Home>>Signaling Pathways>> PROTAC>>TD-428

TD-428

Catalog No.GC34319 Copy One-Click Copy Product Info

TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. 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.

Products are for research use only. Not for human use. We do not sell to patients.

TD-428 Chemical Structure

Cas No.: 2334525-50-5

Size Price Stock Qty
250mg Please Inquire Please Inquire
500mg Please Inquire Please Inquire

Tel:(909) 407-4943 Email: sales@glpbio.com


Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.



Description of TD-428

TD-428 is a highly specific BRD4 degrader with a DC50?of?0.32?nM[1].

TD-428, the BRD4 degrader with TD-106, is highly specific for BET proteins. TD-428 (0.01, 0.1, 1, 10, 100, 1000, and 10000 nM; 72?hours) inhibits the proliferation of 22RV1 cells with a CC50?of??20.1?nM[1].|| Cell Cytotoxicity Assay[1]|| Cell Line:|22RV1 cells|Concentration:|0.01, 0.1, 1, 10, 100, 1000, and 10000 nM|Incubation Time:|72?hours|Result:|Inhibited cell proliferation with a CC50?of?20.1?nM.|| Western Blot Analysis[1]||Cell Line:|U266 cells |Concentration:|1 nM, 10 nM, 100nM, 1000 nM, and 10?μM|Incubation Time:|12?hours|Result:|Induced the degradation of BET proteins.

[1]. Kim SA, et al. A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74.

Chemical Properties of TD-428

Cas No. 2334525-50-5 SDF
Canonical SMILES O=C(NC1=CC(OCCOCCOCCNC2=C3C(N=NN(C(CC4)C(NC4=O)=O)C3=O)=CC=C2)=CC=C1)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5
Formula C43H43ClN10O7S M.Wt 879.38
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of TD-428

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.1372 mL 5.6858 mL 11.3716 mL
5 mM 227.4 μL 1.1372 mL 2.2743 mL
10 mM 113.7 μL 568.6 μL 1.1372 mL
  • Molarity Calculator

  • Dilution Calculator

  • Molecular Weight Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution) of TD-428

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % saline
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

Quality Control & SDS

View current batch:

Reviews

Review for TD-428

Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%