APO-50815

APO-50815 (Compound 14) potently inhibits recombinant human WEE1 kinase with an IC₅₀ of 9 nM, exhibits 10-fold selectivity for WEE1 over PLK1, and is inactive against CHK1 at concentrations up to 10 μM^[1].
APO-50815 (100 pM-100 μM; 5 days) potently reduces viability of TP53-mutated peritoneal metastatic CRC organoid lines PM003 (IC₅₀ = 37 nM) and PM025 (IC₅₀ = 74 nM), with superior efficacy compared to clinical and preclinical WEE1 inhibitors^[1].
APO-50815 (100 pM-100 μM; 5 days) potently reduces viability of TP53-mutated liver metastatic CRC organoid line QEH039LM (IC₅₀ = 50 nM) and exhibits enhanced activity against the KRAS^G12X-mutated, WEE1 inhibitor-resistant line QEH042LM (IC₅₀ = 633 nM), outperforming clinical WEE1 inhibitors^[1].
APO-50815 (100 pM-100 μM; 5 days) potently and selectively reduces viability of primary CRC organoids across diverse mutation profiles, with exceptional therapeutic indices of 238 (RAH051), 146 (RAH035), and 129 (RAH057)^[1].
APO-50815 (300 nM; 48 h) significantly reduces active cycling, amplifies DNA damage and S phase accumulation, and enhances apoptosis in TP53-WT, BRAF^V600E primary CRC organoid line RAH051T^[1].
APO-50815 (90 nM; 2 h) significantly reduces pTyr15-CDK1 levels in MDA-MB-231HM cells, confirming intracellular WEE1 target engagement and functional inhibition^[1].
APO-50815 (1 μM; up to 60 min at 37 °C) has poor metabolic stability in human and mouse liver microsomes, with short half-lives and high intrinsic clearances indicating rapid metabolism^[1].

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