dBET1

Tocris Bioscience | Catalog # 6327

(+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
Tocris Bioscience

Key Product Details

Description

(+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
View all Active Degraders »

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 for dBET1

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.

Select a batch to recalculate based on the batch molecular weight:

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

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 3 publications citing the usage of this product.

Product Documents for dBET1

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for dBET1

For research use only

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