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BI-3802

Cat. No. M21156
BI-3802  Structure
Size Price Availability Quantity
5mg USD 460  USD460 In stock
10mg USD 750  USD750 In stock
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Quality Control & Documentation
Biological Activity

BI-3802 is a potent degradation of oncogenic transcription factor BCL6 with strong inhibitory effect on target genes and anti-proliferative effect.BI-3802 inhibits the BTB structural domain of BCL6, corresponding to an IC50 value ≤ 3 nM.BI-3802 has anti-tumor activity.

Chemical Information
Molecular Weight 484.98
Formula C24H29ClN6O3
CAS Number 2166387-65-9
Solubility (25°C) DMSO : 5 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Solmaz Karimi, et al. Sci Rep. Impact of SNPs, off-targets, and passive permeability on efficacy of BCL6 degrading drugs assigned by virtual screening and 3D-QSAR approach

[2] Lena Nitsch, et al. Cell Rep Methods. BTBBCL6 dimers as building blocks for reversible drug-induced protein oligomerization

[3] Mikołaj Słabicki, et al. Nature. Small-molecule-induced polymerization triggers degradation of BCL6

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  Catalog
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Keywords: BI-3802 supplier, Bcl-2, inhibitors, activators


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