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Merck
CN

F3055

夫拉平度 盐酸盐

≥98% (HPLC), CDK and CDC25 phosphatase family inhibitor, powder

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

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关于此项目

经验公式（希尔记法）:
C21H20ClNO5 ·HCl · xH2O
化学文摘社编号:
131740-09-5
分子量:
438.30 (anhydrous basis)
UNSPSC Code:
12352200
PubChem Substance ID:
24724481
NACRES:
NA.77
MDL number:
MFCD26792554

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产品名称

夫拉平度 盐酸盐, ≥98% (HPLC), powder

SMILES string

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 key

LGMSNQNWOCSPIK-LWHGMNCYSA-N

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

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to light brown

solubility

H2O: ~2 mg/mL
DMSO: >5 mg/mL

storage temp.

2-8°C

Quality Level

100

Gene Information

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

相关类别

Application

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

Biochem/physiol Actions

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。
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)。

Features and Benefits

《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。

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

法规信息

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分析证书(COA)

Lot/Batch Number
0000277078
0000277078
0000213400
0000213400
0000173217

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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
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
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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