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| 250mg |
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Purity: ≥98%
Abacavir (formerly also known as ABC, or 1592U89; trade names: Ziagen; Epzicom) is a commonly used nucleoside analogue of the NRTI class with potent antiviral activity against HIV-1. Abacavir is a widely used antiretroviral medication used to prevent and treat HIV/AIDS. It is of the nucleoside analog reverse transcriptase inhibitor (NRTI) type. Viral strains that are resistant to zidovudine (AZT) or lamivudine (3TC) are generally, but not always, sensitive to abacavir. It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.
| ln Vitro |
In prostate cancer cell lines, abacavir (15 and 150 μM, 0-120 h) sulfate reduces cell proliferation, modifies LINE-1 mRNA expression, changes cell cycle progression, and promotes senescence[1]. Cell migration is greatly reduced and cell invasion is inhibited by abacavir (15 and 150 μM, 18 h) sulfate[1]. Fat apoptosis is induced by abacavir sulfate[4].
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| ln Vivo |
The thrombus development was dose-dependently increased by abacavir (0-7.5 μg/mL, 100 μL, intrascrotal injection; 100 and 200 mg/kg, po; 4 h) sulfate[2]. In high-risk mice carrying medulloblastoma, abacavir (50 mg/kg/d; ip; 14 days) sulfate combined with 0.1 mg/kg/d Decitabine improves survival[3].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: PC3, LNCaP and WI-38 Tested Concentrations: 15 and 150 μM Incubation Duration: 0, 24, 48, 72 and 96 h Experimental Results: demonstrated a dose-dependent growth inhibition on PC3 and LNCaP. Cell Cycle Analysis[1] Cell Types: PC3 and LNCaP Tested Concentrations: 150 μM Incubation Duration: 0, 18, 24, 48, 72, 96 and 120 h Experimental Results: Caused a very high accumulation of cells in S phase in PC3 and LNCaP cells, and G2/M phase increment was observed in PC3 cells. Cell Migration Assay [1] Cell Types: PC3 and LNCaP Tested Concentrations: 15 and 150 μM Incubation Duration: 18 h Experimental Results: Dramatically decreased cell migration. Cell Invasion Assay[1] Cell Types: PC3 and LNCaP Tested Concentrations: 15 and 150 μM Incubation Duration: 18 h Experimental Results: Dramatically inhibited cell invision. |
| Animal Protocol |
Animal/Disease Models: Male mice (9-weeks old, 22-30 g) - wild-type (WT) C57BL/ 6 or homozygous knockout (P2rx7 KO, B6.129P2-P2rx7tm1Gab/J)[2]
Doses: 2.5, 5 and 7.5 μg/mL, 100 μL or 100 and 200 mg/kg Route of Administration: Intrascrotal or oral administration for 4 h Experimental Results: Dose-dependently promoted thrombus formation. Animal/Disease Models: NSGTM mice, patient-derived xenograft (PDX) cells of non-WNT/non-SHH, Group 3 and of SHH/ TP53-mutated medulloblastoma[3] Doses: 50 mg/kg/ d with 0.1 mg/kg/d Decitabine Route of Administration: intraperitoneal (ip)injection, daily for 14 days Experimental Results: Inhibited tumor growth and enhanced mouse survival. |
| References |
[1]. Carlini F, et al. The reverse transcription inhibitor abacavir shows anticancer activity in prostate cancer cell lines. PLoS One. 2010 Dec 3;5(12):e14221.
[2]. Collado-Diaz V, et al. Abacavir Induces Arterial Thrombosis in a Murine Model. J Infect Dis. 2018 Jun 20;218(2):228-233. [3]. Gringmuth M, et al. Enhanced Survival of High-Risk Medulloblastoma-Bearing Mice after Multimodal Treatment with Radiotherapy, Decitabine, and Abacavir. Int J Mol Sci. 2022 Mar 30;23(7):3815. [4]. McComsey GA, et al. Improvements in lipoatrophy, mitochondrial DNA levels and fat apoptosis after replacing stavudine with abacavir or zidovudine. AIDS. 2005 Jan 3;19(1):15-23. |
| Molecular Formula |
C14H18N6O.1/2H2O4S
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| Molecular Weight |
335.35
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| CAS # |
188062-50-2
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| Related CAS # |
Abacavir;136470-78-5;Abacavir monosulfate;216699-07-9;Abacavir hydrochloride;136777-48-5
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| SMILES |
NC1=NC(NC2CC2)=C3N=CN([C@H]4C=C[C@@H](CO)C4)C3=N1.O=S(O)(O)=O.NC5=NC(NC6CC6)=C7N=CN([C@H]8C=C[C@@H](CO)C8)C7=N5
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| InChi Key |
MBFKCGGQTYQTLR-SCYNACPDSA-N
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| InChi Code |
InChI=1S/C14H18N6O.H2O4S/c15-14-18-12(17-9-2-3-9)11-13(19-14)20(7-16-11)10-4-1-8(5-10)6-21;1-5(2,3)4/h1,4,7-10,21H,2-3,5-6H2,(H3,15,17,18,19);(H2,1,2,3,4)/t8-,10+;/m1./s1
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| Chemical Name |
[(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methanol sulfuric acid
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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: ≥ 2.5 mg/mL (7.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 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: ≥ 2.5 mg/mL (7.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (29.82 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9820 mL | 14.9098 mL | 29.8196 mL | |
| 5 mM | 0.5964 mL | 2.9820 mL | 5.9639 mL | |
| 10 mM | 0.2982 mL | 1.4910 mL | 2.9820 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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