TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.
CAS Number: 2334525-50-5
Molecular Weight: 879.38
Chemical Name: 2-((S)-4-(4-chlorophenyl)-2, 3, 9-trimethyl-6H-thieno[3, 2-f][1, 2, 4]triazolo[4, 3-a][1, 4]diazepin-6-yl)-N-(3-(2-(2-(2-((3-(2, 6-dioxopiperidin-3-yl)-4-oxo-3, 4-dihydrobenzo[d][1, 2, 3]triazin-5-yl)amino)ethoxy)ethoxy)ethoxy)phenyl)acetamide
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
TD-428, which comprises TD-106 linked to a BET inhibitor, JQ1 efficiently induce BET protein degradation in the prostate cancer cell line 22Rv1. TD-428 (0.01-10, 000 nM; 72 hours) inhibits the proliferation of 22RV1 cells with a CC50 of 20.1 nM. TD-428 (1 nM-10 μM; 12 hours) induces the degradation of BRD4, IKZF1, and IKZF3 proteins.
- Scheepstra M, et al. Bivalent Ligands for Protein Degradation in Drug Discovery. Comput Struct Biotechnol J. 2019 Jan 25;17:160-176.
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