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ETP-46321

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Purity:99.47%

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COA HPLC HNMR

ETP-46321

Catalog No. TQ0229Cas No. 1252594-99-2

ETP-46321 is an effective and orally bioavailable PI3Kα/PI3Kδ inhibitor (Ki: 2.3/14.2 nM).

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Pack Size	Price	Availability
1 mg	$78	In Stock
5 mg	$189	In Stock
10 mg	$297	In Stock
25 mg	$562	In Stock
50 mg	$787	In Stock
100 mg	$1,080	In Stock
500 mg	$2,180	In Stock
1 mL x 10 mM (in DMSO)	$198	In Stock

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Product Introduction

Bioactivity

Description	ETP-46321 is an effective and orally bioavailable PI3Kα/PI3Kδ inhibitor (Ki: 2.3/14.2 nM).
In vitro	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 (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 vivo	ETP-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.
Animal Research	BALB/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.

Chemical Properties

Molecular Weight	473.55
Formula	C20H27N9O3S
Cas No.	1252594-99-2

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (63.35 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1117 mL	10.5585 mL	21.1171 mL	105.5855 mL
5 mM	0.4223 mL	2.1117 mL	4.2234 mL	21.1171 mL
10 mM	0.2112 mL	1.0559 mL	2.1117 mL	10.5585 mL
20 mM	0.1056 mL	0.5279 mL	1.0559 mL	5.2793 mL
50 mM	0.0422 mL	0.2112 mL	0.4223 mL	2.1117 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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Tech Support

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