vamotinib

Vamotinib (PF-114) is a potent, selective, and orally active small molecule tyrosine kinase inhibitor designed to target the Bcr-Abl fusion oncoprotein—including forms with the T315I gatekeeper mutation—which is associated with resistance to second-generation Bcr-Abl inhibitors. By inhibiting autophosphorylation of BCR/ABL and its T315I mutant form, vamotinib blocks aberrant tyrosine kinase activity in Philadelphia chromosome-positive (Ph+) hematologic malignancies such as chronic myeloid leukemia (CML), leading to reduced proliferation and increased apoptosis of malignant cells. Vamotinib has demonstrated anti-proliferative and anti-tumor activity in preclinical studies and has reached Phase 2 clinical trials for CML resistant to other therapies[1][3][4][5][7].

Other names

1416241-23-0UNII-I8C3R768IZUNII-I-8C3R768IZUNII-I 8C3R768IZ