FAK ligand-Linker Conjugate 1

• CAT Number: I017987
• CAS Number: 2307461-45-4
• Molecular Formula: C25H28F3N5O6S
• Molecular Weight: 583.58
• Purity: ≥95%
• Synonyms: 3-[2-[4-[[4-[[3-[methyl(methylsulfonyl)amino]phenyl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenoxy]ethoxy]propanoic acid
• InChI: InChI=1S/C25H28F3N5O6S/c1-33(40(2,36)37)19-5-3-4-17(14-19)15-29-23-21(25(26,27)28)16-30-24(32-23)31-18-6-8-20(9-7-18)39-13-12-38-11-10-22(34)35/h3-9,14,16H,10-13,15H2,1-2H3,(H,34,35)(H2,29,30,31,32)
• InChIKey: OSVHAJNGZCDBGV-UHFFFAOYSA-N
• SMILES: CN(C1=CC=CC(=C1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC=C(C=C3)OCCOCCC(=O)O)S(=O)(=O)C

FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation[1].

Reference

[1]. Cromm PM, et al. Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation. J Am Chem Soc. 2018 Dec 12;140(49):17019-17026.
 [Content Brief]