dBET6

Tocris Bioscience | Catalog # 6945

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

Key Product Details

Description

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

Product Description

dBET6 is a potent and selective Degrader (PROTAC®) of BET bromodomains (IC50 = ~10 nM). dBET6 comprises BET antagonist (+)-JQ1 (Cat.No. 4499) conjugated to a cereblon E3 ubiquitin ligase ligand. Exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines through BRD4 degradation. Induces apoptosis. Reduces leukemic burden in a mouse model of T-ALL. Cell permeable.

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 dBET6

Molecular Weight

841.38

Formula

C42H45ClN8O7S

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

(6S)-4-(4-Chlorophenyl)-N-[8-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]octyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

CAS Number

1950634-92-0

PubChem ID

121427831

InChI Key

JGQPZPLJOBHHBK-UFXYQILXSA-N

SMILES

CC1=NN=C2[C@H](CC(=O)NCCCCCCCCNC(=O)COC3=C4C(=O)N(C5CCC(=O)NC5=O)C(=O)C4=CC=C3)N=C(C3=C(SC(C)=C3C)N12)C1=CC=C(Cl)C=C1

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 84.14 100

Preparing Stock Solutions for dBET6

The following data is based on the product molecular weight 841.38.

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 1.19 mL 5.94 mL 11.89 mL
5 mM 0.24 mL 1.19 mL 2.38 mL
10 mM 0.12 mL 0.59 mL 1.19 mL
50 mM 0.02 mL 0.12 mL 0.24 mL

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 5 publications citing the usage of this product.

Product Documents for dBET6

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 dBET6

For research use only

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