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  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)

目錄號: HY-10005 純度: 99.73%
COA 產(chǎn)品使用指南

Flavopiridol (Alvocidib) 是一種競爭型的 CDK 廣譜抑制劑, 抑制 CDK1,CDK2,CDK4的IC50 分別為30,170,100 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報,我們不為任何個人用途提供產(chǎn)品和服務(wù)

Flavopiridol Chemical Structure

Flavopiridol Chemical Structure

CAS No. : 146426-40-6

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Customer Review

Other Forms of Flavopiridol:

MCE 顧客使用本產(chǎn)品發(fā)表的 41 篇科研文獻(xiàn)

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

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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)

    細(xì)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]
    體外研究
    (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 號
    性狀

    固體

    顏色

    Light yellow to yellow

    中文名稱

    夫拉平度

    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式

    4°C, stored under nitrogen

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

    溶解性數(shù)據(jù)
    細(xì)胞實驗: 

    DMSO 中的溶解度 : 33.33 mg/mL (82.94 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (stored under nitrogen)。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗:

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

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

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實驗過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 Tween 80,均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

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

    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.73%

    參考文獻(xiàn)
    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.

    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (stored under nitrogen)。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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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