Abacavir hydrochloride 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 hydrochloride 可抑制HIV的复制。Abacavir hydrochloride 在前列腺癌细胞系中显示出抗癌活性。Abacavir hydrochloride 可穿越血脑屏障，抑制端粒酶 (telomerase) 活性。

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

Abacavir hydrochloride (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 hydrochloride (15 and 150 μM, 18 h) significantly reduces cell migration and inhibits cell invasion [1]. Abacavir hydrochloride induces fat apoptosis [4]. Cell Proliferation Assay [1] Cell Line: PC3, LNCaP and WI-38 Concentration: 15 μM and 150 μM Incubation Time: 0, 24, 48, 72 and 96 hours Result: Showed a dose-dependent growth inhibition on PC3 and LNCaP. Cell Cycle Analysis [1] Cell Line: PC3, LNCaP and WI-38 Concentration: 150 μM Incubation Time: 0, 18, 24, 48, 72, 96 and 120 hours 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, LNCaP and WI-38 Concentration: 15 and 150 μM Incubation Time: 18 hours Result: Significantly reduced cell migration. Cell Invasion Assay [1] Cell Line: PC3, LNCaP and WI-38 Concentration: 15 and 150 μM Incubation Time: 18 hours Result: Significantly inhibited cell invision.

Abacavir hydrochloride (100 and 200 mg/kg, p.o.; 4 h) dose-dependently promotes thrombus formation [2]. Abacavir hydrochloride (50 mg/kg/d; i.p.; 14 d) 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: Route 1: 2.5, 5, and 7.5 μg/mL, 100 μL Route 2: 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.

136777-48-5

C28H38N12O6S

670.75

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