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KPT-9274

Cat. No. M9528
KPT-9274 Structure
Synonym:

PAK4-IN-1

Size Price Availability Quantity
5mg USD 270  USD270 In stock
10mg USD 400  USD400 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 610.63
Formula C35H29F3N4O3
CAS Number 1643913-93-2
Purity >98.5%
Solubility DMSO ≥ 62 mg/mL
Storage at -20°C
References

[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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  Catalog
Abmole Inhibitor Catalog




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

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