AZD5582 TFA

SKU: orb1819263

Description

AZD5582 TFA is a potent small molecule antagonist of IAP proteins (cIAP1, cIAP2, XIAP) that promotes apoptosis. It is widely used in cancer research to study programmed cell death mechanisms in both cellular and animal models of oncology.

Research Area

Cell Biology, Immunology & Inflammation

Key Properties

• MW: 1129.31
• Purity: 98.83% (May vary between batches)
• Formula: C₆₀H₇₉F₃N₈O₁₀
• SMILES: O=C([C@H]1N(CCC1)C([C@H](C2CCCCC2)NC([C@H](C)NC)=O)=O)N[C@H]3C4=CC=CC=C4C[C@H]3OCC#CC#CCO[C@H]5[C@H](C6=CC=CC=C6C5)NC([C@H]7N(CCC7)C([C@H](C8CCCCC8)NC([C@H](C)NC)=O)=O)=O.OC(C(F)(F)F)=O
• Target: Apoptosis,IAP
• Solubility: DMSO:50 mg/mL (44.27 mM)

Bioactivity

• Target IC50:
  CIAP2:21 nM|CIAP1:15 nM|XIAP:15 nM
• In Vivo:
  AZD5582 TFA (0.1-3.0 mg/kg; i.v.; once a week; 2 weeks; MDA-MB-231 xenograft-bearing mice) triggers cIAP1 degradation and caspase 3 cleavage within tumor cells. Following a two-week treatment, significant tumor resolution is observed. Upon administering a medium dose of 0.5 mg/kg AZD5582 TFA to mice, cIAP1 degradation occurs upon administration, although it takes some time for the apoptosis-inducing effects to manifest.
• In Vitro:
  AZD5582 TFA (20 nM; 48 h; H1975 NSCLC cell line) in collaboration with IFNγ or viral double-stranded RNA (dsRNA), suppresses cell viability and even induces cell death in H1975 NSCLC cells. AZD5582 TFA (20 nM; 17 or 25 h) induces cIAP-1 downregulation, promotes RIPK1 activation (an upstream regulator of caspase-8), and initiates the activation of both extrinsic (caspase-8) and intrinsic (caspase-9) apoptotic pathways, resulting in the cleavage of caspase-3 and caspase-7. AZD5582 TFA (20 nM; 48 h; H1975 NSCLC cell line) is involved in apoptosis due to induction of cell death and active caspase-3/8 activities by AZD5582 TFA and IFNγ co-treatment in HCC827 NSCLC cells.

Storage & Handling

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

Alternative Names

IAP, 1258392-53-8 free base, 1258392-53-8, AZD5582 TFA, AZD5582 TFA(1258392-53-8 free base), apoptosis

Compound Identifiers

PubChem CID

171360478