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安全信息

F3055

Sigma-Aldrich

夫拉平度 盐酸盐

≥98% (HPLC), powder

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别名:
(−)-2-（2-氯苯基）-5,7-二羟基-8-[(3 S ,4 R )-3-羟基-1-甲基-4-哌啶基]-4 H -1-苯并吡喃-4-酮 盐酸盐, L-86-8276, NSC-649890
经验公式（希尔记法）:
C21H20ClNO5 ·HCl · xH2O
CAS号:
131740-09-5
分子量:
438.30 (anhydrous basis)
MDL编号:
MFCD26792554
UNSPSC代码:
12352200
PubChem化学物质编号:
24724481
NACRES:
NA.77

质量水平

100

检测方案

≥98% (HPLC)

形式

powder

储存条件

desiccated

颜色

white to light brown

溶解性

H2O: ~2 mg/mL
DMSO: >5 mg/mL

储存温度

2-8°C

SMILES字符串

OC1=C(C(C=C(C2=C(Cl)C=CC=C2)O3)=O)C3=C([C@H]4CCN(C)C[C@H]4O)C(O)=C1.Cl

InChI

1S/C21H20ClNO5.ClH/c1-23-7-6-12(17(27)10-23)19-14(24)8-15(25)20-16(26)9-18(28-21(19)20)11-4-2-3-5-13(11)22;/h2-5,8-9,12,17,24-25,27H,6-7,10H2,1H3;1H/t12-,17+;/m0./s1

InChI key

LGMSNQNWOCSPIK-LWHGMNCYSA-N

基因信息

human ... CDK1(983) , CDK2(1017) , CDK4(1019) , CDK6(1021) , CDK7(1022) , CDK9(1025)

应用

夫拉平度盐酸盐已：
  • 用作周期蛋白依赖性激酶9 (CDK9)抑制剂，以研究其对猪胚胎成纤维细胞组蛋白H3赖氨酸36位点甲基化(H3K36)和转录失活的影响
  • 用作RNA聚合酶抑制剂，以研究其对肝细胞的影响
  • 用作RNA转录抑制剂，以研究其对斑马鱼胚胎常染色质粗化的影响

生化/生理作用

黄烷醇是一种从双花叶姜中提取的半合成黄酮类化合物，作为抗肿瘤剂可对抗几种癌症。它还显示出抗癌特性，因此，它已被研究用于治疗急性髓系白血病(AML)。
盐酸 Flavopiridol 是一种强效的 CDK（细胞周期蛋白依赖性激酶）和 CDC25 磷酸酶家族抑制剂。

特点和优势

《受体分类和信号转导》手册的 CDK 页面有该化合物的介绍。想要浏览手册的其他页面， 请单击此处。

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H302

危险分类

Acute Tox. 4 Oral

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves

法规信息

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Saowaluk Saisomboon et al.
Heliyon, 5(5), e01675-e01675 (2019-06-14)
Flavopiridol, a pan-cyclin-dependent kinase (CDK) inhibitor, was recently identified as an effective antitumor agent for several cancers. We investigated the antitumor effect of flavopiridol on cholangiocarcinoma (CCA), in vitro and in vivo. A methylthiotetrazole assay revealed that the proliferation of
Elisa Barbieri et al.
Cell reports, 33(6), 108373-108373 (2020-11-12)
Genome-wide profiling of nascent RNA has become a fundamental tool to study transcription regulation. Unlike steady-state RNA-sequencing (RNA-seq), nascent RNA profiling mirrors real-time activity of RNA polymerases and provides an accurate readout of transcriptome-wide variations. Some species of nuclear RNAs
Uma Raju et al.
Cancer research, 63(12), 3263-3267 (2003-06-18)
Flavopiridol, a cyclin-dependent kinase (cdk) inhibitor, can cause cell cycle arrest, induce apoptosis in cancer cells, and inhibit tumor cell growth in vivo. The present study investigated the in vitro radiosensitizing effect of flavopiridol and the underlying molecular mechanisms in
Stefano de Pretis et al.
Genome research, 27(10), 1658-1664 (2017-09-15)
Overexpression of the MYC transcription factor causes its widespread interaction with regulatory elements in the genome but leads to the up- and down-regulation of discrete sets of genes. The molecular determinants of these selective transcriptional responses remain elusive. Here, we
Anne Pumfery et al.
Current pharmaceutical design, 12(16), 1949-1961 (2006-06-22)
Cyclin-dependent kinases (CDKs) are key regulators of the cell cycle and RNA polymerase II transcription. Several pharmacological CDK inhibitors (PCIs) are currently in clinical trials as potential cancer therapeutics since CDK hyperactivation is detected in the majority of neoplasias. Within
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