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FKBP12 PROTAC dTAG-13

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Chemical Structure| 2064175-41-1 同义名 : Dtag-13
CAS号 : 2064175-41-1
货号 : A1147986
分子式 : C57H68N4O15
纯度 : 99%
分子量 : 1049.168
MDL号 : N/A
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(100.08 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 dTAG-13 is a thalidomide-based PROTAC targeting mutant FKBP12F36V fusion proteins. dTAG-13 at concentration of 500nM could almost completely degrade the carboxy-terminal FKBP12F36V fusions in MV4;11-Cas9 cells post 1h. dTAG-13 inhibited cell proliferation of MV4;11 (Cas9+, ENL-FKBP12F36V–HA+) cells with IC50 value of 49.7nM post 72-hour treatment[1]. Treatment with 100nM for 4h selectively degraded FKBP12F36V in a CRBN-dependent manner in 293FTWT expressing FKBP12F36V. Also, dTAG-13 at concentration of 500nM could efficiently led a rapid degradation of a various nuclear and cytoplasmic FKBP12F36V fusion chimeras, including HDAC1-FKBP12F36V, MYC-FKBP12F36V, PLK1-FKBP12F36V, FKBP12F36V-EZH2, FKBP12F36V-KRASG12V, in MV4;11 cells expressing these fusion chimeras post 24-hour treatment. The degradation of FKBP12F36V-KRASG12V by dTAG-13 caused the decrease of pAkt-S473 and pMek-S221 in a time- and dose-dependent manner, exhibited an anti-proliferative effect on NIH/3T3 cells expressing FKBP12F36V-KRASG12V, as well as rapidly reversed the deregulated proteomic and transcriptional signaling program of transformed cells. Administration of dTAG-13 at dose of 25mg/kg effective degradation of FKBP12F36V in vivo[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.95mL

0.19mL

0.10mL

4.77mL

0.95mL

0.48mL

9.53mL

1.91mL

0.95mL
参考文献

[1]Erb MA, Scott TG, et al. Transcription control by the ENL YEATS domain in acute leukaemia. Nature. 2017 Mar 9;543(7644):270-274.

[2]Nabet B, Roberts JM, et al. The dTAG system for immediate and target-specific protein degradation. Nat Chem Biol. 2018 May;14(5):431-441.