PROTAC AR-V7 degrader-1

• UNSPSC Description:

  PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM[1].

• Target Antigen:

  Androgen Receptor; PROTACs

• Type:

  Reference compound

• Related Pathways:

  PROTAC;Vitamin D Related/Nuclear Receptor

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/protac-ar-v7-degrader-1.html

• Solubility:

  DMSO : 110 mg/mL (ultrasonic)

• Smiles:

  O=C(CCCCOC1=CC=C(C2=CSC(N3CCOCC3)=N2)C=C1)N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(N[C@H](C5=CC=C(C=C5)C6=C(N=CS6)C)C)=O)=O

• Molecular Weight:

  789.02

• References & Citations:

  [1]Archana Bhumireddy, et al. Design, synthesis, and biological evaluation of phenyl thiazole-based AR-V7 degraders. Bioorg Med Chem Lett. 2022 Jan 1;55:128448.

• Shipping Conditions:

  Blue Ice

• Clinical Information:

  No Development Reported

• CAS Number:

  2767440-24-2