Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||100 mg/mL in DMSO|
A phase I study of oral ARRY-614, a p38 MAPK/Tie2 dual inhibitor, in patients with low or intermediate-1 risk myelodysplastic syndromes.
Garcia-Manero G, et al. Clin Cancer Res. 2015 Mar 1;21(5):985-94. PMID: 25480830.
|Related p38 MAPK Products|
R1487 Hydrochloride is an orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.
Dilmapimod (also known as SB-681323 and GW-681323) is a p38 MAPK inhibitor that potentially suppresses inflammation in COPD.
Pamapimod is a novel p38 mitogen-activated protein kinase inhibitor, inhibited p38alpha and p38beta enzymatic activity, with IC50 values of 0.014 +/- 0.002 and 0.48 +/- 0.04 microM, respectively.
SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.
SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po). IC50 value: 170 nM Target: p38MAPK
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