pkmyt1

Lunresertib (RP-6306) is a potent, selective, and orally active PKMYT1 inhibitor with an IC50 of 14 nM. Lunresertib (RP-6306) inhibits the growth of CCNE1-amplified tumor cells in several preclinical xenograft models.

PKMYT1-IN-3 (compound 8ma) is a potent, selective inhibitor of PKMYT1, demonstrating an IC50 of 16.5 nM and exhibiting antitumor activity.

PKMYT1-IN-6 (compound 98) is an inhibitor of PKMYT1, exhibiting an IC50 of less than 50nM.

PKMYT1-IN-4 (compound 27) functions as a PKMYT1 inhibitor with an IC50 value under 50 nM.

PKMYT1-IN-8 (Compound 137) is an inhibitor of PKMYT1, with an IC50 value of 9 nM. It also inhibits EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2, exhibiting IC50 values of 1.79, 3.17, 4.29, 6.32, 6.83, 8.10, and 10.9 μM, respectively. Additionally, PKMYT1-IN-8 suppresses the proliferation of cancer cells OVCAR3 with a GI50 of 2.02 μM.

WEE1 PKMYT1-IN-1 (compound 75) is an effective and orally bioavailable inhibitor of WEE1 and PKMYT1. It demonstrates antiproliferative activity.

PKMYT1-IN-1 (Compound 1), a potent inhibitor of the membrane-associated tyrosine and threonine kinase (PKMYT1), exhibits an IC 50 of 8.8 nM. This compound effectively inhibits the proliferation of the tumor cell line HCC1569, with an IC 50 of 42 nM [1].

PKMYT1-IN-2 (compound 2) serves as a powerful inhibitor of PKMYT1, exhibiting an IC 50 of 5.7 nM. Additionally, it effectively suppresses the proliferation of HCC1569 cells with an IC 50 of 22 nM [1].

GSK-1520489A is an active PKMYT1 inhibitor.