Birinapant

SKU: orb1226656

Description

Birinapant is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM, less potent to XIAP. Phase 2.(In Vitro):Birinapant (TL32711) (30-10000 nM; 24 hours) significantly decreases the viability of SUM190 cells in a dose-dependent manner.Birinapant (TL32711) (30-1000 nM; 4 hours) shows a significant decrease in cIAP1 levels and enhanced PARP cleavage, and induces apoptosis.Birinapant (TL32711) binds with high affinity to the isolated BIR3 domains of cIAP1, cIAP2, and XIAP and the single BIR domain of ML-IAP and rapidly degrades TRAF2-bound cIAP1 and cIAP2 thereby inhibiting TNF-mediated NF-κB activation.(In Vivo):Birinapant (TL32711) (30 mg/kg; i.p.; every third day (*5)) shows antitumor efficacy and are devoid of overt toxicity in preclinical models.

Key Properties

• CAS Number: 1260251-31-7
• MW: 806.94
• Purity: >98% (HPLC)
• Formula: C₄₂H₅₆F₂N₈O₆
• SMILES: C[C@H](NC)C(N[C@@H](CC)C(N1[C@H](CC2=C(C(N3)=C(C[C@H]4N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C4)C5=C3C=C(F)C=C5)NC6=C2C=CC(F)=C6)C[C@H](O)C1)=O)=O
• Target: IAP
• Solubility: DMSO:100 mg/mL (123.92 mM); Ethanol:55 mg/mL (68.15 mM); Water：<1 mg/mL (<1 mM)

Bioactivity

• In Vivo:
  Animal model: Female athymic nude mice (low-passage, patient-derived xenotransplant models of ovarian cancer, colorectal cancer, and melanoma). Dosage: 30 mg/kg. Administration: Intraperitoneal injection; every third day (*5). Result: Resulted in inhibition of tumor growth.
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• In Vitro:
  Cell Viability Assay Cell line: TRAIL-resistant SUM190 IBC cells. Concentration: 30, 100, 300, 1000, 10000 nM. Incubation time: 24 hours. Result: Significantly decreased the viability of SUM190 cells in a dose-dependent manner. Western blot analysis. Cell line: SUM190 cells. Concentration: 30, 300, 1000 nM. Incubation time: 4 hours. Result: Showed a significant decrease in cIAP1 levels and enhanced PARP cleavage.
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Storage & Handling

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

Alternative Names

TL-32711

Quick Database Links

Gene Symbol

IAP