Dapivirine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Dapivirine (TMC120) 是一种 HIV 逆转录酶非核苷抑制剂，IC50 为 24 nM。

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.

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 AssayCell 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.

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.

TMC120

Microbiology/Virology

HIV

HIV reverse transcriptase

Infection

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244767-67-7

329.4

C20H19N5

>98% (HPLC)

DMSO: 34 mg/mL (103.21 mM)

N#CC1=CC=C(NC2=NC=CC(NC3=C(C)C=C(C)C=C3C)=N2)C=C1

4-[[4-[(2,4,6-Trimethylphenyl)amino]-2-pyrimidinyl]amino]benzonitrile

(-20℃)

With Ice Pack

≥ 2 years