TD-428 |
| カタログ番号GC34319 |
TD-428 は、Cereblon と BRD4 のリガンドで接続された PROTAC です。 TD-428 は、DC50of0.32nM の非常に特異的な BRD4 デグレーダーです。 TD-428 は、JQ1 (BET 阻害剤) に結合した TD-106 (CRBN リガンド) を含む BET PROTAC です。 TD-428 は BET タンパク質の分解を効率的に誘導します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2334525-50-5
Sample solution is provided at 25 µL, 10mM.
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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.
| 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 |
| 溶解度 | 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. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.1372 mL | 5.6858 mL | 11.3716 mL |
| 5 mM | 0.2274 mL | 1.1372 mL | 2.2743 mL |
| 10 mM | 0.1137 mL | 0.5686 mL | 1.1372 mL |
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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 ddH2O, 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.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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