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BI-3802

Catalog No.GC32178

BI-3802 is a highly potent BCL6 degrader and inhibits the Bric-à-brac (BTB) domain of BCL6 with an IC50 of ≤3 nM. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1. BI-3802 has antitumor activity.

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BI-3802 Chemical Structure

Cas No.: 2166387-65-9

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

BI-3802 is a highly potent BCL6 degrader, inhibiting the BTB domain of BCL6, with an IC50 of ≤3 nM; BI-3802 has antitumor activity.

BI-3802 is a BCL6 inhibitor, with an IC50 of ≤3 nM. BI-3802 shows an IC50 of 43 nM for the cellular BCL6[1].

[1]. Kerres N, et al. Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6. Cell Rep. 2017 Sep 19;20(12):2860-2875.

Chemical Properties

Cas No. 2166387-65-9 SDF
Canonical SMILES ClC1=CN=C(N2C[C@H](C)C[C@H](C)C2)N=C1NC3=CC(C=C(OCC(NC)=O)C(N4C)=O)=C4C=C3
Formula C24H29ClN6O3 M.Wt 484.98
Solubility DMSO : 5 mg/mL (10.31 mM);Methanol : 2 mg/mL (4.12 mM; ultrasonic and adjust pH to 5 with 1M HCl);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

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1 mg 5 mg 10 mg
1 mM 2.0619 mL 10.3097 mL 20.6194 mL
5 mM 0.4124 mL 2.0619 mL 4.1239 mL
10 mM 0.2062 mL 1.031 mL 2.0619 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.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 11 reference(s) in Google Scholar.)

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