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MedChemExpressModel Tulmimetostat -2567686-02-4

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Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor that targets and inhibits the EZH2 enzyme.Tulmimetostat has antitumor activity and is used in a variety of solid tumor studies[1][2][3][4].
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Tulmimetostat

MCE China:Tulmimetostat

Brand:MedChemExpress (MCE)

Cat. No.HY-145602

CAS:2567686-02-4

Synonyms:CPI-0209

Purity:98.75%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

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

Description:Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor that targets and inhibits the EZH2 enzyme.Tulmimetostat has antitumor activity and is used in a variety of solid tumor studies.

In Vitro:Tulmimetostat is sensitive to AR-dependent prostate cancer cell lines (including LNCaP, 22Rv1, and VCaP) and AR-dependent cell line-derived transplanted tumor (CDX) and patient-derived transplanted tumor (PDX) models[5].

In Vivo:Tulmimetostat has a synergistic effect on Enzalutamide (HY-70002) in prostate cancer CDX and PDX models, overcoming anti-androgen resistance induced by AR changes and enhancing tumor growth inhibition[5].

IC50 & Target:EZH2 EZH1

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References:

[1]. WHO Drug Information, Vol. 35, No. 4, 2021. Geneva: World Health Organization; 2022.

[2]. Drescher C, et al. EZH2/EZH1 inhibitor tulmimetostat (CPI-0209): preliminary phase II results and first biomarker findings in patients with arid1a-mutant ovarian clear cell or endometrial carcinomas (OCCC/EC) 2023.

[3]. Morschhauser F, et al. Taking the EZ way: Targeting enhancer of zeste homolog 2 in B-cell lymphomas. Blood Rev. 2022 Nov;56:100988.  [Content Brief]

[4]. Qiu J, et al. The complex role of EZH2 in the tumor microenvironment: opportunities and challenges for immunotherapy combinations. Future Med Chem. 2020 Aug;12(15):1415-1430.  [Content Brief]

[5]. Rentian Wu, et al. Abstract 2126: Therapeutic potential of CPI-0209. Cancer Res 1 July 2021; 81 (13_Supplement): 2126.

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。