| Legal Status: | Investigational New Drug |
| Cas Number: | 1073154-85-4 |
| Pubchem: | 25117126 |
| Drugbank: | DB12282 |
| Chemspiderid: | 32695161 |
| Unii: | 53O87HA2QU |
| Kegg: | D10618 |
| Chembl: | 3137331 |
| Pdb Ligand: | 7KD |
| Synonyms: | PF-04554878, VS-6063 |
| Iupac Name: | N-methyl-4-4-3-[methyl(methylsulfonyl)amino]pyrazin-2-ylmethylamino]-5-(trifluoromethyl)pyrimidin-2-ylamino]benzamide| C=20 | H=21 | F=3 | N=8 | O=3 | S=1| SMILES = CNC(=O)C1=CC=C(C=C1)NC2=NC=C(C(=N2)NCC3=NC=CN=C3N(C)S(=O)(=O)C)C(F)(F)F| StdInChI = 1S/C20H21F3N8O3S/c1-24-18(32)12-4-6-13(7-5-12)29-19-28-10-14(20(21,22)23)16(30-19)27-11-15-17(26-9-8-25-15)31(2)35(3,33)34/h4-10H,11H2,1-3H3,(H,24,32)(H2,27,28,29,30)| StdInChIKey = FWLMVFUGMHIOAA-UHFFFAOYSA-N}}Defactinib (INN, codenamed VS-6063) is an inhibitor of PTK2, also known as focal adhesion kinase (FAK), Pyk2, and MELK which was developed by Pfizer and licensed to Verastem Oncology as a potential treatment for solid tumors. Development for mesothelioma was discontinued in 2015 due to lack of efficacy in a placebo-controlled phase II trial.[1] [2] Subsequent research in patients with specific NF2 mutations also found limited activity.[3] As of 2022, it remains in trials in combination with other medications for other types of cancer. References |