keep away from direct sunlight,keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, inhibits ERα, and has an EC50 value for estrogen receptor degradation of 0.3 nM.ERα degrader-2 can be used for the prevention and treatment of HER-positive breast cancer.
Pack Size | Availability | Price/USD | Quantity |
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1 mg | In stock | $ 263.00 |
Description | ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, inhibits ERα, and has an EC50 value for estrogen receptor degradation of 0.3 nM.ERα degrader-2 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[1]. ERα degrader-2 (oral gavage; single dose of 2 mg/kg) exhibits better pharmacokinetic properties than AZD9496, with a plasma exposure (AUC) of 16073.7 h*ng/mL, a half-life period of 12.1 hours, and an oral availability of 80.5%[1]. |
Molecular Weight | 492.53 |
Formula | C29H27F3N2O2 |
CAS No. | 2235396-63-9 |
keep away from direct sunlight,keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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