| Identification | Back Directory | [Name]
dTAG-13 | [CAS]
2064175-41-1 | [Synonyms]
dTAG-13
FKBP12 PROTAC DTAG-13
2-Piperidinecarboxylic acid, 1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-, (1R)-3-(3,4-dimethoxyphenyl)-1-[2-[2-[[6-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]hexyl]amino]-2-oxoethoxy]phenyl]propyl ester, (2S)- | [Molecular Formula]
C57H68N4O15 | [MDL Number]
MFCD32670722 | [MOL File]
2064175-41-1.mol | [Molecular Weight]
1049.17 |
| Chemical Properties | Back Directory | [Melting point ]
106-111°C | [Boiling point ]
1134.0±65.0 °C(Predicted) | [density ]
1.260±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C Freezer | [solubility ]
DMF (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
10.70±0.40(Predicted) | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Uses]
dTAG-13 is a degradation tag which was tested for its efficiency at depleting FKBP12F36V -MELK(sg3R) and was found to have significantly degraded FKBP12F36V -MELK(sg3R) within 4 hours.Used in the study of cancer research. | [Biological Activity]
dTAG-13 is a degradation tag (dTAG) system heterobifunctional degrader composed of an E3 ubiquitin ligase cereblon (CRBN)-binding thalidomide moiety and an FKBP12(F36V) mutant-specific ligand AP1867 void of affinity for endogenous (wild-type) FKBP12allowing selective degradation of target proteins of interest when expressed as an FKBP12(F36V) in-frame fusion (by transgene expression or locus-specific knock-in) by bridging them with CRBN for ubiquitination. dTAG-13 is shown to potently degrade FKBP12F36V-MELK(sg3R) in MDA-MB-468 cells (100 nM for 4 hrs) as well as ENL-FKBP12F36V-HAbut not endogenous ENLin MV4;1 cells (500 nM for 0.5-1 hrs). | [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]. | [IC 50]
Cereblon; FKBP12(F36V) | [storage]
Store at -20°C |
|
|