led a decrease of transcription of BRD2, BRD3, MYC and PIM1 targeted by BRD4, in MV4;11 cells. dBET1 at concentration of 0.25μM, 1μM and 2.5μM caused apoptosis of MV4;11 and DHL4 cells more potently than JQ1 post 24h, which could be marked by cleaved PARP and Caspase-3 at 4h or 8h. Similar increase of apoptosis of primary AML cells could be observed by treatment with 1μM and 10μM dBET1 post 24h. Intraperitoneal administration of 50mg/kg dBET1 daily for 14 days achieved suppression of tumor growth MV4;11 xenograft mice. Decreased leukemic burden in bone marrow could be achieved by 19-day administration. dBET1(R) works as a negative control of dBET1^[2].
动物研究
剂量
Mice: 10 mg/kg^[5] (i.p.), 50 mg/kg^[2] (i.p.)

给药途径
i.p.

动物研究
剂量	Mice: 10 mg/kg^[5] (i.p.), 50 mg/kg^[2] (i.p.)
给药途径	i.p.

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
- 1.2734 mL
- 6.3672 mL
- 12.7345 mL
- 5 mM
- 0.2547 mL
- 1.2734 mL
- 2.5469 mL
- 10 mM
- 0.1273 mL
- 0.6367 mL
- 1.2734 mL

技术信息

CAS号

1799711-21-9

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C38H37ClN8O7S

运输

蓝冰

分子量

785.27

别名

JQ1-Thalidomide conjugate

溶解度

DMSO	100.0 mg/mL (127.3 mM)
Water	Insoluble
Ethanol	39.0 mg/mL (49.7 mM)

动物实验配方

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dBET1 Catalog No. CSN22286

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