XY-06-007
Tocris Bioscience, part of Bio-Techne | Catalog # 7669
Potent and selective Degrader of Brd4BD1 L94V fusion proteins
Key Product Details
Description
Potent and selective Degrader of Brd4BD1 L94V fusion proteins
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 InstituteProduct Specifications
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.
| 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for XY-06-007
For research use only
Loading...
Loading...