Abacavir monosulfate 是一种竞争性的口服活性核苷逆转录酶（nucleoside reverse transcriptase）抑制剂。 Abacavir monosulfate 可抑制HIV的复制。Abacavir monosulfate 在前列腺癌细胞系中显示出抗癌活性。Abacavir monosulfate 可突破血脑屏障，抑制端粒酶（telomerase）活性。
| 生物活性 | Abacavir monosulfate is a competitive, orally activenucleosidereverse transcriptaseinhibitor. Abacavir monosulfate can inhibits the replication ofHIV. Abacavir monosulfate shows anticancer activity in prostatecancercell lines. Abacavir monosulfate 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) monosulfate 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) monosulfate significantly reduces cell migration and inhibits cell invasion[1].
Abacavir monsulfate 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) monosulfate dose-dependently promoted thrombus formation[2].
Abacavir (50 mg/kg/d; i.p.; 14 days) monosulfate 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 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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