TD-428


Catalog No. Size PriceQuantity
M8006-2 contact us $525
M8006-10 contact us $2,100

Description

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.

Product information

CAS Number: 2334525-50-5

Molecular Weight: 879.38

Formula: C43H43ClN10O7S

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

Smiles: CC1=NN=C2[C@H](CC(=O)NC3=CC(=CC=C3)OCCOCCOCCNC3=CC=CC4N=NN(C5CCC(=O)NC5=O)C(=O)C=43)N=C(C3=CC=C(Cl)C=C3)C3=C(SC(C)=C3C)N12

InChiKey: XEZUBGASURUNMF-CDRRMRQFSA-N

InChi: InChI=1S/C43H43ClN10O7S/c1-24-25(2)62-43-37(24)39(27-10-12-28(44)13-11-27)47-33(40-51-49-26(3)53(40)43)23-36(56)46-29-6-4-7-30(22-29)61-21-20-60-19-18-59-17-16-45-31-8-5-9-32-38(31)42(58)54(52-50-32)34-14-15-35(55)48-41(34)57/h4-13,22,33-34,45H,14-21,23H2,1-3H3,(H,46,56)(H,48,55,57)/t33-,34?/m0/s1

Technical Data

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

In Vitro:

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.

References:

  1. Scheepstra M, et al. Bivalent Ligands for Protein Degradation in Drug Discovery. Comput Struct Biotechnol J. 2019 Jan 25;17:160-176.

Products are for research use only. Not for human use.

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed