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AZD9496

Name: AZD9496
Brand: TargetMol
SKU: T3975
Price: 51 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T3975Cas No. 1639042-08-2

AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity.

AZD9496

🥰Excellent

Purity: 98.47%

Catalog No. T3975Cas No. 1639042-08-2

AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$51	In Stock	In Stock
2 mg	$71	In Stock	In Stock
5 mg	$118	In Stock	In Stock
10 mg	$198	In Stock	In Stock
25 mg	$370	In Stock	In Stock
50 mg	$548	In Stock	In Stock
100 mg	$792	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$113	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

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Batch Information

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Purity:98.47%

Color:White to Yellow

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

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)

Chemical Properties

Molecular Weight	442.47
Formula	C₂₅H₂₅F₃N₂O₂
Cas No.	1639042-08-2
Smiles	C(C(C)(C)F)N1[C@@H](C2=C(C=3C(N2)=CC=CC3)C[C@H]1C)C4=C(F)C=C(/C=C/C(O)=O)C=C4F
Relative Density.	1.286 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (282.51 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 82 mg/mL (185.32 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.46 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2600 mL	11.3002 mL	22.6004 mL	113.0020 mL
5 mM	0.4520 mL	2.2600 mL	4.5201 mL	22.6004 mL
10 mM	0.2260 mL	1.1300 mL	2.2600 mL	11.3002 mL
20 mM	0.1130 mL	0.5650 mL	1.1300 mL	5.6501 mL
50 mM	0.0452 mL	0.2260 mL	0.4520 mL	2.2600 mL
100 mM	0.0226 mL	0.1130 mL	0.2260 mL	1.1300 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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc