| CAS NO: | 131740-09-5 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 100mg | 电议 |
| 1g | 电议 |
| 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 |
| 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 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。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。 |
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.
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