VS-4718

VS-4718 is an orally bioavailable, selective, and reversible small molecule inhibitor of focal adhesion kinase (FAK), a cytoplasmic tyrosine kinase involved in tumor cell invasion, migration, proliferation, and cancer stem cell survival. By inhibiting FAK autophosphorylation at Tyr397, VS-4718 blocks integrin-mediated activation of downstream signaling pathways such as ERK, JNK/MAPK, and PI3K/Akt. This results in reduced cancer stem cell populations and inhibition of tumor growth and metastasis. It also reverses multidrug resistance mediated by ABCB1 and ABCG2 transporters. Developed primarily for oncology indications including acute myeloid leukemia (AML), B-cell acute lymphoblastic leukemia (ALL), pancreatic cancer, solid tumors, breast cancer, ovarian cancer, and malignant pleural mesothelioma. The drug was originally developed by Verastem (now Verastem Oncology) with preclinical work from The Scripps Research Institute[1][3][4][5][6][7].

Other names

VS-4718VS4718VS 4718PND-1186PND1186PND 1186