AMG 511 is a potent and selective pan class I PI3K inhibitor, capable of inhibiting PI3K signaling and inducing robust anti-proliferative effects via a G1 arrest in many tumor cell lines, with evidence of cell killing in a subset of lines.AMG 511 is highly selective over mTOR (IC50 > 10000 nM), hVPS34 (IC50 > 9000 nM), DNAPK (IC50 = 12000 nM), and a broad panel of other protein kinases. It effectively inhibited pAKT in tumor tissue in a dose- and time-dependent manner (up to 16 hours). In animal studies it efficaciously inhibited tumor growth in PTEN-null, KRAS mutant, and HER2 amplified xenograft models. It is currently in clinical trials for cancer treatment.
|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.
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.
Norman MH, et al. J Med Chem. 2012 Sep 13;55(17):7796-816. PMID: 22897589.
|Related PI3K Products|
GNE-317 is a potent, brain-penetrant PI3K inhibitor.
Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase.
SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
IPI549 is a potent and selective PI3Kγ Inhibitor with IC50 of 16 nM.
Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.