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.
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 |
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.
[2] Thomas P Garner, et al. Curr Opin Chem Biol. Progress in targeting the BCL-2 family of proteins
Related Bcl-2 Products |
---|
BAD (103-127) (human)
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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.