Catalog No.: PC-24518Not For Human Use, Lab Use Only.
BEN-28010 is a potent selective, orally bioavailable and brain-penetrant checkpoint kinase 1 (CHK1) inhibitor with IC50 of 4 nM, 450-fold selective over CHK2.
BEN-28010 is a potent selective, orally bioavailable and brain-penetrant checkpoint kinase 1 (CHK1) inhibitor with IC50 of 4 nM, 450-fold selective over CHK2.
BEN-28010 potently inhibits pCHK1 in SW620 cells with IC50 of 0.45 uM, inhibits LN-18/A172 cell viability with IC50 of 0.14/3.3 uM.
BEN-28010 also has good selectivity for CHK1 over the diverse Cerep SafetyScreen87 panel of 87 enzymes.
BEN-28010 demonstrated efficacy in several GBM CDX and PDX models as a monotherapy and in combination with ionizing radiation, including improved overall survival in an intracranially implanted GBM PDX mouse model.
