KPT 9274 ( ATG-019)

Catalog No.S8444

For research use only.

KPT 9274 ( ATG-019) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay.

KPT 9274 ( ATG-019) Chemical Structure

CAS No. 1643913-93-2

Selleck's KPT 9274 ( ATG-019) has been cited by 1 Publication

Purity & Quality Control

Choose Selective NAMPT Inhibitors

Biological Activity

Description KPT 9274 ( ATG-019) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay.
PAK4 [1]
(Cell-free assay)
(Cell-free assay)
~120 nM
In vitro

KPT-9274 interferences with PAK4 and NAD biosynthetic pathways results in reduction of G2/M transit as well as induction of apoptosis and decrease in cell invasion and migration in several human RCC cell lines. The inhibition of the PAK4 pathway by KPT-9274 attenuates nuclear β-catenin as well as the Wnt/β-catenin targets cyclin D1 and c-Myc[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-8-5-11 NUnjT4s6eUiWUzDhd5NigQ>? MY\QMYdtgWOxcILveIVqdiC|dXLzeJJifGW|IHnk[Y51cW[rZXSgbY4hU0JvOD21MVEyKGGmZX7vZ4Fz[2mwb33hJINmdGxibHnu[UwheUiWUzD0bIVz[XCndYTpZ{BtcWK{YYL5JJNkemWnbh?= MmjJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3MUWyPFQoRjNzNUG1Nlg1RC:jPh?=
KB-3-1 NX7TR|lTeUiWUzDhd5NigQ>? NFW5[pRRNWeueXPvdJJwfGWrbjDzeYJ{fHKjdHXzJIll\W62aX\p[YQhcW5iS1KtN{0yKGGmZX7vZ4Fz[2mwb33hJINmdGxibHnu[UwheUiWUzD0bIVz[XCndYTpZ{BtcWK{YYL5JJNkemWnbh?= M4TjN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUG1Nlg1Lz5|MUWxOVI5PDxxYU6=
In vivo KPT-9274 administration to a 786-O (VHL-mut) human RCC xenograft model leads to dose-dependent inhibition of tumor growth with no apparent toxicity[1]. It also shows remarkable anti-tumor activity in sub-cutaneous xenograft models of pancreatic ductal adenocarcinoma (PDAC) cell lines and cancer stem cells as a single agent. KPT-9274 possesses desirable PK properties and is well tolerated in mice with the absence of any signs of toxicity when 200 mg/kg daily is administered either intravenously or orally[2].

Protocol (from reference)

Cell Research:


  • Cell lines: 786-0, ACHN, Caki-1 and U-2 OS cells
  • Concentrations: 1μM and 5μM
  • Incubation Time: 12 hours
  • Method:

    The in vitro cell migration and invasion assays were performed using transwell chambers. For the transwell migration assay, 1.5×104 cells were seeded on top of the polycarbonate filters, and 0.6 ml of growth medium with DMSO or KPT-9274 (1μM and 5μM) was added to both the upper and lower wells. After incubation for 12 hours, the filters were swabbed with a cotton swab, fixed with methanol, and then stained with Giemsa solution. For the in vitro invasion assay, filters were coated with Matrigel, and 2.5×104 cells were seeded onto the Matrigel and incubated for 20 hours. The cells attached to the lower surface of the filter were counted under a light microscope (10× magnification).

Animal Research:


  • Animal Models: 786-O (VHL-mut) human RCC xenograft model (nude mice)
  • Dosages: 100 and 200 mg/kg
  • Administration: by oral gavage

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(163.76 mM)
Ethanol 100 mg/mL
(163.76 mM)
Water Insoluble

Chemical Information

Molecular Weight 610.62


CAS No. 1643913-93-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1(F)F)C(=O)C2=CC=C(C=C2)C3=CC(=C4C(=C3)C=C(O4)CNC(=O)C=CC5=CN=C(C=C5)N)C6=CC=C(C=C6)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy KPT 9274 ( ATG-019) | KPT 9274 ( ATG-019) supplier | purchase KPT 9274 ( ATG-019) | KPT 9274 ( ATG-019) cost | KPT 9274 ( ATG-019) manufacturer | order KPT 9274 ( ATG-019) | KPT 9274 ( ATG-019) distributor