SA-VA

• Description:

  SA-VA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase[1].

• UNSPSC:

  12352005

• Target:

  Apoptosis; Ephrin Receptor; PROTACs; VEGFR

• Type:

  Reference compound

• Related Pathways:

  Apoptosis; PROTAC; Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/sa-va.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C(NCC1=CN(CCCCC(N[C@@H](C(C)(C)C)C(N2[C@H](C(NCC3=CC=C(C4=C(C)N=CS4)C=C3)=O)C[C@@H](O)C2)=O)=O)N=N1)C5=NC=CC(OC6=CC=C(NC(NC7=CC=C(Cl)C(C(F)(F)F)=C7)=O)C=C6)=C5

• Molecular Formula:

  C50H53ClF3N11O7S

• Molecular Weight:

  1044.54

• References & Citations:

  [1]Ru Si, et al. Discovery of intracellular self-assembly protein degraders driven by tumor-specific activatable bioorthogonal reaction. Eur J Med Chem. 2023 Sep 5;257:115497.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  VEGFR2/KDR/Flk-1; von Hippel-Lindau (VHL)