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PROTAC BET degrader-2

Catalog No.GC32980

PROTAC BET degradador-2 es un PROTAC conectado por ligandos para Cereblon y BET con un valor IC50 de 9,6 nM en la inhibiciÓn del crecimiento celular en las células RS4;11 y capaz de lograr la regresiÓn tumoral.

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

PROTAC BET degrader-2 Chemical Structure

Cas No.: 2093388-33-9

Tamaño Precio Disponibilidad Cantidad
1mg
196,00 $
Disponible
5mg
432,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description of PROTAC BET degrader-2

PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.

PROTAC BET degrader-2 (compound 25) is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression[1].

[1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.

Chemical Properties of PROTAC BET degrader-2

Cas No. 2093388-33-9 SDF
Canonical SMILES O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NCCCC7=CC=CC8=C7CN(C(CC9)C(NC9=O)=O)C8=O
Formula C41H42N10O6 M.Wt 770.84
Solubility DMSO : 50 mg/mL (64.86 mM);Water : < 0.1 mg/mL (insoluble) 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 PROTAC BET degrader-2

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1 mg 5 mg 10 mg
1 mM 1.2973 mL 6.4864 mL 12.9729 mL
5 mM 0.2595 mL 1.2973 mL 2.5946 mL
10 mM 0.1297 mL 0.6486 mL 1.2973 mL
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In vivo Formulation Calculator (Clear solution) of PROTAC BET degrader-2

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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.

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Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

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