| Size | Price | |
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| 5mg | ||
| 10mg | ||
| 25mg | ||
| 50mg | ||
| 100mg | ||
| 250mg |
Abacavir monosulfate is an orally bioavailable NRTI/nucleoside reverse transcriptase inhibitor with antiviral activity. It can inhibit the replication of HIV. Abacavir monosulfate also exhibits anticancer activity and can trespass the blood-brain-barrier and suppresses telomerase activity.
| ln Vitro |
In prostate cancer cell lines, abacavir (15 and 150 μM, 0-120 h) monosulfate suppresses cell proliferation, modifies the expression of LINE-1 mRNA, influences the progression of the cell cycle, and promotes senescence[1]. Abacavir monosulfate (15 and 150 μM, 18 h) dramatically decreases cell migration and prevents cell invasion[1]. Fat apoptosis is induced by abacavir monsulfate[4].
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| ln Vivo |
Abacavir (0.7–7.5 μg/mL, 100 μL, intrascrotal injection; 100 and 200 mg/kg, po; 4 h) increased the formation of thrombus in a dose-dependent manner[2]. In high-risk mice carrying medulloblastoma, abacavir (50 mg/kg/d; ip; 14 days) monosulfate 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 |
C14H20N6O5S
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|---|---|
| Molecular Weight |
384.410800933838
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| CAS # |
216699-07-9
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| Related CAS # |
Abacavir;136470-78-5;Abacavir sulfate;188062-50-2;Abacavir hydrochloride;136777-48-5
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| SMILES |
S(O)(O)(=O)=O.N(C1CC1)C1N=C(N)N=C2N([C@H]3C=C[C@@H](CO)C3)C=NC=12
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6014 mL | 13.0069 mL | 26.0139 mL | |
| 5 mM | 0.5203 mL | 2.6014 mL | 5.2028 mL | |
| 10 mM | 0.2601 mL | 1.3007 mL | 2.6014 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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