XY-06-007

Name: XY-06-007
Brand: Tocris Bioscience
SKU: 7669

Tocris Bioscience, part of Bio-Techne | Catalog # 7669

COA / SDS

Potent and selective Degrader of Brd4BD1 L94V fusion proteins

Key Product Details

Description:	Potent and selective Degrader of Brd4^{BD1 L94V} fusion proteins
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
Purity:	≥98% (HPLC)
Molecular Weight:	809.28

View Full Technical Details for XY-06-007

Technical Data
Citations

Biological Activity for XY-06-007

XY-06-007 is a highly selective and potent "Bump & Hole" TAG Degrader (DC_50,6h = 10 nM, T_1/2 < 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 Brd4^{BD1 L94V} variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4^{BD1 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 Brd4^{BD1 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

Technical Data for XY-06-007

M. Wt	809.28
Formula	C₄₁H₄₁ClN₈O₈
Storage	Store at -20°C
Purity	≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for XY-06-007

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 will affect the solvent volumes required to prepare stock solutions.

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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References for XY-06-007

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

Nowak Structure-guided design of a "Bump-and-Hole" Bromodomain-based degradation tag. J.Med.Chem. 2021 PMID: 34279939