Flavopiridol hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Storage | Store at -20°C |
M.Wt | 438.3 |
Cas No. | 131740-09-5 |
Formula | C21H21Cl2NO5 |
Solubility | ≥21.9 mg/mL in DMSO; ≥53.5 mg/mL in H2O; ≥8.54 mg/mL in EtOH with ultrasonic |
Chemical Name | 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one;hydrochloride |
SDF | Download SDF |
Canonical SMILES | CN1CCC(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。 |
质量控制和MSDS
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