PR-104A is a Hypoxia-Selective DNA Cross-Linking Agent and Cytotoxin
PR-104, like TH-302, is a prodrug of nitrogen mustard that has shown some degree of efficacy in adult patients with relapsed/refractory acute myeloid leukemia (AML). PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Therefore, this compound...
BSJ-4-116 is a Highly Potent and Selective PROTAC Based CDK12 Degrader
CDKs are serine/threonine protein kinases. They play major roles in regulating many different aspects of mammalian cellular function, most notably cell cycle and transcription. CDK12 is an emerging therapeutic target due to its role in regulating the transcription of DNA-damage response (DDR) genes. For example, ovarian and triple-negative breast...
PF-06465469 is a Covalent Inhibitor of ITK
Peripheral T-cell lymphomas (PTCL) accounted for about 5% of all non-Hodgkin’s lymphomas. Standard first line treatment is with combination chemotherapy but the majority of patients relapse. There is no standard treatment for refractory or relapsed disease. However, histone deacetylase inhibitors, panabinostat and romidepsin, and pralatrexate are licensed for use...