Our preclinical study revealed a novel synergistic combination of OTS167 and RGB-286638 in ACC that effectively targets multiple molecules associated with ACC aggressiveness. A phase Ib/II clinical trial in patients with advanced ACC is therefore warranted.

2 years ago

Preclinical • Journal

CTNNB1 (Catenin (cadherin-associated protein), beta 1) • CASP3 (Caspase 3) • VIM (Vimentin) • MELK (Maternal Embryonic Leucine Zipper Kinase) • CASP7 (Caspase 7) • CDK1 (Cyclin-dependent kinase 1)

OTS167 • RGB-286638

over3years

CDK inhibitors in cancer therapy, an overview of recent development. (PubMed, Am J Cancer Res)

We reviewed first-generation pan-CDKIs Flavopiridol and Roscovitine, and second-generation CDKIs Dinaciclib, P276-00, AT7519, TG02, Roniciclib, RGB-286638 by focusing on their developing stages, clinical trials and targeting cancers. These CDKIs include CDK4/6, CDK7, CDK9, and CDK12/13 inhibitors. Finally, the efficacy and discrepancy of combination therapy with CDK inhibitors and PD1/PDL1 antibodies were analyzed, which might give insights into the development of promising strategy for cancer treatment.

over 3 years ago

Review • Journal

CDK12 (Cyclin dependent kinase 12) • CDK7 (Cyclin Dependent Kinase 7) • CDK9 (Cyclin Dependent Kinase 9)

HR positive

alvocidib (DSP-2033) • dinaciclib (MK-7965) • zotiraciclib (TG02) • AT7519 • RGB-286638 • riviciclib (P27600) • roniciclib (BAY1000394)

almost4years

Data-driven prioritization and preclinical evaluation of therapeutic targets in glioblastoma. (PubMed, Neurooncol Adv)

The MAPK9 inhibitor RGB-286638 showed promising in vitro results. Furthermore, in vivo target engagement studies and combination therapies with this compound warrant further exploration.

almost 4 years ago

Preclinical • Journal

EGFR (Epidermal growth factor receptor) • RRM2 (Ribonucleotide Reductase Regulatory Subunit M2)

RGB-286638