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。

Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity [1] [2] [3].

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.

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 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-P2rx7 tm1Gab /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: NSG TM mice, 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.

216699-07-9

C14H20N6O5S

384.41

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years