Category: Hematological Malignancies

CM-272, a First-in-class, Reversible and Dual G9a/DNMTs Inhibitor

Therapy of hematological malignancies is undergoing a paradigm shift. It is away from the traditional chemotherapy towards the targeting of proteins driving the cancer phenotype. The novel therapeutic approach relies on the use of epigenetic drugs. It aims to reverse critical epigenetic events underlying human cancer pathogenesis, particularly abnormalities...

CC-223 is an Orally Bioavailable mTOR Kinase Inhibitor

mTOR is a serine/threonine kinase that regulates cell growth, metabolism, proliferation, and survival. mTORC1 is a master regulator of cell growth and metabolism. mTORC1 positively regulates cell growth and proliferation. mTORC2 regulates cytoskeletal organization. CC-223 is a potent mTOR kinase inhibitor with an IC50 of 0.016 μM. CC-223 is...

Alisertib is an Oral Active and Selective Aurora A Kinase Inhibitor

As we all know, Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor. Aurora kinases are essential mediators in cell mitosis. Amplification of these kinases can lead to the development of malignancy and may be associated with inferior survival. Alisertib is an oral aurora kinase inhibitor which...