Abacavir 是一种具有口服活性、竞争性核苷酸逆转录酶 (nucleoside reverse transcriptase) 抑制剂。 Abacavir 可抑制HIV的复制。Abacavir 在前列腺癌细胞系中显示出抗癌活性。Abacavir 可突破血脑屏障，抑制端粒酶 (telomerase) 活性。
| 生物活性 | Abacavir is an orally active and competitivenucleosidereverse transcriptaseinhibitor. Abacavir can inhibits the replication ofHIV. Abacavir shows anticancer activity in prostatecancercell lines. Abacavir can trespass the blood-brain-barrier and suppressestelomeraseactivity[1][2][3]. |
体外研究
(In Vitro) | Abacavir (15 and 150 μM, 0-120 h) inhibits cell growth, affects cell cycle progression, induces senescence and modulates LINE-1 mRNA expression in prostate cancer cell lines[1].
Abacavir (15 and 150 μM, 18 h) significantly reduces cell migration and inhibits cell invasion[1].
Abacavir induces fat apoptosis[4].
Cell Proliferation Assay[1] | Cell Line: | PC3, LNCaP and WI-38 | | Concentration: | 15 and 150 μM | | Incubation Time: | 0, 24, 48, 72 and 96 h | | Result: | Showed a dose-dependent growth inhibition on PC3 and LNCaP. |
Cell Cycle Analysis[1] | Cell Line: | PC3 and LNCaP | | Concentration: | 150 μM | | Incubation Time: | 0, 18, 24, 48, 72, 96 and 120 h | | Result: | 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 Line: | PC3 and LNCaP | | Concentration: | 15 and 150 μM | | Incubation Time: | 18 h | | Result: | Significantly reduced cell migration. |
Cell Invasion Assay[1] | Cell Line: | PC3 and LNCaP | | Concentration: | 15 and 150 μM | | Incubation Time: | 18 h | | Result: | Significantly inhibited cell invision. |
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体内研究
(In Vivo) | Abacavir (100 and 200 mg/kg, p.o.; 4 h) dose-dependently promoted thrombus formation[2].
Abacavir (50 mg/kg/d; i.p.; 14 d) with 0.1 mg/kg/d Decitabine (HY-A0004) enhances survival of high-risk medulloblastoma-bearing mice[3].
| Animal Model: | Male mice (9-weeks old, 22-30 g) - wild-type (WT) C57BL/6 or homozygous knockout (P2rx7 KO, B6.129P2-P2rx7tm1Gab/J)[2] | | Dosage: | 2.5, 5 and 7.5 μg/mL, 100 μL or 100 and 200 mg/kg | | Administration: | Intrascrotal or oral administration for 4 h | | Result: | Dose-dependently promoted thrombus formation. |
| Animal Model: | NSGTMmice, patient-derived xenograft (PDX) cells of non-WNT/non-SHH, Group 3 and of SHH/ TP53-mutated medulloblastoma[3] | | Dosage: | 50 mg/kg/d with 0.1 mg/kg/d Decitabine | | Administration: | Intraperitoneal injection, daily for 14 days | | Result: | Inhibited tumor growth and enhanced mouse survival. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(349.25 mM;Need ultrasonic) H2O : 2 mg/mL(6.98 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.4925 mL | 17.4624 mL | 34.9247 mL | | 5 mM | 0.6985 mL | 3.4925 mL | 6.9849 mL | | 10 mM | 0.3492 mL | 1.7462 mL | 3.4925 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 3.33 mg/mL (11.63 mM); Clear solution; Need ultrasonic and warming 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (8.73 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.73 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.73 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.73 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.73 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.73 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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