APG-1387

SKU: orb1220178

Description

APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). APG-1387 induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. APG-1387 can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.

Key Properties

• CAS Number: 1570231-89-8
• MW: 1157.4
• Purity: >98% (HPLC)
• Formula: C??H??N??O??S?
• SMILES: O=S(C1=CC=CC(S(=O)(N(C[C@@H]2NC([C@@H](NC)C)=O)CC[C@](CC[C@H]3C(NC(C4=CC=CC=C4)C5=CC=CC=C5)=O)([H])N3C2=O)=O)=C1)(N(C[C@@H]6NC([C@@H](NC)C)=O)CC[C@](CC[C@H]7C(NC(C8=CC=CC=C8)C9=CC=CC=C9)=O)([H])N7C6=O)=O
• Target: IAP
• Solubility: DMSO : 50 mg/mL (43.20 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) sensitizes HCCLM3 tumors toward NK cell-mediated killing in mice. Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) monotherapy exhibits some degree of anti-tumor effect and is well tolerated in mice. Animal model: Non-obese diabetic and severe combined immunodeficiency (NOD-SCID) mice bearing HCCLM3 tumors are injected with NK cells. Dosage: 20 mg/kg. Administration: i.p. every 3 days for 4 weeks. Result: Decreased the expression of cIAP1 and cIAP2, and less potent to XIAP expression. Potentiated the effects of pre-activated NK cells on HCCLM3 xenograft tumor growth and tumor weight.
  Read more...
• In Vitro:
  Dasminapant (0.02-20 μM; 24 h) induces rapid degradation of cIAPs in HepG2 and HCCLM3 cells. Dasminapant (2 μM; 24 h) enhances TNF-α- and TRAIL-mediated anti-cancer activities in HepG2 and HCCLM3 cells. Dasminapant sensitizes HepG2 and HCCLM3 cells to NK cell-mediated killing in vitro. Western blot analysis. Cell line: HepG2 and HCCLM3 cells. Concentration: 0.02, 0.2, 2, 20 μM Incubation time: 1, 6, 24 hours. Result: Decreased the expression of cIAP1 and cIAP2 in both cell lines in a dose- and time-dependent manner. Inhibited the expression of X chromosome-linked IAP (XIAP) at a high dose.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

IAP