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MedChemExpressModel Fulzerasib - 2641747-54-6

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Fulzerasib (GFH925) is an irreversible KRAS G12C inhibitor, has a synergistic anti-cancer effect with cetuximab (HY-P9905).[1][2].
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Fulzerasib

MCE China:Fulzerasib

Brand:MedChemExpress (MCE)

Cat. No.HY-152848

CAS:2641747-54-6

Synonyms:IBI351; GFH925

Purity:99.60%

Storage:Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Fulzerasib (GFH925) is an irreversible KRAS G12C inhibitor, has a synergistic anti-cancer effect with cetuximab (HY-P9905)..

In Vitro:Fulzerasib covalently inhibits GDP/GTP nucleotide exchange on KRAS G12C (IC50: 29 nM), locking KRAS in its inactive GDP-bound state (RAS-GTP IC50: 74 nM), thereby blocking the KRAS signaling pathway (pERK IC50: 37 nM)[1]. Fulzerasib inhibits the growth of tumor cell lines carrying the KRAS G12C mutation (IC50: 2-20 nM)[1].

In Vivo:Fulzerasib shows strong anti-tumor activity in various models, including the pancreatic cancer cell line MIA Paca-2 CDX, human lung adenocarcinoma NCI-H358 CDX, patient-derived xenograft colon adenocarcinoma SW837 CDX, and lung cancer LU2529 PDX[1].

IC50 & Target:KRAS(G12C)

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Trending products:Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

References:

[1]. Rafael Rosell, et al. KRAS G12C-mutant driven non-small cell lung cancer (NSCLC). Crit Rev Oncol Hematol. 2024 Mar:195:104228.  [Content Brief]

[2]. Vanesa Gregorc, et al. KROCUS: A phase II study investigating the efficacy and safety of fulzerasib. Free access.June 05, 2024

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas;
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects;
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services;
•   It has a professional experimental center and strict quality control and verification system;
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products;
•   The biological activity of the products has been verified by the experiments of customers in various countries;
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers;
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world;
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。