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Postion:Product Catalog >Biochemical Engineering>Biochemical Reagents>Agonist Inhibitors>ETP-46321
ETP-46321
  • ETP-46321

ETP-46321 NEW

Price $33 $79 $125
Package 1mg 5mg 10mg
Supply Ability: 10g
Update Time: 2026-04-21

Product Details

Product Name: ETP-46321 CAS No.: 1252594-99-2
Purity: 99.80% Supply Ability: 10g
Release date: 2026/04/21

Product Introduction

Bioactivity

NameETP-46321
DescriptionETP-46321 is an effective and orally bioavailable PI3Kα/PI3Kδ inhibitor (Ki: 2.3/14.2 nM).
Animal ResearchBALB/C mice are treated daily with ETP-46321 (50 mg/kg, p.o.) for three weeks. Tumor volumes of four mice in each treatment group are measured and compared to the starting volume at the beginning of the treatment.
In vitroETP-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 (Kiapp=2.33, 1.77 and 1.89 nM for PI3Kα-H1047R, PI3Kα-E545K and PI3Kα-E542K, respectively). ETP-46321 inhibits the phosphorylation of AKT in the U2OS cell line (IC50: 8.3 nM).
In vivoETP-46321 has been chosen for in vivo studies due to its promising pharmacokinetic profile in BALB-C mice, characterized by low in vivo Clearance (0.6 L/h/Kg) and high oral bioavailability (90%). This selection was further justified for a preliminary in vivo evaluation in a lung tumor mouse model influenced by a K-RasG12V oncogenic mutation, where it exhibited notable tumor growth inhibition.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility InformationDMSO : 30 mg/mL (63.35 mM), Sonication is recommended.
KeywordsPI3Kδ | PI3Kα-H1047R | PI3Kα-E545K | PI3Kα-E542K | PI3Kα | PI3K | Phosphoinositide 3-kinase | p110δ | p110γ | p110β | p110α | Inhibitor | inhibit | ETP-46321 | ETP46321 | ETP 46321
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Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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TargetMol Chemicals Inc.
2026-04-22

TargetMol Chemicals Inc.

4YR United StatesUnited States
  • Since: 2011-01-07
  • Address: 36 Washington Street, Wellesley Hill, USA
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