Asciminib (ABL001) is a potent and selective allosteric ABL1 inhibitor with IC50 of 0.25 nM in BCR-ABL1-transformed BaF3 cells.
Asciminib (ABL-001) binds (Kd=0.5-0.8 nM) to the myristoyl pocket of ABL1 and induces the formation of an inactive kinase conformation.
Asciminib (ABL-001) inhibits phosphorylation of both STAT5 (Tyr694; pSTAT5) and BCR–ABL1 (Tyr245; pBCR–ABL1), and shows selective activity against all BCR–ABL1 cell lines (IC50=1-20 nM).
Asciminib (ABL-001) retains activity against mutated ABL-1 Thr315Ile at low nanomolar concentrations.
Asciminib (ABL-001) is active in vivo, moderate oral absorption.
