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AZD9496
Catalog No. T3975Cas No. 1639042-08-2
AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity.
AZD9496
Catalog No. T3975Cas No. 1639042-08-2
AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $51 | In Stock | |
| 2 mg | $71 | In Stock | |
| 5 mg | $118 | In Stock | |
| 10 mg | $198 | In Stock | |
| 25 mg | $370 | In Stock | |
| 50 mg | $548 | In Stock | |
| 100 mg | $792 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $113 | In Stock |
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Purity:98.47%
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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 | AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity. |
| Targets&IC50 | ERα:0.28 nM. |
| In vitro | AZD9496 showed pmol/L equipotent binding to both ERα and ERβ isoforms. AZD9496 directly targets ERα for downregulation in vitro. And it also antagonizes and downregulates mutant ER in vitro and in vivo. The IC50s of ERα binding, ERα downregulation, ERα antagonism for AZD9496 are 0.82, 0.14 and 0.28 nM, respectively[1]. |
| In vivo | AZD9496 showed high oral bioavailability across three species (F% 63, 91, and 74, rat, mouse, and dog, respectively) with generally low volume and clearance across species, albeit a higher clearance in mouse. The percent free levels in human plasma of 0.15% were 5-fold higher than those measured for fulvestrant. AZD9496 is a potent, oral inhibitor of breast tumor growth in vivo. AZD9496 causes tumor regressions in combination with PI3K pathway and CDK4/6 inhibitors and in an estrogen-deprived ER+ model of resistance. This effect was accompanied by a dose-dependent decrease in PR protein levels. AZD9496 is currently being evaluated in a phase I Clinicalal trial[1]. |
| Cell Research | Cells were grown in steroid-free conditions in SILAC media containing 13C615N4 L-arginine to label ERα peptide as "heavy" and then switched to grow in media containing unlabeled l-arginine to label newly synthesized protein as "normal" with 0.1% DMSO, 300 nmol/L tamoxifen, 100 nmol/L AZD9496, or 100 nmol/L fulvestrant for the time indicated. (Only for Reference) |
| Molecular Weight | 442.47 |
| Formula | C25H25F3N2O2 |
| Cas No. | 1639042-08-2 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 82 mg/mL (185.3 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 82 mg/mL (185.3 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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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% 
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(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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