Abacavir sulfate (Abacavir Hemisulfate) 是一种竞争性的口服活性核苷逆转录酶(nucleoside reverse transcriptase)抑制剂。 Abacavir sulfate 可抑制HIV的复制。Abacavir sulfate 在前列腺癌细胞系中显示出抗癌活性。Abacavir sulfate 可突破血脑屏障,抑制端粒酶(telomerase)活性。
生物活性 | Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally activenucleosidereverse transcriptaseinhibitor. Abacavir sulfate can inhibits the replication ofHIV. Abacavir sulfate shows anticancer activity in prostatecancercell lines. Abacavir sulfate 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) sulfate 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) sulfate significantly reduces cell migration and inhibits cell invasion[1]. Abacavir sulfate 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 (0-7.5 μg/mL, 100 μL, intrascrotal administration; 100 and 200 mg/kg, p.o.; 4 h) sulfate dose-dependently promoted thrombus formation[2]. Abacavir (50 mg/kg/d; i.p.; 14 days) sulfate 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 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
溶解性数据 | In Vitro: DMSO : 50 mg/mL(149.08 mM;Need ultrasonic) H2O : 33.33 mg/mL(99.38 mM;Need ultrasonic) 配制储备液 1 mM | 2.9817 mL | 14.9085 mL | 29.8169 mL | 5 mM | 0.5963 mL | 2.9817 mL | 5.9634 mL | 10 mM | 0.2982 mL | 1.4908 mL | 2.9817 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 (stored under nitrogen)。-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: 10 mg/mL (29.82 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.45 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.45 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 (7.45 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.45 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 (7.45 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.45 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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