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AZD4320 

Cat. No. M28240
AZD4320  Structure
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Biological Activity

AZD4320 is a novel BH3-mimicking dual BCL2/BCLxL inhibitor with IC50s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively.

Chemical Information
Molecular Weight 945.53
Formula C45H48ClF3N4O7S3
CAS Number 1357576-48-7
Form Solid
Solubility (25°C) DMSO 125 mg/mL (ultrasonic)
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] Wenwen Chien, et al. J Ovarian Res. Treatment for ovarian clear cell carcinoma with combined inhibition of WEE1 and ATR

[2] Surein Arulananda, et al. Cell Death Discov. A novel BH3-mimetic, AZD0466, targeting BCL-XL and BCL-2 is effective in pre-clinical models of malignant pleural mesothelioma

[3] Claire M Patterson, et al. Commun Biol. Design and optimisation of dendrimer-conjugated Bcl-2/xL inhibitor, AZD0466, with improved therapeutic index for cancer therapy

[4] Srividya B Balachander, et al. Clin Cancer Res. AZD4320, A Dual Inhibitor of Bcl-2 and Bcl-xL, Induces Tumor Regression in Hematologic Cancer Models without Dose-limiting Thrombocytopenia

[5] Tomoko Takimoto-Shimomura, et al. Invest New Drugs. Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2

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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)

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  Catalog
Abmole Inhibitor Catalog




Keywords: AZD4320  supplier, Bcl-2, inhibitors, activators


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