切换导航
关闭
  • 菜单
  • Setting

Flavopiridol hydrochloride

盐酸夫拉平度
Catalog No.
A8640
CDK抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 454.00
现货
10mg
¥ 454.00
现货
25mg
¥ 909.00
现货
100mg
¥ 3,327.00
现货
1g
¥ 20,900.00
Ship with 10-15 days

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

A

背景

Flavopiridol hydrochloride是一种选择性的CDK1、CDK2、CDK4和CDK6抑制剂,IC50值均为约41 nM,对CDK7的IC50值为300nM[1][2][3]。据报道,flavopiridol hydrochloride也抑制表皮生长因子受体和蛋白激酶A,IC50值分别为21和122 μM[3]。

CDKs蛋白激酶家族参与调节转录、mRNA加工、细胞分化和细胞周期过程。据报道,CDKs在多种细胞中异常表达[3]。

Flavopiridol hydrochloride是一种有效的CDK抑制剂,不同于UCN-01。在乳腺癌细胞系MCF-7中,flavopiridol hydrochloride具有高抑制能力,通过抑制CDK2和CDK4,诱导G1期细胞周期阻滞[1]。在7个淋巴瘤细胞系中,flavopiridol hydrochloride以400 nM的浓度处理后通过抑制CDK4、CDK6、CDK7或CDK9,从而抑制Rb的磷酸化和抗凋亡蛋白(Mcl-1和XIAP),进而诱导细胞凋亡[4]。

在HL-60皮下异种移植小鼠模型中,flavopiridol hydrochloride(7.5 mg/kg)静脉给药后诱导91.67%的晚期动物肿瘤完全消退,并在flavopiridol治疗一个疗程后,保持几个月的无病状态[5]。

参考文献:
[1].  Carlson, B.A., et al., Flavopiridol induces G1 arrest with inhibition of cyclin-dependent kinase (CDK) 2 and CDK4 in human breast carcinoma cells. Cancer Res, 1996. 56(13): p. 2973-8.
[2].  Losiewicz, M.D., et al., Potent inhibition of CDC2 kinase activity by the flavonoid L86-8275. Biochem Biophys Res Commun, 1994. 201(2): p. 589-95.
[3].  Senderowicz, A.M., The cell cycle as a target for cancer therapy: basic and clinical findings with the small molecule inhibitors flavopiridol and UCN-01. Oncologist, 2002. 7 Suppl 3: p. 12-9.
[4].  Ema, Y., et al., Investigation of the cytotoxic effect of flavopiridol in canine lymphoma cell lines. Vet Comp Oncol, 2015.
[5].  Arguello, F., et al., Flavopiridol induces apoptosis of normal lymphoid cells, causes immunosuppression, and has potent antitumor activity In vivo against human leukemia and lymphoma xenografts. Blood, 1998. 91(7): p. 2482-90.

化学属性

StorageStore at -20°C
M.Wt438.3
Cas No.131740-09-5
FormulaC21H21Cl2NO5
Solubility≥21.9 mg/mL in DMSO; ≥53.5 mg/mL in H2O; ≥8.54 mg/mL in EtOH with ultrasonic
Chemical Name2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one;hydrochloride
SDFDownload SDF
Canonical SMILESCN1CCC(C(C1)O)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O.Cl
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

质量控制

化学结构

Flavopiridol hydrochloride