BI 2536 (GMP)

Exceeding a 100-fold concentration range starting at 10 nM, BI 2536 (GMP) causes HeLa cells to accumulate with a 4N DNA content, indicative of a cell-cycle block in either G2 phase or mitosis. In addition to HeLa cells, BI 2536 (GMP) potently inhibits the proliferation of a panel of 32 human cancer cell lines, representing diverse organ derivations (including carcinomas of the breast, colon, lung, pancreas, and prostate, melanomas, and hematopoietic cancers) and varied patterns of tumor suppressor or oncogene mutations (including RB1, TP53, PTEN, andKRAS status). The half-maximal effective concentration (EC₅₀) values in this cell panel ranged 2-25 nM, whereas a concentration of 100 nM of BI 2536 (GMP) is typically sufficient for inducing a complete mitotic arrest. The proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells is blocked at EC₅₀values ranging 12-31 nM, indicating a comparable sensitivity of cycling nontransformed cells to BI 2536 (GMP)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.