Birinapant

SKU: orb1301184

Description

Birinapant

Research Area

Cell Biology, Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 1260251-31-7
• MW: 806.94
• Purity: 99.78%
• Formula: C₄₂H₅₆F₂N₈O₆
• SMILES: CC[C@H](NC(=O)[C@H](C)NC)C(=O)N1C[C@@H](O)C[C@H]1Cc1c([nH]c2cc(F)ccc12)-c1[nH]c2cc(F)ccc2c1C[C@@H]1C[C@H](O)CN1C(=O)[C@H](CC)NC(=O)[C@H](C)NC
• Target: HIV Protease,Apoptosis,IAP
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:245 mg/mL (303.62 mM);Ethanol:51 mg/mL (63.2 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (4.09 mM)

Bioactivity

• Target IC50:
  XIAP:45 nM(Kd)|CIAP1:<1 nM(Kd)
• In Vivo:
  Birinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with.
• In Vitro:
  Birinapant binds with XIAP and cIAP1 with Kd of 45 and <1 nM, respectively. Birinapant induces cell death as a single agent in TRAIL-insensitive SUM190 (ErbB2-overexpressing) cells (IC50, ~300 nM), and significantly increases potency of TRAIL-induced apoptosis in TRAIL-sensitive SUM149 (triple-negative, EGFR-activated) cells. Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation. Birinapant in combination with TNF-α exhibits a strong antimelanoma effect in vitro. Birinapant in combination with TNF-α(1 ng/mL) inhibits the growth of human melanoma cell lines WTH202, WM793B, WM1366 and WM164 with IC50s of 1.8, 2.5, 7.9 and 9 nM, respectively, while neither compound is effective individually. Birinapant singly treatment induces inhibition on proliferation of WM9 cells with IC50 of 2.4 nM. Birinapant significantly inhibits the target protein cIAP1 and cIAP2 in these cell lines.
• Cell Research:
  Cells are allowed to attach for 24 hours and subsequently incubated with Birinapant and/or TNF-α for 24 or 72 hours. Then MTS assay is conducted(Only for Reference)

Storage & Handling

• Storage: store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, HIV, HIV Protease, HIVProtease, Inhibitor, Human immunodeficiency virus, IAP, Birinapant, Apoptosis, cIAP1, TL 32711, TL32711, TL-32711, XIAP

Compound Identifiers

PubChem CID

49836020