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Cat. No. M9528
KPT-9274 Structure


Size Price Availability Quantity
5mg USD 270  USD270 In stock
10mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

KPT-9274, also known as PAK4-IN-1, is a potent, selective and dual PAK4/NAMPT inhibitor with IC50s less than 100 and 120 nM, respectively. KPT-9274 interferences with PAK4/NAMPT signaling pathways, which 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. KPT-9274 demonstrated the expected on-target effects in this mouse model. KPT-9274 (oral administation; 100mg/kg or 200 mg/kg; twice a day; 14 days) demonstrates a decrement of xenograft growth and exists no significant weight loss in animals receiving KPT-9274. 8 hours after, KPT-9274 are measured at the end of the experiment in mouse plasma and tumors with 10757 ng/ml and 10647 ng/ml, respectively.

Chemical Information
Molecular Weight 610.63
Formula C35H29F3N4O3
CAS Number 1643913-93-2
Solubility (25°C) DMSO ≥ 62 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Chetan Rane, et al. Sci Rep. A Novel Orally Bioavailable Compound KPT-9274 Inhibits PAK4, and Blocks Triple Negative Breast Cancer Tumor Growth.

[2] Omran Abu Aboud, et al. Mol Cancer Ther. Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth

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Keywords: KPT-9274, PAK4-IN-1 supplier, PAK, inhibitors, activators

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