LX-039

• UNSPSC Description:

  LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity[1].

• Target Antigen:

  Estrogen Receptor/ERR

• Type:

  Reference compound

• Related Pathways:

  Vitamin D Related/Nuclear Receptor

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/lx-039.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C(O)/C=C/C1=CC=C(/C(C(N2)=C(Cl)C3=C2C=CC=C3)=C(C4=CC=C(F)C=C4Cl)\CC)C=C1

• Molecular Weight:

  480.36

• References & Citations:

  [1]Lu J, Chan CC, Sun D, et al. Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD). Bioorg Med Chem Lett. 2022;66:128734.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  Phase 1

• CAS Number:

  2135341-09-0