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ETP-46321
🥰Excellent
Catalog No. TQ0229Cas No. 1252594-99-2
ETP-46321 is an effective and orally bioavailable PI3Kα/PI3Kδ inhibitor (Ki: 2.3/14.2 nM).
ETP-46321
🥰Excellent
Purity: 99.80%
Catalog No. TQ0229Cas No. 1252594-99-2
ETP-46321 is an effective and orally bioavailable PI3Kα/PI3Kδ inhibitor (Ki: 2.3/14.2 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | 44 € | In Stock | |
| 5 mg | 107 € | In Stock | |
| 10 mg | 169 € | In Stock | |
| 25 mg | 320 € | In Stock | |
| 50 mg | 448 € | In Stock | |
| 100 mg | 615 € | In Stock | |
| 200 mg | 833 € | In Stock | |
| 1 mL x 10 mM (in DMSO) | 113 € | In Stock |
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Purity:99.80%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | ETP-46321 is an effective and orally bioavailable PI3Kα/PI3Kδ inhibitor (Ki: 2.3/14.2 nM). |
| Targets&IC50 | p110α:2.3 nM (Ki), p110γ:179 nM (Ki), p110β:170 nM (Ki), PI3Kα (E542K):1.77 nM (Ki), PI3Kα (H1047R):2.33 nM (Ki), p110δ:14.2 nM (Ki), PI3Kα (E542K):1.89 nM (Ki) |
| 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. |
| Molecular Weight | 473.55 |
| Formula | C20H27N9O3S |
| Cas No. | 1252594-99-2 |
| Smiles | CS(=O)(=O)N1CCN(Cc2cn3cc(nc(N4CCOCC4)c3n2)-c2cnc(N)nc2)CC1 |
| Relative Density. | 1.59 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (63.35 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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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 . A total of 10 animals were administered, and the formula you used is 5% 
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 (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.
(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 main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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