ETP-46321 - Moligand™,10mM in DMSO , CAS No.1252594-99-2

CAS: 1252594-99-2 Cat. No.: E655057 Molecular Weight: 473.55 PubChem CID: 46927938

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with K iapp s of 2.3 and 14.2 nM, respectively.

In Vitro

ETP-46321 is selected to be screened against other PI3K isoforms. ETP-46321 is more potent against isoform α (K iapp =2.3 nM). ETP-4632, has been profiled and shown to be a potent PI3K α and δ inhibitor, highly selective versus mTOR and 288 representative kinases. ETP-46321 is also tested against three of the p110α mutant enzymes detected in human cancers (E542K, E545K and H1047R), being equipotent against these mutants when compared to the wild type protein (K iapp =2.33, 1.77 and 1.89 nM for PI3Kα-H1047R, PI3Kα-E545K and PI3Kα-E542K, respectively). ETP-46321 inhibits the phosphorilation of AKT in U2OS cell line with an IC 50 of 8.3 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ETP-46321, is selected for in vivo studies based on its appealing pharmacokinetic profile in BALB-C mice, low in vivo Clearance (0.6 L/h/Kg) and good oral bioavailability (90%). ETP-46321 demonstrates a good pharmacokinetic profile in mice and is selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation, showing significant tumor growth inhibition, and reduction of the tumor metabolic activity as measured by positron emission tomography (PET) techniques . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:p110α 2.3 nM (Ki) PI3Kα-E545K 1.77 nM (Ki) PI3Kα-E542K 1.89 nM (Ki) PI3Kα-H1047R 2.33 nM (Ki) p110δ 14.2 nM (Ki) p110β 170 nM (Ki) p110γ 179 nM (Ki)

Specifications

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with K iapp s of 2.3 and 14.2 nM, respectively.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Names and Identifiers

• Isomeric SMILES: CS(=O)(=O)N1CCN(CC1)CC2=CN3C=C(N=C(C3=N2)N4CCOCC4)C5=CN=C(N=C5)N
• PubChem CID: 46927938
• MeSH Entry Terms: ETP-46321
• Molecular Weight: 473.55

Associated Targets(Human)

PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (4 Activities)

Discover Target: PIK3CA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)