Abacavir monosulfate(Synonyms: 阿巴卡韦单硫酸盐)

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Abacavir monosulfate (Synonyms: 阿巴卡韦单硫酸盐)

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(Synonyms: 阿巴卡韦单硫酸盐)

Abacavir monosulfate Chemical Structure

CAS No. : 216699-07-9

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Abacavir monosulfate 的其他形式现货产品:

Abacavir Abacavir sulfate

生物活性

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].

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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: NSGTM 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.

分子量

384.41

Formula

C14H20N6O5S

CAS 号

216699-07-9

中文名称

阿巴卡韦单硫酸盐

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.

参考文献
  • [1]. Carlini F, et al. The reverse transcription inhibitor abacavir shows anticancer activity in prostate cancer cell lines. PLoS One. 2010 Dec 3;5(12):e14221.

    [2]. Collado-Diaz V, et al. Abacavir Induces Arterial Thrombosis in a Murine Model. J Infect Dis. 2018 Jun 20;218(2):228-233.

    [3]. Gringmuth M, et al. Enhanced Survival of High-Risk Medulloblastoma-Bearing Mice after Multimodal Treatment with Radiotherapy, Decitabine, and Abacavir. Int J Mol Sci. 2022 Mar 30;23(7):3815.

    [4]. McComsey GA, et al. Improvements in lipoatrophy, mitochondrial DNA levels and fat apoptosis after replacing stavudine with abacavir or zidovudine. AIDS. 2005 Jan 3;19(1):15-23.

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