FKBP12 PROTAC dTAG-13 dTAG-13,99.75%

产品编号:Bellancom-114421| CAS NO:2064175-41-1| 分子式:C57H68N4O15| 分子量:1049.17

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-114421
5500.00 杭州 北京(现货)
Bellancom-114421
8800.00 杭州 北京(现货)

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FKBP12 PROTAC dTAG-13 dTAG-13

产品介绍 FKBP12 PROTAC dTAG-13 (dTAG-13) 是一种基于 PROTAC 的双功能降解剂,可降解 FKBP12F36V。FKBP12 PROTAC dTAG-13 有效地接合 FKBP12F36V 和 CRBN,从而选择性地降解 FKBP12F36V
生物活性

FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12F36V and CRBN, thereby selectively degrading FKBP12F36V.

体外研究

TAG-13 (1-1000 nM; 4 hours; 293FTWT cells) treatment potently reduces FKBP12F36V-Nluc levels in 293FTWT cell, indicating the requirement of CRBN for the observed effects.
Treatment of MV4;11 cells expressing BRD4(short)-FKBP12F36V with dTAG-13 leads to robust degradation of BRD4. dTAG-13 treatment leads to rapid degradation of BRD4 within one hou. dTAG-13 treatment leads to rapid and potent degradation of the BRD4 fusion chimera in the heterozygous and homozygous knock-in clones, with no effect on endogenous FKBP12WT.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line: 293FTWT cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 4 hours
Result: Potently reduced FKBP12F36V-Nluc levels in 293FTWT cell.
体内研究
(In Vivo)

Following bone marrow engraftment of MV4;11 cells expressing luc-FKBP12F36V in mice, the bioluminescent signal after vehicle or dTAG-13 administration is monitored. A significant, rapid, and durable effect on bioluminescent signal is observed four hours after dTAG-13 administration, indicating effective degradation of luc-FKBP12F36V. Twenty-eight hours following the final treatment, the recovery of cellular bioluminescence to levels comparable between vehicle and dTAG-13 treatment groups is observed.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Following bone marrow engraftment of MV4;11 cells expressing luc-FKBP12F36V in mice, the bioluminescent signal after vehicle or dTAG-13 administration is monitored. A significant, rapid, and durable effect on bioluminescent signal is observed four hours after dTAG-13 administration, indicating effective degradation of luc-FKBP12F36V. Twenty-eight hours following the final treatment, the recovery of cellular bioluminescence to levels comparable between vehicle and dTAG-13 treatment groups is observed.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Following bone marrow engraftment of MV4;11 cells expressing luc-FKBP12F36V in mice, the bioluminescent signal after vehicle or dTAG-13 administration is monitored. A significant, rapid, and durable effect on bioluminescent signal is observed four hours after dTAG-13 administration, indicating effective degradation of luc-FKBP12F36V. Twenty-eight hours following the final treatment, the recovery of cellular bioluminescence to levels comparable between vehicle and dTAG-13 treatment groups is observed.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状Solid
溶解性数据
In Vitro: 

DMSO : 180 mg/mL (171.56 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9531 mL 4.7657 mL 9.5313 mL
5 mM 0.1906 mL 0.9531 mL 1.9063 mL
10 mM 0.0953 mL 0.4766 mL 0.9531 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
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