Bemcentinib is a selective small molecule inhibitor of Axl kinase, which showed activity to blocks tumor spread and prolongs survival in models of metastatic breast cancer. The receptor tyrosine kinase Axl may play an important role in cancer progression, invasion, metastasis, drug resistance, and patient mortality. R428 inhibits Axl with low nanomolar activity and blocked Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. Pharmacologic investigations revealed favorable exposure after oral administration such that R428-treated tumors displayed a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. In support of an earlier study, R428 inhibited angiogenesis in corneal micropocket and tumor models. R428 administration reduced metastatic burden and extended survival in MDA-MB-231 intracardiac and 4T1 orthotopic (median survival, >80 days compared with 52 days; P < 0.05) mouse models of breast cancer metastasis. Additionally, R428 synergized with cisplatin to enhance suppression of liver micrometastasis. Our results show that Axl signaling regulates breast cancer metastasis at multiple levels in tumor cells and tumor stromal cells and that selective Axl blockade confers therapeutic value in prolonging survival of animals bearing metastatic tumors.https://www.bocsci.com/bemcentinib-cas-1037624-75-1-item-456603.html

BOC Sciences is a brand of BOCSCI Inc. We leverage our wide spectrum of business in the fields of development, manufacturing, marketing, and distribution to help you make best-informed decisions tailored to your evolving needs for premium chemicals. Our complete suite of CRO services spans the entire molecule development pipeline including contract research for target identification, building blocks, compound synthesis, biochemical and cellular analysis, preclinical animal tests, and clinical studies.

Products:

BOC Sciences provides a wide range of research chemicals and biochemicals including inhibitors, building blocks, GMP Products, impurities and metabolites, APIs for Veterinary, Natural Compounds, ADCs, Stem Cell Molecule and chiral compounds.

Over eight years of successful operation in the pharmaceutical industry has enabled us to possess a full-bodied array of building blocks in numerous pack sizes. BOC Sciences is constantly seeking to expand our product lines by incorporating additional potential drug like molecules.



Services:

BOC Sciences provides a wide range of services to support the pharmaceutical industry through all stages of drug discovery including Custom Synthesis of those chemicals that are not in stock, Isotope Labeling Service, Chiral Synthesis and Resolution, Bioconjugation, PEGylation services, analytical services.

Our capacity to provide pharmaceutical discovery services across the entire spectrum of the drug discovery process has assisted many of our esteemed clients in reaching their R&D goals. We are actively improving our capabilities and capacity through new expansions in BOC Sciences’s global business.



Manufacturing services:

-> Manufacture of raw materials, registered GMP starting materials and intermediates from small scale (1kg) to commercial quantities (1000 kg);
-> Production of APIs to support drug candidate selections;
-> GLP toxicology studies and clinical studies;
-> Development and optimization of environmentally friendly process;
-> Competitive quality and price comparable to commodity chemical suppliers


Our clients



As a leading provider of building blocks, synthetic intermediates, and custom synthesis, BOC Sciences is committed to supplying cost-effective products and services, which are being utilized by our customers worldwide in molecule discovery on a daily basis to promote innovations in various industries.