NVP-CLR457 is an orally administered, non-CNS-penetrating, pan-IA-like phosphoinositide 3-kinase (PI3K) inhibitor.NVP-CLR457 shows a significant dose-dependent PK / PD / efficacy relationship.NVP-CLR457 has antitumor activity.
|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.
|Related PI3K Products|
PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts.The Ki of PF-06843195 acting on PI3Kα and PI3Kδ is less than 0.018 nM and 0.28 nM, respectively.PF-06843195 has a significant inhibitory effect on PI3K/mTOR signaling pathway and had a long-lasting anti-tumor effect.
AZD8154 is a novel inhaled selective PI3Kγδ dual inhibitor targeting airway inflammatory diseases.
ME-401 (PWT-143, P110δ-IN-1) is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay.
3-Hydroxyanthranilic Acid (3-HAA, 3-HANA), a tryptophan metabolite, has an immunomodulatory effect that may result from inhibition of PI3K/Akt/mTOR and NF-κB activity, thereby decreasing the production of pro-inflammatory mediators.
|Selective PI3Kδ Inhibitor 1 (compound 7n)
Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].
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