Catalog No.: PC-73399Not For Human Use, Lab Use Only.
RP-6306 (Lunresertib, RP6306) is a first-in-class, potent and selective, orally available inhibitor of PKMYT1 with IC50 of 2.4 nM, displays less potency (>35-fold) against EphA1-2, and EphB2-4, and Wee1.
RP-6306 (Lunresertib, RP6306) is a first-in-class, potent and selective, orally available inhibitor of PKMYT1 with IC50 of 2.4 nM, displays less potency (>35-fold) against EphA1-2, and EphB2-4, and Wee1.
RP-6306 inhibits the phosphorylation of CDK1 Thr14 in vivo in tumor tissue and inhibits CCNE1-amplified tumor cell growth in several preclinical xenograft models.
PKMYT1 is an important regulator of CDK1 phosphorylation and is a compelling therapeutic target for the treatment of certain types of DNA damage response cancers due to its established synthetic lethal relationship with CCNE1 amplification.
PKMYT1 is a member of the Wee-kinase family protein kinases, PKMYT1 is involved in G2/M checkpoint regulation of the cell cycle.
