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

Padnarsertib  (Synonyms: KPT-9274)

Cat. No.: HY-12793 Purity: 99.86%
COA Handling Instructions

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.

Padnarsertib Chemical Structure

Padnarsertib Chemical Structure

CAS No. : 1643913-93-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 242 In-stock
Solution
10 mM * 1 mL in DMSO USD 242 In-stock
Solid
1 mg USD 70 In-stock
5 mg USD 180 In-stock
10 mg USD 290 In-stock
25 mg USD 480 In-stock
50 mg USD 690 In-stock
100 mg USD 940 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Padnarsertib

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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.

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
×
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: 99.86%

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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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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