GDC-0994 - CAS 1453848-26-4
Catalog number: 1453848-26-4
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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GDC-0994, also known as RG7842, is an orally available inhibitor of extracellular signal-regulated kinase (ERK), with potential antineoplastic activity. Upon oral administration, GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways. This prevents ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.
Solid powder
GDC-0994; GDC0994; GDC 0994; RG7842; RG-7842; RG 7842.
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1.Study of the osteogenesis effect of icariside II and icaritin on canine bone marrow mesenchymal stem cells.
Luo G;Xu B;Wang W;Wu Y;Li M J Bone Miner Metab. 2017 Dec 20. doi: 10.1007/s00774-017-0889-5. [Epub ahead of print]
This study aimed to identify the osteogenesis effect of icariside II (ICSII) and icaritin (ICT) in vitro. Bone marrow mesenchymal stem cells (BMSCs) were treated with ICSII and ICT in order to detect the proliferation and differentiation of BMSCs, the expression of the osteogenesis-related proteins with or without osteogenic medium (OM) and genes, Runt-related transcription factor 2 (Runx-2), osteocalcin (OCN), osteopontin (OPN), osterix, and basic fibroblast growth factor (bFGF), and the phosphorylation levels of mitogen-activated protein kinase (MAPK). We found that the optical density increased and alkaline phosphatase decreased after the BMSCs were treated with different concentrations of ICSII; however, ICT showed an opposing effect. The formation of calcium nodules was observed after the BMSCs were treated with ICSII and ICT. The expression level of osteogenesis-related proteins was enhanced following treatment with both ICSII or ICT, while the expression level of the osteogenesis-related genes Runx-2, OCN, OPN, osterix, and bFGF significantly increased with ICSII treatment (P < 0.05), and only Runx-2 and bFGF significantly increased (P < 0.01) with ICT. The expression of osteogenic differentiation-related proteins (except OPN) following treatment with ICSII + OM or ICT + OM was not notably increased.
2.Specificity of Phosphorylation Responses to Mitogen Activated Protein (MAP) Kinase Pathway Inhibitors in Melanoma Cells.
Basken J;Stuart SA;Kavran AJ;Lee T;Ebmeier CC;Old WM;Ahn NG Mol Cell Proteomics. 2018 Apr;17(4):550-564. doi: 10.1074/mcp.RA117.000335. Epub 2017 Dec 18.
The BRAF-MKK1/2-ERK1/2 pathway is constitutively activated in response to oncogenic mutations of BRAF in many cancer types, including melanoma. Although small molecules that inhibit oncogenic BRAF and MAP kinase kinase (MKK)1/2 have been successful in clinical settings, resistance invariably develops. High affinity inhibitors of ERK1/2 have been shown in preclinical studies to bypass the resistance of melanoma and colon cancer cells to BRAF and MKK1/2 inhibitors, and are thus promising additions to current treatment protocols. But still unknown is how molecular responses to ERK1/2 inhibitors compare with inhibitors currently in clinical use. Here, we employ quantitative phosphoproteomics to evaluate changes in phosphorylation in response to the ERK inhibitors, SCH772984 and GDC0994, and compare these to the clinically used MKK1/2 inhibitor, trametinib. Combined with previous studies measuring phosphoproteomic responses to the MKK1/2 inhibitor, selumetinib, and the BRAF inhibitor, vemurafenib, the outcomes reveal key insights into pathway organization, phosphorylation specificity and off-target effects of these inhibitors. The results demonstrate linearity in signaling from BRAF to MKK1/2 and from MKK1/2 to ERK1/2.
3.Clinical responses to ERK inhibition in
Kirouac DC;Schaefer G;Chan J;Merchant M;Orr C;Huang SA;Moffat J;Liu L;Gadkar K;Ramanujan S NPJ Syst Biol Appl. 2017 Jun 2;3:14. doi: 10.1038/s41540-017-0016-1. eCollection 2017.
Approximately 10% of colorectal cancers harbor ;BRAF;V600E; mutations, which constitutively activate the MAPK signaling pathway. We sought to determine whether ERK inhibitor (GDC-0994)-containing regimens may be of clinical benefit to these patients based on data from in vitro (cell line) and in vivo (cell- and patient-derived xenograft) studies of cetuximab (EGFR), vemurafenib (BRAF), cobimetinib (MEK), and GDC-0994 (ERK) combinations. Preclinical data was used to develop a mechanism-based computational model linking cell surface receptor (EGFR) activation, the MAPK signaling pathway, and tumor growth. Clinical predictions of anti-tumor activity were enabled by the use of tumor response data from three Phase 1 clinical trials testing combinations of EGFR, BRAF, and MEK inhibitors. Simulated responses to GDC-0994 monotherapy (overall response rate = 17%) accurately predicted results from a Phase 1 clinical trial regarding the number of responding patients (2/18) and the distribution of tumor size changes ("waterfall plot"). Prospective simulations were then used to evaluate potential drug combinations and predictive biomarkers for increasing responsiveness to MEK/ERK inhibitors in these patients.
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CAS 1453848-26-4 GDC-0994

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