AZD5582 acetate (1258392-53-8 free base)

SKU: orb1308611

Description

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

Research Area

Cell Biology

Key Properties

• MW: 1075.36
• Purity: 97.76% (May vary between batches)
• Formula: C₆₀H₈₂N₈O₁₀
• SMILES: C[C@H](NC)C(N[C@H](C(N1CCC[C@H]1C(N[C@@H]2[C@H](OCC#CC#CCO[C@@H]3CC4=CC=CC=C4[C@@H]3NC([C@@H]5CCCN5C([C@@H](NC([C@@H](NC)C)=O)C6CCCCC6)=O)=O)CC7=CC=CC=C27)=O)=O)C8CCCCC8)=O.CC(O)=O
• Target: IAP
• Solubility: DMSO:55 mg/mL (51.15 mM)

Bioactivity

• Target IC50:
  XIAP:15 nM|CIAP1:15 nM|CIAP2:21 nM
• In Vivo:
  AZD5582 (intravenous injection; 0.1-3.0 mg/kg; once a week; 2 weeks) causes degradation of cIAP1 and caspase 3 cleavage in tumor cells, and after a two-week treatment, the tumors largely resolved. When the mice are given a medium dose (0.5 mg/kg) of AZD5582, cIAP1 degrades after administration, but it takes a while time to reach apoptosis-inducing effect.
• In Vitro:
  AZD5582 (20 nM; 48 hours) inhibited cell viability by cooperation with IFNγ or viral double-stranded RNA (dsRNA) in H1975 NSCLC cells. AZD5582 (20 nM; 48 hours) involves in apoptosis due to induction of cell death and active caspase-3/ -8 activities by AZD5582 and IFNγ co-treatment in HCC827 NSCLC cells. AZD5582 (20 nM; 17 or 25 hours) down-regulates cIAP-1, activates RIPK1( upstream regulator of caspase-8), and triggers the activation of extrinsic (caspase-8) and intrinsic (caspase-9) apoptosis pathways, causing the cleavage of caspase-3 and caspase-7.

Storage & Handling

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

Alternative Names

cIAP2-BIR3, cIAP2, cIAP1, 1258392-53-8, 1258392-53-8 free base, AZD 5582 Acetate, AZD5582 Acetate, AZD-5582 Acetate, AZD5582 acetate (1258392 53 8 free base), AZD5582 acetate (1258392538 free base), AZD-5582 acetate (1258392-53-8 free base), XIAP

Compound Identifiers

PubChem CID

155977627