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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 62 mg/mL|
|Related PAK Products|
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 is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
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.
FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively.
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.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.