FKBP12 PROTAC dTAG-13

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CAS NO:

2064175-41-1

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品名称

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FKBP12^F36V。FKBP12 PROTAC dTAG-13 有效地接合FKBP12^F36V和 CRBN，从而选择性地降解FKBP12^F36V。

生物活性

FKBP12PROTACdTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader ofFKBP12^F36Vwith expression of FKBP12F36V in-frame with a protein of interest. FKBP12PROTACdTAG-13 effectively engagesFKBP12^F36Vand CRBN, thereby selectively degradingFKBP12^F36V^[1].

IC₅₀& Target^[1]

Cereblon

FKBP12(F36V)

体外研究
(In Vitro)

TAG-13 (1-1000 nM; 4 hours; 293FT^WTcells) treatment potently reduces FKBP12^F36V-Nluc levels in 293FT^WTcell, indicating the requirement of CRBN for the observed effects^[1].
Treatment of MV4;11 cells expressing BRD4(short)-FKBP12^F36Vwith 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 FKBP12^WT^[1].

Western Blot Analysis^[1]

Cell Line:	293FT^WTcells
Concentration:	1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time:	4 hours
Result:	Potently reduced FKBP12^F36V-Nluc levels in 293FT^WTcell.

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^[1].

分子量

1049.17

性状

Solid

Formula

C₅₇H₆₈N₄O₁₅

CAS 号

2064175-41-1

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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。