1. Cell Cycle/DNA Damage Autophagy Anti-infection Apoptosis
  2. CDK Autophagy HIV Apoptosis
  3. Flavopiridol

Flavopiridol  (Synonyms: 夫拉平度; HMR-1275; Alvocidib; L86-8275)

目录号: HY-10005 纯度: 99.73%
COA 产品使用指南

Flavopiridol (Alvocidib) 是一种竞争型的 CDK 广谱抑制剂, 抑制 CDK1,CDK2,CDK4的IC50 分别为30,170,100 nM。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Flavopiridol Chemical Structure

Flavopiridol Chemical Structure

CAS No. : 146426-40-6

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Customer Review

Other Forms of Flavopiridol:

MCE 顾客使用本产品发表的 41 篇科研文献

RT-PCR
Proliferation Assay

    Flavopiridol purchased from MCE. Usage Cited in: Sci Rep. 2015 Dec 1;5:17675.  [Abstract]

    Flavopiridol (FP) significantly decreases renilla luciferase mRNA levels time-dependently. The bar graphs (upper panel) represent renilla luciferase mRNA levels in pRL-SV40-transfected A549 cells treated with FP normalized to that in FP free cells. The bottom panel indicates renilla luciferase mRNA levels determined by RT-PCR using 1 μg of total RNA as template.

    Flavopiridol purchased from MCE. Usage Cited in: Biomaterials. 2014 Aug;35(24):6585-94.  [Abstract]

    Flavopiridol at concentrations >0.1 μM significantly inhibits the proliferation of astrocytes, and at ≥1 μM even inhibits their survival.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.

    IC50 & Target[3]

    CDK1/Cyc B1

    30 nM (IC50)

    CDK2/Cyc E

    170 nM (IC50)

    CDK4/Cyc D1

    100 nM (IC50)

    MAP

    19000 nM (IC50)

    PKC

    14000 nM (IC50)

    EGFR

    22000 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A2780 GI50
    0.023 μM
    Compound: Flavopiridol
    Cytotoxicity against human A2780 cells after 24 hrs by MTT assay
    Cytotoxicity against human A2780 cells after 24 hrs by MTT assay
    [PMID: 23301767]
    A2780 GI50
    0.029 μM
    Compound: Flavopiridol
    Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
    Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
    [PMID: 23301767]
    A2780 GI50
    0.031 μM
    Compound: Flavopiridol
    Cytotoxicity against human A2780 cells after 48 hrs by MTT assay
    Cytotoxicity against human A2780 cells after 48 hrs by MTT assay
    [PMID: 23301767]
    A2780 GI50
    0.064 μM
    Compound: Flavopiridol
    Growth inhibition of human A2780 cells after 48 hrs by MTT assay
    Growth inhibition of human A2780 cells after 48 hrs by MTT assay
    [PMID: 33581551]
    A549 GI50
    0.14 μM
    Compound: FVP
    Antiproliferative activity against human A549 cells after 3 days by SRB method
    Antiproliferative activity against human A549 cells after 3 days by SRB method
    [PMID: 25914804]
    A549 GI50
    0.145 μM
    Compound: Flavopiridol
    Growth inhibition of human A549 cells after 48 hrs by MTT assay
    Growth inhibition of human A549 cells after 48 hrs by MTT assay
    [PMID: 33581551]
    BJ EC50
    > 86.2069 μM
    Compound: 4
    Antiproliferative activity against human BJ cells after 72 hrs by CelTiter-Glo assay
    Antiproliferative activity against human BJ cells after 72 hrs by CelTiter-Glo assay
    [PMID: 29407975]
    DU-145 GI50
    0.15 μM
    Compound: FVP
    Antiproliferative activity against human DU145 cells after 3 days by SRB method
    Antiproliferative activity against human DU145 cells after 3 days by SRB method
    [PMID: 25914804]
    HCT-116 EC50
    0.034 μM
    Compound: Flavopiridol
    Antiproliferative activity against human HCT116 cells after 72 hrs by Celltiter-Glo reagent based assay in presence of 10% fetal bovine serum
    Antiproliferative activity against human HCT116 cells after 72 hrs by Celltiter-Glo reagent based assay in presence of 10% fetal bovine serum
    [PMID: 26985305]
    HCT-116 GI50
    0.056 μM
    Compound: Flavopiridol
    Growth inhibition of human HCT-116 cells after 48 hrs by MTT assay
    Growth inhibition of human HCT-116 cells after 48 hrs by MTT assay
    [PMID: 33581551]
    HCT-116 EC50
    0.059 μM
    Compound: Flavopiridol
    Antiproliferative activity against human HCT116 cells after 72 hrs by Celltiter-Glo reagent based assay in presence of 0.625% fetal bovine serum
    Antiproliferative activity against human HCT116 cells after 72 hrs by Celltiter-Glo reagent based assay in presence of 0.625% fetal bovine serum
    [PMID: 26985305]
    HCT-116 EC50
    0.059 μM
    Compound: Flavopiridol
    Antiproliferative activity against human HCT116 cells assessed as growth inhibition in presence of 0.625% FBS after 72 hrs
    Antiproliferative activity against human HCT116 cells assessed as growth inhibition in presence of 0.625% FBS after 72 hrs
    [PMID: 27326333]
    HCT-116 IC50
    20 nM
    Compound: Alvocidib
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    [PMID: 32402934]
    HeLa GI50
    0.043 μM
    Compound: Flavopiridol
    Growth inhibition of human HeLa cells after 48 hrs by MTT assay
    Growth inhibition of human HeLa cells after 48 hrs by MTT assay
    [PMID: 33581551]
    HeLa CC50
    0.12 μM
    Compound: 8; Alvocidib
    Cytotoxicity against human HeLa cells assessed as decrease in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as decrease in cell viability after 72 hrs by MTT assay
    [PMID: 27171036]
    HepG2 EC50
    0.1464 μM
    Compound: 4
    Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay
    Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay
    [PMID: 29407975]
    HMEC-1 GI50
    0.061 μM
    Compound: Flavopiridol
    Cytotoxicity against human HMEC1 cells after 24 hrs by MTT assay
    Cytotoxicity against human HMEC1 cells after 24 hrs by MTT assay
    [PMID: 23301767]
    HMEC-1 GI50
    0.062 μM
    Compound: Flavopiridol
    Cytotoxicity against human HMEC1 cells after 48 hrs by MTT assay
    Cytotoxicity against human HMEC1 cells after 48 hrs by MTT assay
    [PMID: 23301767]
    HMEC-1 GI50
    0.066 μM
    Compound: Flavopiridol
    Cytotoxicity against human HMEC1 cells after 72 hrs by MTT assay
    Cytotoxicity against human HMEC1 cells after 72 hrs by MTT assay
    [PMID: 23301767]
    HT-29 GI50
    0.131 μM
    Compound: Flavopiridol
    Growth inhibition of human HT-29 cells after 48 hrs by MTT assay
    Growth inhibition of human HT-29 cells after 48 hrs by MTT assay
    [PMID: 33581551]
    K562 IC50
    125 nM
    Compound: Alvocidib
    Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    [PMID: 32402934]
    KB GI50
    0.16 μM
    Compound: FVP
    Antiproliferative activity against human KB cells after 3 days by SRB method
    Antiproliferative activity against human KB cells after 3 days by SRB method
    [PMID: 25914804]
    KOPN-8 EC50
    0.1926 μM
    Compound: 4
    Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay
    Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay
    [PMID: 29407975]
    MCF7 GI50
    0.092 μM
    Compound: Flavopiridol
    Growth inhibition of human MCF7 cells after 48 hrs by MTT assay
    Growth inhibition of human MCF7 cells after 48 hrs by MTT assay
    [PMID: 33581551]
    MDA-MB-468 GI50
    0.096 μM
    Compound: Flavopiridol
    Growth inhibition of human MDA-MB-468 cells after 48 hrs by MTT assay
    Growth inhibition of human MDA-MB-468 cells after 48 hrs by MTT assay
    [PMID: 33581551]
    MIA PaCa-2 GI50
    0.078 μM
    Compound: Flavopiridol
    Growth inhibition of human MIA PaCa-2 cells after 48 hrs by MTT assay
    Growth inhibition of human MIA PaCa-2 cells after 48 hrs by MTT assay
    [PMID: 33581551]
    MIA PaCa-2 IC50
    320 nM
    Compound: Alvocidib
    Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    [PMID: 32402934]
    MRC5 GI50
    0.028 μM
    Compound: Flavopiridol
    Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay
    Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay
    [PMID: 23301767]
    MRC5 GI50
    0.039 μM
    Compound: Flavopiridol
    Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
    Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
    [PMID: 23301767]
    MRC5 GI50
    0.049 μM
    Compound: Flavopiridol
    Cytotoxicity against human MRC5 cells after 24 hrs by MTT assay
    Cytotoxicity against human MRC5 cells after 24 hrs by MTT assay
    [PMID: 23301767]
    MT4 EC50
    0.015 μM
    Compound: FVP
    Antiviral activity against Human immunodeficiency virus 1 NL 4-3 infected in MT4 cells measured on day 4 post infection by p24 assay
    Antiviral activity against Human immunodeficiency virus 1 NL 4-3 infected in MT4 cells measured on day 4 post infection by p24 assay
    [PMID: 25914804]
    MV4-11 IC50
    0.079 μM
    Compound: 1
    Growth inhibition of human MV4-11 cells incubated after 72 hrs by CTG- luminescence assay
    Growth inhibition of human MV4-11 cells incubated after 72 hrs by CTG- luminescence assay
    [PMID: 34415148]
    NCI-N87 IC50
    111 nM
    Compound: Alvocidib
    Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    [PMID: 32402934]
    PC-3 IC50
    110 nM
    Compound: Alvocidib
    Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    [PMID: 32402934]
    SEM EC50
    0.2043 μM
    Compound: 4
    Antiproliferative activity against human SEM cells after 72 hrs by CelTiter-Glo assay
    Antiproliferative activity against human SEM cells after 72 hrs by CelTiter-Glo assay
    [PMID: 29407975]
    Sf21 IC50
    395 nM
    Compound: 8; Alvocidib
    Inhibition of full length human N-terminal His6-tagged CDK6/N-terminal GST-tagged cyclin D3 expressed in sf21 cells using histone H1 substrate
    Inhibition of full length human N-terminal His6-tagged CDK6/N-terminal GST-tagged cyclin D3 expressed in sf21 cells using histone H1 substrate
    [PMID: 27171036]
    Sf9 IC50
    0.13 μM
    Compound: FVP
    Inhibition of CDK2/cyclin E1 (unknown origin) expressed in Sf9 insect cells using UlightCFFKNIVTPRTPPPSQGK-amide substrate after 15 mins by autoradiography
    Inhibition of CDK2/cyclin E1 (unknown origin) expressed in Sf9 insect cells using UlightCFFKNIVTPRTPPPSQGK-amide substrate after 15 mins by autoradiography
    [PMID: 25914804]
    Sf9 IC50
    2.5 nM
    Compound: 8; Alvocidib
    Inhibition of human His6-tagged CDK9/cyclin T1 expressed in baculovirus infected sf9 cells using GST-CTD as substrate after 10 mins in presence of [gamma-32P]ATP by SDS-PAGE analysis
    Inhibition of human His6-tagged CDK9/cyclin T1 expressed in baculovirus infected sf9 cells using GST-CTD as substrate after 10 mins in presence of [gamma-32P]ATP by SDS-PAGE analysis
    [PMID: 27171036]
    SK-BR-3 IC50
    75 nM
    Compound: Alvocidib
    Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    [PMID: 32402934]
    SK-OV-3 IC50
    0.22 μM
    Compound: Alvocidib
    Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
    [PMID: 32402934]
    SUP-B15 EC50
    > 86.2069 μM
    Compound: 4
    Antiproliferative activity against human SUP-B15 cells after 72 hrs by CelTiter-Glo assay
    Antiproliferative activity against human SUP-B15 cells after 72 hrs by CelTiter-Glo assay
    [PMID: 29407975]
    UoC-B1 EC50
    0.2084 μM
    Compound: 4
    Antiproliferative activity against human UOCB1 cells after 72 hrs by CelTiter-Glo assay
    Antiproliferative activity against human UOCB1 cells after 72 hrs by CelTiter-Glo assay
    [PMID: 29407975]
    体外研究
    (In Vitro)

    Flavopiridol (2 μM) robustly induces a distinct pattern of ER stress in CLL cells that contributes to cell death through IRE1-mediated activation of ASK1 and possibly downstream caspases[1]. Flavopiridol results in potent upregulation of a number of PRGs in treatments lasting 4-24 h. Flavopiridol has and immediate and long-term effect on the expression of several PRGs. In serum starved cells re-stimulated with serum, flavopiridol also inhibits the expression of these genes, but subsequently, JUNB, GADD45B and EGR1 are upregulated in the presence of flavopiridol[2].
    Flavopiridol (Alvocidib) also inhibits cyclin E1 and induces apoptosis[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    401.84

    Formula

    C21H20ClNO5

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    夫拉平度

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 33.33 mg/mL (82.94 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4886 mL 12.4428 mL 24.8855 mL
    5 mM 0.4977 mL 2.4886 mL 4.9771 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (stored under nitrogen)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.22 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.22 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.73%

    参考文献
    Cell Assay
    [1]

    The cells treated with flavopiridol are washed after 4 hours with PBS and resuspended in regular growth medium (RPMI 1640) supplemented with 10% human serum and antibiotics for the remainder of the incubation time. In the case of flavopiridol/NSC-187208 samples, NSC-187208 is re-added in the fresh media after flavopiridol is washed at 4 hours. For all the other conditions, cells are incubated with the respective drugs for 24 hours continuously.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (stored under nitrogen)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4886 mL 12.4428 mL 24.8855 mL 62.2138 mL
    5 mM 0.4977 mL 2.4886 mL 4.9771 mL 12.4428 mL
    10 mM 0.2489 mL 1.2443 mL 2.4886 mL 6.2214 mL
    15 mM 0.1659 mL 0.8295 mL 1.6590 mL 4.1476 mL
    20 mM 0.1244 mL 0.6221 mL 1.2443 mL 3.1107 mL
    25 mM 0.0995 mL 0.4977 mL 0.9954 mL 2.4886 mL
    30 mM 0.0830 mL 0.4148 mL 0.8295 mL 2.0738 mL
    40 mM 0.0622 mL 0.3111 mL 0.6221 mL 1.5553 mL
    50 mM 0.0498 mL 0.2489 mL 0.4977 mL 1.2443 mL
    60 mM 0.0415 mL 0.2074 mL 0.4148 mL 1.0369 mL
    80 mM 0.0311 mL 0.1555 mL 0.3111 mL 0.7777 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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