RGB-286638 / Agennix - LARVOL DELTA

An Overview of CDK Enzyme Inhibitors in Cancer Therapy. (PubMed, Curr Cancer Drug Targets) - "We have mentioned first-generation pan-CDKIs, flavopiridol and roscovitine, as well as second-generation CDKIs, dinaciclib, P276-00, AT7519, TG02, roniciclib, and RGB-286638, based on their research phases, clinical trials, and cancer targeting. CDKIs are CDK4/6, CDK7, CDK9, and CDK12 inhibitors. Finally, we have looked into the efficacy of CDK inhibitors and PD1/PDL1 antibodies when used together, which could lead to the development of a viable cancer treatment strategy."

Journal • Oncology • CDK4 • CDK7 • CDK9

Preclinical assessment of synergistic efficacy of MELK and CDK inhibitors in adrenocortical cancer. (PubMed, J Exp Clin Cancer Res) - "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."

Journal • Preclinical • Adrenal Cortex Carcinoma • Genito-urinary Cancer • Oncology • Solid Tumor • CASP3 • CASP7 • CDK1 • CTNNB1 • MELK • VIM

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."

Journal • Review • Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • CDK12 • CDK7 • CDK9

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."

Journal • Preclinical • Glioblastoma • Oncology • Solid Tumor

[VIRTUAL] Synergistic Combination of Maternal Embryonic Leucine Zipper Kinase (MELK) Inhibitor and Multi-cdk Inhibitor Targets -catenin in Adrenocortical Carcinoma via a Novel Pathway (SSO 2020) - "To investigate the effects on cancer invasiveness, we found a lower expression of epithelial-mesenchymal-transition (EMT) markers such as fibronectin and SNAIL2, compare to the single-drug groups. In summary, the combination of OTS167 and RGB286638 is synergistically effective in ACC via AXIN2/GSK3-/FOXM1/-catenin and the reduction of EMT markers."

Genito-urinary Cancer • Oncology • Solid Tumor • CDK1 • CDKN1A • CDKN2C