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AZD-5991

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Catalog No. T10434Cas No. 2143061-81-6
Alias AZD5991

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.

AZD-5991

AZD-5991

😃Good
Purity: 98.08%
Catalog No. T10434Alias AZD5991Cas No. 2143061-81-6
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.
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2 mg$356 5 days
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Purity:98.08%
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Product Introduction

Bioactivity
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]
AliasAZD5991
Chemical Properties
Molecular Weight672.26
FormulaC35H34ClN5O3S2
Cas No.2143061-81-6
SmilesCc1c-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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM1.4875 mL7.4376 mL14.8752 mL74.3760 mL
5 mM0.2975 mL1.4875 mL2.9750 mL14.8752 mL
10 mM0.1488 mL0.7438 mL1.4875 mL7.4376 mL
20 mM0.0744 mL0.3719 mL0.7438 mL3.7188 mL
50 mM0.0298 mL0.1488 mL0.2975 mL1.4875 mL
100 mM0.0149 mL0.0744 mL0.1488 mL0.7438 mL

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