Dapivirine

SKU: orb1225535

Description

Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates. Phase 3.(In Vitro):Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h).Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells.Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells.Dapivirine (TMC120-R147681) apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration.(In Vivo):Dapivirine (16 mg/kg, once every 3 days for 12 days) exhibits potent antitumor activity in human glioblastoma models in mice.Dapivirine has been shown to have a half-life in the range of 65 to 90 h.

Key Properties

• CAS Number: 244767-67-7
• MW: 329.4
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₉N₅
• SMILES: N#CC1=CC=C(NC2=NC=CC(NC3=C(C)C=C(C)C=C3C)=N2)C=C1
• Target: HIV
• Solubility: DMSO: 34 mg/mL (103.21 mM)

Bioactivity

• In Vivo:
  Dapivirine (16 mg/kg, once every 3 days for 12 days) exhibits potent antitumor activity in human glioblastoma models in mice. Dapivirine has been shown to have a half-life in the range of 65 to 90 h. Animal model: U87 cells were subcutaneously injected into the nude mice. Dosage: 16 mg/kg. Administration: Once every 3 days for 12 days. Result: Significantly decreased the tumor volumes. A significant decrease in Ki67 (a marker for proliferating cells that is overexpressed in many cancers) staining in sections of dapivirine-treated tumors compared to tumors from vehicle-treated mice.
• In Vitro:
  Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h). Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells. Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells. Dapivirine(TMC120-R147681) apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration. Cell Proliferation Assay Cell line: U87 glioblastoma cells. Concentration: 4, 8, 16 μM. Incubation time: 24, 48, 72, 96 and 120 hours. Result: Inhibited proliferation of glioma cells. IC50 was 10.73 μM. Apoptosis Analysis Cell line: U87 glioblastoma cells. Concentration: 16 μM. Incubation time: 12h, 24h and 48h. Result: Induced apoptosis.

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

TMC120

Quick Database Links

Gene Symbol

HIV