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Akt inhibitor

Also known as GDC-0068, is a strong ATP-competitive pan-AKT inhibitor. It was initially derived during the screening and optimization process of a series of 6,7-dihydro-5H-cyclopenta[d]pyrimidine compounds. Ipatasertib shows a powerful inhibition of all protein kinase B (Akt) isoforms but a weak suppression towards other members of the protein kinase family.<br>

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Akt inhibitor

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  1. Akt inhibitor https://www.creative-biolabs.com/adc

  2. Ipatasertib • Also known as GDC-0068, is a strong ATP-competitive pan-AKT inhibitor. It was initially derived during the screening and optimization process of a series of 6,7-dihydro-5H-cyclopenta[d]pyrimidine compounds. Ipatasertib shows a powerful inhibition of all protein kinase B (Akt) isoforms but a weak suppression towards other members of the protein kinase family.

  3. X-ray single-crystal structure of Ipatasertib mono-HCl (Org. Process Res. Dev., 2014).

  4. CONTENTS 01 Ipatasertib mechanism of action 02 Ipatasertib-based ADCs

  5. ipatasertib mechanism of action • Akt, an abbreviated name for protein kinase B (PKB), is a serine/threonine-specific protein kinase that plays a key role in the PI3K/Akt pathway as a regulator for a number of biological processes, including glucose metabolism, cell differentiation, and transcription. The mechanisms of the Akt pathway in tumorigenesis are complicated. • The activated Akt contributes to tumor anti-apoptotic activities through the inhibition of mitochondrial cytochrome c release or the regulation of other downstream effectors, including Bcl-2 family proteins, FOXO transcription factors and MDM2.Akt activation regulates cell cycle progression through the inhibition of glycogen synthase kinase 3beta, preventing the action of p21WAF1 and p27Kip1 via phosphorylation of AKT/mTOR kinases.

  6. The PI3K/Akt/mTOR signaling pathway (Left, Infect Agents Cancer, 2013) and X-ray structure of Ipatasertib bound to Akt1 (Right, J Med Chem, 2012), a process that inhibits Akt activity and down-regulates the subsequent signaling pathways in caner.

  7. Ipatasertib-based ADCs • ADCs are composed of cytotoxic agents conjugated to monoclonal antibodies that target antigens differentially overexpressed on tumor cells. The strong cytotoxic agents are expected to induce cell death after being internalized into the tumor cell and released by various mechanisms • Studies have proven that ipatasertib was highly efficacious in a variety of tumor models and cancer cell lines. Based on its potent cytotoxicity, ipatasertib is considered to be a promising cytotoxic payload for the construction of ADCs.

  8. Creative Biolabs also provides other various services regarding ADC development. Please feel free to contact us for more information and a detailed quote.

  9. GET IN TOUCH CONTACT US Established in 2004, Creative Biolabs is highly specialized in advanced antibody biochemistry and engineering. With more than a decade of exploration and expansion, our current research and service capacity covers the entire new drug discovery and development pipeline, ranging from early discovery, preclinical evaluations, cGMP manufacturing, to clinical trails. Creative Biolabs 45-1 Ramsey Road, Shirley, NY 11967, USA Email: marketing@creative-biolabs.com

  10. THANKS

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