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AZD-5991 Racemate

Cat. No. M10283
AZD-5991 Racemate Structure
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50mg USD 1800  USD1800 Out of stock
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Biological Activity

AZD-5991 Racemate is a Mcl-1 inhibitor with an IC50 of <3 nM in FRET assay. AZD-5991 Racemate is the racemate of AZD-5991. AZD5991 binds directly to Mcl-1 and induces rapid apoptosis in cancer cells, most notably myeloma and acute myeloid leukemia (GI50 < 100nM), by activating the Bak-dependent mitochondrial apoptotic pathway. In a panel of cancer-derived cell lines of hematological or solid tumor origin, AZD5991 preferentially kills hematological cells.

Chemical Information
Molecular Weight 672.26
Formula C35H34ClN5O3S2
CAS Number 2143010-83-5
Solubility (25°C) DMSO
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] Adriana E Tron, et al. Nat Commun. Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia

[2] Thomas P Garner, et al. Curr Opin Chem Biol. Progress in targeting the BCL-2 family of proteins

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Keywords: AZD-5991 Racemate supplier, Bcl-2, inhibitors, activators


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