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PROTAC B-Raf degrader 1

Catalog No.GC65479 Copy One-Click Copy Product Info

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.

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

PROTAC B-Raf degrader 1 Chemical Structure

Cas No.: 2364367-27-9

Size Price Stock Qty
5mg
$442.00
In stock
10mg
$747.00
In stock

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Sample solution is provided at 25 µL, 10mM.



Description of PROTAC B-Raf degrader 1

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity[1].

The IC50 values of PROTAC B-Raf degrader 1 (compound 2) towards MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM, respectively[1].PROTAC B-Raf degrader 1 (5 or 10 μM) can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf[1].MCF-7 cells achieve an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation of PROTAC B-Raf degrader 1 with the concentration of 20 μM[1].PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase[1].

[1]. Chen H, et al. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation. Bioorg Chem. 2019 Mar 19;87:191-199.

Protocol of PROTAC B-Raf degrader 1

B-Raf

 

Chemical Properties of PROTAC B-Raf degrader 1

Cas No. 2364367-27-9 SDF
Formula C36H37N5O12S M.Wt 763.77
Solubility DMSO : 25 mg/mL (32.73 mM; Need ultrasonic) Storage Store at -20°C, stored under nitrogen
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 B-Raf degrader 1

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1 mg 5 mg 10 mg
1 mM 1.3093 mL 6.5465 mL 13.0929 mL
5 mM 261.9 μL 1.3093 mL 2.6186 mL
10 mM 130.9 μL 654.6 μL 1.3093 mL
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In vivo Formulation Calculator (Clear solution) of PROTAC B-Raf degrader 1

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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 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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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