AZD-5991

SKU: orb1710350

Description

AZD-5991 is a potent and selective MCL-1 inhibitor that triggers Bak-dependent mitochondrial apoptosis in cancer cells. It is utilized in research for hematological malignancies like multiple myeloma and AML, as well as solid tumors such as triple-negative inflammatory breast cancer, with studies demonstrating activity in both in vitro and in vivo models.

Research Area

Cell Biology

Key Properties

• CAS Number: 2143061-81-6
• MW: 672.26
• Purity: 98.95% (May vary between batches)
• Formula: C₃₅H₃₄ClN₅O₃S₂
• SMILES: Cc1c-2c(CSCc3cc(CSc4cc(OCCCc5c(C(O)=O)n(C)c6c-2c(Cl)ccc56)c2ccccc2c4)n(C)n3)nn1C
• Target: Bcl-2 Family
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (7.44 mM);H2O:＜0.1 mg/mL (insoluble);DMSO:200 mg/mL (297.5 mM)

Bioactivity

• Target IC50:
  McL1:0.7 nM|McL1:0.17 nM (Kd)
• 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).
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZD 5991, AZD5991, AZD-5991, Mcl-1

Compound Identifiers

PubChem CID

131634760