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].
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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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Clinical Trial |
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分子量 |
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Formula |
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CAS 号 |
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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