2. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease
  3. PAK NAMPT
  4. Padnarsertib

Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively.

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

CAS No. : 1643913-93-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 3 publication(s) in Google Scholar

Padnarsertib Related Antibodies

Top Publications Citing Use of Products
Flow Cytometry
Bio/Physico-chemical Assay
Cell Proliferation/Viability Assay

    Padnarsertib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jan 3;44(1):3.  [Abstract]

    Padnarsertib (KPT-9274) (0.25 μM) led to the mitigation of the facilitating effect of CYP3A5 overexpression on the neurosphere number in GSCs.

    Padnarsertib purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2026 Jan;1872(1):168065.  [Abstract]

    Padnarsertib (KPT-9274) (50-200 nM; 72 h) enhanced venetoclax-induced cell death in MV4-11VR and MOLM- 13VR cells.

    Padnarsertib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2022 Oct;9(30):e2200717.  [Abstract]

    Apoptotic analysis of Hct116 cells treated with Padnarsertib (KPT-9274; PAK4i) (2-10 μM).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively[1][2][3].

    IC50 & Target[1][2]

    PAK4

    100 nM (IC50)

    Nampt

    120 nM (IC50)

    In Vitro

    Padnarsertib attenuates the PAK4/β-catenin pathway, results in NAD depletion, and attenuates viability, invasion, and migration in several RCC cell lines. Inhibition of NAMPT in a cell-free enzymatic assay using recombinant NAMPT shows an IC50 of approximately 120 nM for Padnarsertib. Padnarsertib attenuates G2–M transit and induces apoptosis in RCC cell lines[2].

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

    Padnarsertib Related Antibodies
    In Vivo

    Padnarsertib demonstrates a decrement of xenograft growth comparable with that of Sunitinib (HY-10255A). There are minimal Padnarsertib effects on the normal human RPTECs and no apparent toxicity in vivo[2].
    Padnarsertib is currently being investigated in a phase I human clinical trial of patients with advanced solid malignancies and NHL[2].
    Padnarsertib (oral administation; 100mg/kg or 200 mg/kg; twice a day; 14 days) demonstrates a decrement of xenograft growth without no significant weight loss. 8 hours after, Padnarsertib are measured at the end of the experiment in mouse plasma and tumors with 10757 ng/mL and 10647 ng/mL, respectively[3].

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

    Animal Model: Mice[1]
    Dosage: 100mg/kg or 200 mg/kg
    Administration: Oral administation; 100mg/kg or 200 mg/kg; twice a day; 14 days
    Result: Showed a significant decrease of xenograft growth in KPT-9274 treated mouse.
    Clinical Trial
    Molecular Weight

    610.63

    Formula

    C35H29F3N4O3
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    FC(C=C1)=CC=C1C2=C(OC(CNC(/C=C/C3=CN=C(N)C=C3)=O)=C4)C4=CC(C5=CC=C(C(N6CCC(F)(F)CC6)=O)C=C5)=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (163.77 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 1.6377 mL 8.1883 mL 16.3765 mL
    5 mM 0.3275 mL 1.6377 mL 3.2753 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. 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: 2.08 mg/mL (3.41 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (3.41 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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).
    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: 99.58%

    SDS (393 KB)

    COA (247 KB) LCMS (97 KB)

    Handling Instructions (2659 KB)
    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. 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 1.6377 mL 8.1883 mL 16.3765 mL 40.9413 mL
    5 mM 0.3275 mL 1.6377 mL 3.2753 mL 8.1883 mL
    10 mM 0.1638 mL 0.8188 mL 1.6377 mL 4.0941 mL
    15 mM 0.1092 mL 0.5459 mL 1.0918 mL 2.7294 mL
    20 mM 0.0819 mL 0.4094 mL 0.8188 mL 2.0471 mL
    25 mM 0.0655 mL 0.3275 mL 0.6551 mL 1.6377 mL
    30 mM 0.0546 mL 0.2729 mL 0.5459 mL 1.3647 mL
    40 mM 0.0409 mL 0.2047 mL 0.4094 mL 1.0235 mL
    50 mM 0.0328 mL 0.1638 mL 0.3275 mL 0.8188 mL
    60 mM 0.0273 mL 0.1365 mL 0.2729 mL 0.6824 mL
    80 mM 0.0205 mL 0.1024 mL 0.2047 mL 0.5118 mL
    100 mM 0.0164 mL 0.0819 mL 0.1638 mL 0.4094 mL
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    Padnarsertib Related Classifications

    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.

    Keywords:

    Padnarsertib1643913-93-2KPT-9274KPT9274KPT 9274PAKNAMPTp21 activated kinasesNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorInhibitorinhibitorinhibit

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