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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 |
| 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.
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LCH-7749944 (GNF-PF-2356) is a novel and potent p21-activated kinase 4 (PAK4) inhibitor with an IC50 of 14.93 μM and has less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4. |
| G-5555 hydrochloride
G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM. |
| 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. |
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FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively. |
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