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Purity: ≥98%
Dapivirine (also known as TMC120) is a potent non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, it inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates. Dapivirine prevents HIV-induced syncytium formation in the nanomolar range and shows a low cytostatic activity. Dapivirine apparently blocks HIV-1 infection in the primary cultures at a 10 nM concentration, but secondary cultures reveals that a 100 nM concentration is needed to completely prevent proviral integration.
| ln Vitro |
Dapivirine (16 μM, 12-48 h) causes apoptosis and suppresses the growth of glioma cells at concentrations of 4-64 μM, 24, 48, 72, 96, and 120 hours[1]. Glioma cell invasion is enhanced by dapivirine (8 and 16 μM, 12 h)[1]. In U87 cells, dapivirine (16 μM, 12 h, 24 h, and 48 h) stimulates autophagy[1]. In primary cultures, dapivirine (TMC120-R147681) appeared to stop infection at a concentration of 10 nM; however, secondary cultures showed that a 100 nM dosage was required to fully prevent proviral integration[3].
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| ln Vivo |
In mice with human glioblastoma models, dapivirine (16 mg/kg, once every three days for 12 days) has strong anticancer activity[1]. It has been demonstrated that the half-life of dipivirine is between 65 and 90 hours[4].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: U87 glioblastoma cells. Tested Concentrations: 4, 8, 16 μM. Incubation Duration: 24, 48, 72, 96 and 120 hrs (hours). Experimental Results: Inhibited proliferation of glioma cells. IC50 was 10.73 μM. Apoptosis Analysis[1] Cell Types: U87 glioblastoma cells. Tested Concentrations: 16 μM. Incubation Duration: 12h, 24h and 48h. Experimental Results: Induced apoptosis. diminished caspase-3. |
| Animal Protocol |
Animal/Disease Models: U87 cells were subcutaneously (sc) injected into the nude mice[1].
Doses: 16 mg/kg. Route of Administration: Once every 3 days for 12 days. Experimental Results: Dramatically diminished 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. |
| References |
[1]. Weiwen Liu, et al. Antitumor Activity and Mechanism of a Reverse Transcriptase Inhibitor, Dapivirine, in Glioblastoma. J Cancer. 2018 Jan 1;9(1):117-128.
[2]. Bríd Devlin, et al. Development of dapivirine vaginal ring for HIV prevention. Antiviral Res. 2013 Dec;100 Suppl:S3-8. [3]. Yven Van Herrewege, et al. In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides. Antimicrob Agents Chemother. 2004 Jan;48(1):337-9. [4]. Michael E Halwes, et al. Pharmacokinetic modeling of a gel-delivered dapivirine microbicide in humans. Eur J Pharm Sci. 2016 Oct 10;93:410-8. |
| Molecular Formula |
C20H19N5
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| Molecular Weight |
329.4
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| CAS # |
244767-67-7
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| Related CAS # |
Dapivirine-d11;1329613-10-6
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| SMILES |
N([H])(C1C([H])=C([H])N=C(N([H])C2C([H])=C([H])C(C#N)=C([H])C=2[H])N=1)C1C(C([H])([H])[H])=C([H])C(C([H])([H])[H])=C([H])C=1C([H])([H])[H]
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| InChi Key |
ILAYIAGXTHKHNT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19N5/c1-13-10-14(2)19(15(3)11-13)24-18-8-9-22-20(25-18)23-17-6-4-16(12-21)5-7-17/h4-11H,1-3H3,(H2,22,23,24,25)
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| Chemical Name |
4-[[4-[(2,4,6-Trimethylphenyl)amino]-2-pyrimidinyl]amino]benzonitrile
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.31 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0358 mL | 15.1791 mL | 30.3582 mL | |
| 5 mM | 0.6072 mL | 3.0358 mL | 6.0716 mL | |
| 10 mM | 0.3036 mL | 1.5179 mL | 3.0358 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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