FK-3000

Names

[ Name ]:
FK-3000

Biological Activity

[Description]:

FK-3000 is a potent anti-tumor agent that inhibits the growth of carcinoma cells through apoptosis and induction cell cycle arrest. FK-3000 also exhibit antiviral effects against HSV-1 and HIV-1[1][2][3][4].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Anti-infection >> HSV

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

[In Vitro]

FK-3000 (0-5 μg/mL; 48 h) 抑制细胞增殖，抑制 MDA-MB-231，MCF-7，PC-3，A-431，HT-29 和 CT-26细胞的 IC50 值分别为 0.52，0.77，0.22，2.70，0.40 和 1.90 μg/mL[1]。 FK-3000 (0.5-5.0 μg/mL; 24-48 h) 以剂量和时间依赖性方式诱导 MDA-MB-231 细胞凋亡[1]。 FK-3000 (0.5-5.0 μg/mL; 24-48 h) 以剂量和时间依赖性方式诱导 MDA-MB-231 和 MCF-7 细胞的 G2/M 期阻滞[2]。 FK-3000 (0.5-5.0 μg/mL; 60-120 min or 24-48 h) 降低 MDA-MB-231 细胞中的 NF-κB 磷酸化水平和 COX-2 表达[1]。 FK-3000 (5.0 μg/mL; 120 min) 有效阻断 MDA-MB-231 细胞中 NF-κB 从细胞质向细胞核的易位[1]。

[In Vivo]

FK-3000 (1 mg/kg/day; i.p. daily for 24 d) 抑制MDA-MB-231 异种移植小鼠模型中肿瘤生长，并且没有显示出毒性迹象[1]。 FK-3000 (10-25 mg/kg; p.o. for 10 d) 显着延迟皮肤损伤，限制进一步损伤的发展并延长 HSV-1 感染小鼠的平均存活时间[3]。

[References]

[1]. Xu HD, et, al. FK-3000 isolated from Stephania delavayi Diels. inhibits MDA-MB-231 cell proliferation by decreasing NF-κB phosphorylation and COX-2 expression. Int J Oncol. 2015;46(6):2309-16.

[2]. Li YC, et, al. 6,7-di-O-acetylsinococuline (FK-3000) induces G2/M phase arrest in breast carcinomas through p38 MAPK phosphorylation and CDC25B dephosphorylation. Int J Oncol. 2015 Feb;46(2):578-86.

[3]. Nawawi A, et, al. In vivo antiviral activity of Stephania cepharantha against herpes simplex virus type-1. Phytother Res. 2001 Sep;15(6):497-500.

[4]. Lee JH, et, al. Development of a LC-MS method for quantification of FK-3000 and its application to in vivo pharmacokinetic study in drug development. J Pharm Biomed Anal. 2012 Nov;70:587-91.

Chemical & Physical Properties

[ Density]:
1.33±0.1 g/cm3(Predicted)

[ Boiling Point ]:
572.0±50.0 °C(Predicted)

[ Molecular Formula ]:
C₂₂H₂₇NO₇

[ Molecular Weight ]:
417.45

Related Compounds

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