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  2. Estrogen Receptor/ERR

AZD9496 

Cat. No.: HY-12870 Purity: 99.55% ee.: 100.00%
Handling Instructions

AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM.

For research use only. We do not sell to patients.
AZD9496 Chemical Structure

AZD9496 Chemical Structure

CAS No. : 1639042-08-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 128 In-stock
2 mg USD 84 In-stock
5 mg USD 132 In-stock
10 mg USD 228 In-stock
25 mg USD 456 In-stock
50 mg USD 684 In-stock
100 mg USD 1020 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of AZD9496:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM.

IC50 & Target

IC50: 0.28 nM (ERα antagonism), 0.14 nM (ERα downregulation), 0.82 nM (ERα binding)[1]

In Vitro

The potency of AZD9496 with IC50 of 0.82 nM, 0.14 nM, and 0.28 nM in ERα binding, downregulation, and antagonism, respectively. AZD9496 significantly inhibits MCF-7 cell growth with EC50 of 0.04 nM[1]. Selectivity of AZD9496 over other tested nuclear hormone receptors is high: androgen receptor (AR), IC50=30 μM; glucocorticoid receptor (GR), IC50=9.2 μM; progesterone receptor (PR), IC50=0.54 μM[2].

In Vivo

Significant tumor growth inhibition is observed as low as 0.5 mg/kg dose in the estrogen-dependent MCF-7 xenograft model, where this effect is accompanied by a dose-dependent decrease in PR protein levels, demonstrating potent antagonist activity. Combining AZD9496 with PI3K pathway and CDK4/6 inhibitors lead to further growth-inhibitory effects compared with monotherapy alone. AZD9496, given once daily orally at 5 and 25 mg/kg produced statistically significant increases in uterine weight compared with the fulvestrant control (P<0.001) but significantly lower than tamoxifen (P=0.001)[1]. AZD9496 is also tested in a long-term estrogen deprived model (LTED), using the HCC-1428 LTED cell line that grows in the absence of estrogen and is thought to best represent a model of aromatase inhibition. AZD9496 shows significant activity, with a dose of 5 mg/kg giving tumor regressions in this model[2].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.2600 mL 11.3002 mL 22.6004 mL
5 mM 0.4520 mL 2.2600 mL 4.5201 mL
10 mM 0.2260 mL 1.1300 mL 2.2600 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

AZD9496 is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 0.1%) before use[1].

Effect of AZD9496, Fulvestrant, and Tamoxifen on ERα peptide turnover in MCF-7 cells. Cells are grown in steroid-free conditions in SILAC media containing 13C615N4 L-arginine to label ERα peptide as “heavy” (blue line) and then switched to grow in media containing unlabeled L-arginine to label newly synthesized protein as “normal” (red line) with 0.1% DMSO, 300 nM Tamoxife, 100 nM AZD9496, or 100 nM Fulvestrant for the time indicated. Data shown is representative of two independent experiments[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

AZD9496 is prepared in PEG/captisol (Mice)[1].

Mice[1]
In vivo efficacy of AZD9496 in MCF-7 xenograft model. MCF-7 xenografts, grown in male SCID mice, are dosed daily with either PEG/captisol (vehicle) or AZD9496 (0.02, 0.1, 0.5, 10, and 50 mg/kg, p.o., q.d.). Tumor growth is measured by caliper at regular intervals and mean tumor volumes plotted for each dosed group. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

442.47

Formula

C₂₅H₂₅F₃N₂O₂

CAS No.

1639042-08-2

Storage

4°C, protect from light, stored under nitrogen

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 104.5 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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AZD9496
Cat. No.:
HY-12870
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