ALK5 Inhibitor is a potent and selective inhibitor of the TGF-β RI kinase with IC50 values of 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding, respectively. It enhances the efficiency of cellular reprogramming. ALK5 Inhibitor affects a range of related kinases selectively, including p38 MAPK, GSK3 and JNK1 (IC50 > 16 μM).
|Cell lines||iPS cells|
|Preparation method||Cell Cyle Analysis Cells were treated with 25 μΜ RepSox in mES media without feeders for 72 hours and subjected to cell cycle analysis by propidium iodide staining and flow cytometry. Cells were harvested with .25% trypsin and fixed with 70% ethanol overnight. Following at least one hour of incubation with propidium iodide staining solution (50 μg/ml propidium iodide in PBS, .1% BSA, .1% Rnase A) in the dark, samples were analyzed on a BD LRSII Flow Cytometer (BD Biosciences).|
|Incubation time||72 h|
|Animal models||chimeric embryos E13.5|
|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||DMSO ≥5 mg/mL|
|Related ALK Products|
Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2.
Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK. Crizotinib inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM). Crizotinib is useful in treatment of anaplastic large-cell lymphoma.
Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
ALK-IN-1 is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.
CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.