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 可透过血脑屏障,抑制端粒酶 (telomerase) 活性。
生物活性 | Abacavir hydrochloride is a competitive, orally activenucleosidereverse transcriptaseinhibitor. Abacavir hydrochloride can inhibits the replication ofHIV. Abacavir hydrochloride shows anticancer activity in prostatecancercell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppressestelomeraseactivity[1][2][3]. |
体外研究 (In Vitro) | 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. |
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体内研究 (In Vivo) | 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/dDecitabine(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: | 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: | 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. |