[CAS NO. 1643913-93-2] KPT 9274 ( ATG-019)
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PRODUCTS SPECIFICATIONS [1643913-93-2]
Store
Catalog
SLK-S8444
Brand
Selleck
CAS
1643913-93-2
DESCRIPTION [1643913-93-2]
Overview
| MDL | MFCD30207881 |
|---|---|
| Molecular Weight | 610.62 |
| Molecular Formula | C35H29F3N4O3 |
| SMILES | O=C(NCC1=CC2=CC(C3=CC=C(C(N4CCC(F)(F)CC4)=O)C=C3)=CC(C5=CC=C(F)C=C5)=C2O1)/C=C/C6=CC=C(N)N=C6 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6377 mL | 8.1884 mL | 16.3768 mL |
| 5 mM | 0.3275 mL | 1.6377 mL | 3.2754 mL |
| 10 mM | 0.1638 mL | 0.8188 mL | 1.6377 mL |
| 50 mM | 0.0328 mL | 0.1638 mL | 0.3275 mL |
Description
KPT 9274 ( ATG-019) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of and . It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay.
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.
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. 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.
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