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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.
| 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 |
| Related PAK Products |
|---|
| PF-3758309
PF-3758309 is a potent (Kd = 2.7 nM), ATP-competitive PAK4 inhibitor with IC50 / Ki values of 1.3 / 18.7 nM. |
| FRAX486
FRAX486 is a potent p21-activated kinase (PAK) inhibitor with IC50 values of 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively. |
| FRAX597
FRAX597 is a potent, ATP-competitive inhibitor of group I PAKs with IC50 of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively. |
| G-5555
G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively. |
| G-5555 hydrochloride
G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM. |
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