>>Signaling Pathways>> PROTAC>>PROTAC BET Degrader-1

PROTAC BET Degrader-1

Catalog No.GC33109

PROTAC BET Degrader-1은 Cereblon과 BET의 리간드로 연결된 PROTAC으로 저농도에서 BRD2, BRD3, BRD4 단백질 수준을 감소시킨다.

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

PROTAC BET Degrader-1 Chemical Structure

Cas No.: 2093386-22-0

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$750.00
재고 있음
5mg
US$506.00
재고 있음
10mg
US$782.00
재고 있음
25mg
US$1,701.00
재고 있음

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


고객 리뷰

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

Description of PROTAC BET Degrader-1

PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

PROTAC BET Degrader-1 (Compound 9) is a potent BET degrader based on PROTAC, decreases the level of BRD2, BRD3, and BRD4 proteins in RS4;11 cells at 3-10 nM, and inhibits the growth of this cell line with an IC50 of 4.3 nM, and 45.5 nM for MOLM-13 cells[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-1

Cas No. 2093386-22-0 SDF
Canonical SMILES CCN1C(NC2=C3C4=CC(OC)=C(C(C(C)=NO5)=C5C)C=C4NC3=NC(C(NCCCCNC(COC6=C(C(N7C(CCC8=O)C(N8)=O)=O)C(C7=O)=CC=C6)=O)=O)=N2)=CC(C9CC9)=N1
Formula C44H45N11O9 M.Wt 871.9
Solubility DMSO : ≥ 50 mg/mL (57.35 mM) 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-1

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.1469 mL 5.7346 mL 11.4692 mL
5 mM 229.4 μL 1.1469 mL 2.2938 mL
10 mM 114.7 μL 573.5 μL 1.1469 mL
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In vivo Formulation Calculator (Clear solution) of PROTAC BET Degrader-1

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

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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.)

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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 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.

Product Documents

Quality Control & SDS

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리뷰

Review for PROTAC BET Degrader-1

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

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