XY-06-007

Tocris Bioscience | Catalog # 7669

Potent and selective Degrader of Brd4BD1 L94V fusion proteins
Tocris Bioscience

Key Product Details

Description

Potent and selective Degrader of Brd4BD1 L94V fusion proteins
View all TAG Degradation Platforms »

Product Description

XY-06-007 is a highly selective and potent "Bump & Hole" TAG Degrader (DC50,6h = 10 nM, T1/2 < 43.2 min). XY-06-007 comprises a cereblon (CRBN) E3 ligase ligand joined by a linker to a (+)-JQ1 (Cat. No. 4499) derivative (the "bump" bearer) that selectively binds the Brd4BD1 L94V variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4BD1 L94V, XY-06-007 drives formation of a ternary complex between CRBN and the tagged protein, leading to ubiquitination and subsequent proteasomal degradation of the entire protein. XY-06-007 is highly selective for Brd4BD1 L94V over wild-type, and is broadly selective across the proteome. XY-06-007 can be combined with the dTAG approach to achieve simultaneous degrader-mediated depletion of their respective protein fusions. XY-06-007 is suitable for in vivo studies.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Product Specifications for XY-06-007

Molecular Weight

809.28

Formula

C41H41ClN8O8

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

(2R)-2-((S)-6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-(5-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)pentyl)propanamide

CAS Number

2757045-94-4

PubChem ID

162526515

InChI Key

QTDHGBJLMBQHOW-BPJPHOPQSA-N

SMILES

COC1=CC=C(C2=C1)N3C([C@H]([C@@H](C)C(NCCCCCNC(COC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C

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 80.93 100

Preparing Stock Solutions for XY-06-007

The following data is based on the product molecular weight 809.28.

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 1.24 mL 6.18 mL 12.36 mL
5 mM 0.25 mL 1.24 mL 2.47 mL
10 mM 0.12 mL 0.62 mL 1.24 mL
50 mM 0.02 mL 0.12 mL 0.25 mL

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Background References

References are publications that support the biological activity of the product.

Product Documents for XY-06-007

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 XY-06-007

For research use only

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