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Catalog:
SLK-S8643
Brand:
Selleck
CAS:
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
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.
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.
