FKBP12 PROTAC dTAG-13 - CAS 2064175-41-1

FKBP12 PROTAC dTAG-13 is a bifunctional PROTAC® degrader targeting mutant FKBP12F36V fusion proteins, consisting of a ligand selective for F36V single-point mutated FKBP12 conjugated to a cereblon ligand by a linker.

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Molecular Formula
C57H68N4O15
Molecular Weight
1049.17

FKBP12 PROTAC dTAG-13

    • Specification
      • Purity
        ≥95%
        Solubility
        Soluble in DMSO, Ethanol
        Appearance
        White Solid
        Storage
        Store at -20°C
        Shipping
        Room temperature in continental US; may vary elsewhere.
        IUPAC Name
        [(1R)-3-(3,4-dimethoxyphenyl)-1-[2-[2-[6-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyhexylamino]-2-oxoethoxy]phenyl]propyl] (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate
        Synonyms
        (1R)-3-(3,4-Dimethoxyphenyl)-1-(2-(2-((6-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)hexyl)amino)-2-oxoethoxy)phenyl)propyl (2S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate; 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)-; (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 (2S)-1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2-piperidinecarboxylate; dTAG-13
    • Properties
      • Boiling Point
        1134.0±65.0°C at 760 Torr
        Density
        1.260±0.06 g/cm3
        InChI Key
        BJFBRLAWLPZOMJ-QHVFGHLPSA-N
        InChI
        InChI=1S/C57H68N4O15/c1-7-37(36-32-47(71-4)52(73-6)48(33-36)72-5)54(65)60-29-14-12-19-41(60)57(68)76-43(25-22-35-23-26-44(69-2)46(31-35)70-3)38-17-10-11-20-42(38)75-34-50(63)58-28-13-8-9-15-30-74-45-21-16-18-39-51(45)56(67)61(55(39)66)40-24-27-49(62)59-53(40)64/h10-11,16-18,20-21,23,26,31-33,37,40-41,43H,7-9,12-15,19,22,24-25,27-30,34H2,1-6H3,(H,58,63)(H,59,62,64)/t37-,40?,41-,43+/m0/s1
        Canonical SMILES
        O=C(OC(C=1C=CC=CC1OCC(=O)NCCCCCCOC2=CC=CC=3C(=O)N(C(=O)C23)C4C(=O)NC(=O)CC4)CCC5=CC=C(OC)C(OC)=C5)C6N(C(=O)C(C7=CC(OC)=C(OC)C(OC)=C7)CC)CCCC6
        Pub Chem ID
        124187630
    • Reference Reading
      • 1. The dTAG system for immediate and target-specific protein degradation.
        Nabet, B., Roberts, J.M., Buckley, D.L., Paulk, J., Dastjerdi, S., Yang, A., Leggett, A.L., Erb, M.A., Lawlor, M.A., Souza, A. and Scott, T.G., 2018. Nature chemical biology, 14(5), pp.431-441.
        Dissection of complex biological systems requires target-specific control of the function or abundance of proteins. Genetic perturbations are limited by off-target effects, multicomponent complexity, and irreversibility. Most limiting is the requisite delay between modulation to experimental measurement. To enable the immediate and selective control of single protein abundance, we created a chemical biology system that leverages the potency of cell-permeable heterobifunctional degraders. The dTAG system pairs a novel degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. By transgene expression or CRISPR-mediated locus-specific knock-in, we exemplify a generalizable strategy to study the immediate consequence of protein loss. Using dTAG, we observe 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. This technology platform will confer kinetic resolution to biological investigation and provide target validation in the context of drug discovery.
    • Preparing Stock Solutions
      • ConcentrationVolumeMass1 mg5 mg10 mg
        0.5 mM1.91 mL9.53 mL19.06 mL
        2.5 mM0.38 mL1.91 mL3.81 mL
        5 mM0.19 mL0.95 mL1.91 mL
        25 mM0.04 mL0.19 mL0.38 mL
Bio Calculators
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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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