[CAS NO. 2143010-83-5] AZD5991
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PRODUCTS SPECIFICATIONS [2143010-83-5]
Store
Catalog
SLK-S8643
Brand
Selleck
CAS
2143010-83-5
DESCRIPTION [2143010-83-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 672.26 |
| Molecular Formula | C35H34ClN5O3S2 |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4875 mL | 7.4376 mL | 14.8752 mL |
| 5 mM | 0.2975 mL | 1.4875 mL | 2.9750 mL |
| 10 mM | 0.1488 mL | 0.7438 mL | 1.4875 mL |
| 50 mM | 0.0298 mL | 0.1488 mL | 0.2975 mL |
Description
AZD5991 is a macrocyclic inhibitor with sub-nanomolar affinity for MCL-1 (Ki = 0.13 nM). The binding affinity of AZD5991 is about 25-fold lower for mouse Mcl-1 vs. human Mcl-1 but only four-fold lower for rat Mcl-1.
In vitro
AZD5991 is a potent and direct inhibitor of Mcl-1 with high selectivity versus other Bcl-2 family proteins. 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.
References
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