ERα degrader-2

SKU: orb1984610

Description

ERα degrader-2 is a potent and selective SERD that degrades the estrogen receptor with an EC50 of 0.3 nM. It demonstrates anticancer activity and is a research tool for studying HER2-positive breast cancer, applicable in both in vitro and in vivo experimental models.

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 2235396-63-9
• MW: 492.53
• Purity: 99.71% (May vary between batches)
• Formula: C₂₉H₂₇F₃N₂O₂
• SMILES: [H][C@@]1(N(CC(C)(C)F)[C@H](C)Cc2c1[nH]c1ccccc21)c1c(F)cc(cc1F)-c1ccc(cc1)C(O)=O
• Target: ERK,Estrogen Receptor/ERR
• Solubility: DMSO:1.66 mg/mL (3.37 mM)

Bioactivity

• Target IC50:
  ERα:4.6 nM
• 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%.
• 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.

Storage & Handling

• 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/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ERK, ERα degrader 2, ERα degrader2, ERα degrader-2, ERalpha degrader-2, ERa degrader-2

Compound Identifiers

PubChem CID

135230895