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AZD-5991, an antitumor compound, is a highly selective, potent and direct MCL-1 inhibitor that induces rapid apoptosis in cancer cells by activating the Bak-dependent mitochondrial apoptotic pathway, used for multiple myeloma, acute myeloid leukemia, and triple-negative inflammatory breast cancer.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $356 | 5 days |
Description | AZD-5991, an antitumor compound, is a highly selective, potent and direct MCL-1 inhibitor that induces rapid apoptosis in cancer cells by activating the Bak-dependent mitochondrial apoptotic pathway, used for multiple myeloma, acute myeloid leukemia, and triple-negative inflammatory breast cancer. |
Targets&IC50 | McL1:0.7 nM, McL1:0.17 nM (Kd) |
In vitro | Methods: A panel of MCL cell lines were treated with AZD-5991 (10-1000 nM, 24 hours) and cell viability was measured using the CellTiter-Glo cell viability assay (Promega). Results: MCL cell lines that were sensitive or resistant to ibrutinib or venetoclax were sensitive to AZD-5991 (IC50 values ranged from 69.3 to 523.5 nM), with Mino showing particularly high sensitivity to AZD-5991. [2] |
In vivo | Methods: MOLP-8 tumor model mice were treated with AZD-5991 (10-100 mg/kg, intravenous injection) and the efficacy of AZD-5991 on MOLP-8 tumor growth in vivo was evaluated. Results: AZD-5991 produced dose-dependent antitumor effects ranging from tumor growth inhibition (TGI) to tumor regression (TR). After ten days of treatment, AZD-5991 showed a TGI of 52% and 93% at 10 and 30 mg/kg, respectively (p < 0.0001). [1] |
Alias | AZD5991 |
Molecular Weight | 672.26 |
Formula | C35H34ClN5O3S2 |
Cas No. | 2143061-81-6 |
Smiles | Cc1c-2c(CSCc3cc(CSc4cc(OCCCc5c(C(O)=O)n(C)c6c-2c(Cl)ccc56)c2ccccc2c4)n(C)n3)nn1C |
Relative Density. | 1.42 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: <0.1 mg/mL (insoluble) DMSO: 200 mg/mL (297.5 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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