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FKBP12 PROTAC dTAG-13

Names

[ CAS No. ]:
2064175-41-1

[ Name ]:
FKBP12 PROTAC dTAG-13

[Synonym ]:
(1R)-3-(3,4-Dimethoxyphenyl)-1-(2-{2-[(6-{[2-(2,6-dioxo-3-piperidinyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]oxy}hexyl)amino]-2-oxoethoxy}phenyl)propyl (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]-2-piperidinecarboxylate
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)-

Biological Activity

[Description]:

FKBP12 PROTAC dTAG-13 (dTAG-13) is an in vivo-active heterobifunctional adation tag (dTAG) small molecule that engage FKBP12F36V and CRBN, selectively degrade FKBP12F36V in a CRBN-dependent manner in cells; causes rapid degradation of nuclear and cytoplasmic FKBP12F36V fusion chimeras, and an unexpected superior antiproliferative effect of pan-BET bromodomain degradation over selective BRD4 degradation, characterize immediate effects of KRASG12V loss on proteomic signaling, and demonstrate rapid degradation in vivo.

[References]

References 1. Nabet B, et al. Nat Chem Biol. 2018 May;14(5):431-441. View Related Products by Target PROTAC

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
1134.0±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C57H68N4O15

[ Molecular Weight ]:
1049.168

[ Flash Point ]:
639.6±34.3 °C

[ Exact Mass ]:
1048.468140

[ LogP ]:
6.98

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.581

Related Compounds