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  2. CDK Autophagy HIV Apoptosis
  3. Flavopiridol

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

Cat. No.: HY-10005 Purity: 99.73%
SDS COA Handling Instructions Technical Support

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

For research use only. We do not sell to patients.

Flavopiridol Chemical Structure

Flavopiridol Chemical Structure

CAS No. : 146426-40-6

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Customer Review

Based on 43 publication(s) in Google Scholar

Other Forms of Flavopiridol:

Top Publications Citing Use of Products

41 Publications Citing Use of MCE Flavopiridol

RT-PCR
Proliferation Assay

    Flavopiridol purchased from MedChemExpress. 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 MedChemExpress. 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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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)

    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]
    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].

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

    Clinical Trial
    Molecular Weight

    401.84

    Formula

    C21H20ClNO5

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C2=C(C=C(C([C@]3([H])[C@H](O)CN(C)CC3)=C2OC(C4=CC=CC=C4Cl)=C1)O)O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, stored under nitrogen

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (82.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.73%

    References
    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.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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      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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    Flavopiridol
    Cat. No.:
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