Tulmimetostat  (Synonyms: CPI-0209)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

562.12

C₂₈H₃₆ClN₃O₅S

2567686-02-4

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Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.