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CCT373566 

Cat. No. M29579
CCT373566  Structure
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Biological Activity

CCT373566 is a potent and orally active degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo.

Chemical Information
Molecular Weight 547
Formula C26H29ClF2N6O3
CAS Number 2378853-66-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Alice C Harnden, et al. J Med Chem. Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

[2] Rosemary Huckvale, et al. J Med Chem. Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

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BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL.

Bim BH3, Peptide IV

Bim BH3, Peptide IV is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins.

Bax inhibitor peptide, negative control

Bax inhibitor peptide, negative control is a inhibitor of Bax.

Bad BH3 (mouse)

Bad BH3 (mouse) is a biological active peptide.

Bid BH3 (80-99)

Bid BH3 (80-99) is a biological active peptide.

  Catalog
Abmole Inhibitor Catalog




Keywords: CCT373566  supplier, Bcl-2, inhibitors, activators


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