XZ8078

XZ8078 (compound C16a) potently inhibits the proliferation of MDA-MB-436 breast cancer cells with an IC₅₀ of 0.006 nM, and also potently suppresses the proliferation of Capan-1 pancreatic cancer cells with an IC₅₀ of 3.08 nM; it blocks the interaction between PARP1 and DNA in a cell-free system, with a corresponding EC₅₀ of 14.02 nM^[1].
XZ8078 exhibits around 19-fold loss of antiproliferative potency in PARP1-knockout Capan-1 pancreatic cancer cells and an approximately 8.41-fold activity drop in CRBN-knockout Capan-1 pancreatic cancer cells, verifying its antiproliferative effects rely on both PARP1 and CRBN^[1].
XZ8078 (10-1000 nM; 48 h) selectively degrades PARP without interfering with PARP2, with DC₅₀ values of 98.52 nM and 23.01 nM in MDA-MB-436 and Capan-1 cells, respectively; its PARP1 degradation activity is significantly attenuated in Olaparib (HY-10162)-resistant Capan-1/OP cells and HR wild-type HCT116 cells, with corresponding DC₅₀ values of 292.6 nM and > 1000 nM^[1].
XZ8078 (10-1000 nM; 48 hours) induces concentration-dependent and selective degradation of IKZF3 without altering IKZF1 expression, with DC₅₀ values of 86.81 nM and 23.20 nM in MDA-MB-436 and Capan-1 cells, respectively. The IKZF3-degrading activity of this molecule decreases significantly in Olaparib-resistant Capan-1/OP cells and HR-proficient HCT116 cells, with corresponding DC₅₀ values of 258.10 nM and > 1000 nM. The IKZF3-degrading capacity correlates with cytotoxicity.
XZ8078 (1 μM; 24 h) mediates the degradation of PARP1 in MDA-MB-436 breast cancer cells, a process dependent on CRBN recruitment, the ubiquitin-proteasome system, and target binding to PARP1^[1].
XZ8078 (administration dose range; administered for 7 days) is a broad-spectrum antiproliferative agent that inhibits the growth of HR-deficient, HR-proficient and hematologic malignant cell lines, with IC₅₀ values ranging from 0.006 nM to 388.99 nM^[1].

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