dBET1
Tocris Bioscience, part of Bio-Techne | Catalog # 6327
(+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
Key Product Details
Description
(+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
Product Description
dBET1 is a Degrader (PROTAC®) comprising BET bromodomain antagonist (+)-JQ1 (Cat. No. 4499) conjugated to a cereblon E3 ubiquitin ligase ligand. Depletes BET bromodomains in cancer cell lines in vitro (EC50 = 430 nM in breast cancer cells) and induces apoptosis. Delays tumor growth and downregulates MYC in mice bearing human AML xenografts. Antibody validated for Western Blot also available: NBP2-77359.PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Licensing Information
Sold under license from Dana-Farber Cancer Institute.Product Specifications
Molecular Weight
785.27
Formula
C38H37ClN8O7S
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(6S)-4-(4-Chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
CAS Number
1799711-21-9
PubChem ID
91799313
InChI Key
LKEGXJXRNBALBV-PMCHYTPCSA-N
SMILES
CC1=NN=C2[C@@H](N=C(C3=CC=C(C=C3)Cl)C4=C(N12)SC(C)=C4C)CC(NCCCCNC(COC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 78.53 | 100 |
Preparing Stock Solutions
for dBET1
The following data is based on the product molecular weight 785.27
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.27 mL | 6.37 mL | 12.73 mL |
| 5 mM | 0.25 mL | 1.27 mL | 2.55 mL |
| 10 mM | 0.13 mL | 0.64 mL | 1.27 mL |
| 50 mM | 0.03 mL | 0.13 mL | 0.25 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Wurz A "click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 2017 PMID: 28378579
- Winter Drug Development. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science 2015 PMID: 25999370
Product Specific Notices for dBET1
For research use only
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