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ERα degrader-2
ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, exhibiting an EC50 value of 0.3 nM for ERα degradation. It can be used for the prevention and treatment of HER-positive breast cancer.
Catalog No. T39727Cas No. 2235396-63-9
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Purity:99.71%
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ERα degrader-2
Catalog No. T39727Cas No. 2235396-63-9
ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, exhibiting an EC50 value of 0.3 nM for ERα degradation. It can be used for the prevention and treatment of HER-positive breast cancer.
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. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $263 | In Stock |
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CitedProduct Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, exhibiting an EC50 value of 0.3 nM for ERα degradation. It can be used for the prevention and treatment of HER-positive breast cancer. |
| Targets&IC50 | ERα:4.6 nM |
| In vitro | In MCF-7 cells,ERα degrader-2 (0.01-40 nM) decreases ERα expression but does not fully degrade ERα even at a higher biochemical concentration. |
| In vivo | ERα degrader-2 (oral administration; 2-6 mg/kg; once daily; 21 days) demonstrates significant tumor growth inhibition in mice. Additionally, ERα degrader-2 (oral gavage; single dose of 2 mg/kg) exhibits superior pharmacokinetic properties compared to AZD9496, with a plasma exposure (AUC) of 16073.7 h*ng/mL, a half-life of 12.1 hours, and an oral availability of 80.5%[1]. |
| Molecular Weight | 492.53 |
| Formula | C29H27F3N2O2 |
| Cas No. | 2235396-63-9 |
| Storage | keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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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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