(+)-BAY-1251152

(+)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation (+). (+)-BAY-1251152 is a potent and selective CDK9 inhibitor with an IC₅₀ of 3 nM. (+)-BAY-1251152 has anti-tumour activity^[1][2]. In Vitro: (+)-BAY-1251152 (Example 2) inhibits HeLa, HeLa-MaTu-ADR, NCI-H460, DU145, Caco-2, B16F10, A2780 and MOLM-13 cells proliferation with IC₅₀ values of 110 nM, 33 nM, 75 nM, 33 nM, 62 nM, 240 nM, 110 nM and 29 nM, respectively^[1].
An efficient inhibition of the proliferation of both ABC (Activated B-cell type) and GCB (Germinal-centre B-cell type) subtypes of diffuse large B-cell lymphoma (DLBCL) by (+)-BAY-1251152 (Compound A')^[2]. In Vivo: (+)-BAY-1251152 (Compound A’; 10 mg/kg; intravenous injection; once every seven days; for 14 days; female SCID mice) treatment reaches a Treatment to Control ratios (T/C) by area of 0.29 and a T/C by weight of 0.24. (+)-BAY-1251152 inhibits tumour growth and had good tolerability^[2].