For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I045091 |
| CAS Number | 2567686-02-4 |
| Synonyms | (2R)-7-chloro-2-[4-(3-methoxyazetidin-1-yl)cyclohexyl]-2,4-dimethyl-N-[(6-methyl-4-methylsulfanyl-2-oxo-1H-pyridin-3-yl)methyl]-1,3-benzodioxole-5-carboxamide |
| Molecular Formula | C28H36ClN3O5S |
| Purity | ≥95% |
| InChI | InChI=1S/C28H36ClN3O5S/c1-15-10-23(38-5)21(27(34)31-15)12-30-26(33)20-11-22(29)25-24(16(20)2)36-28(3,37-25)17-6-8-18(9-7-17)32-13-19(14-32)35-4/h10-11,17-19H,6-9,12-14H2,1-5H3,(H,30,33)(H,31,34)/t17?,18?,28-/m1/s1 |
| InChIKey | CAAWBLRXQXMGHV-WOLMIXIISA-N |
| SMILES | CC1=CC(=C(C(=O)N1)CNC(=O)C2=CC(=C3C(=C2C)OC(O3)(C)C4CCC(CC4)N5CC(C5)OC)Cl)SC |
| Reference | [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. [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. [5]. Rentian Wu, et al. Abstract 2126: Therapeutic potential of CPI-0209. Cancer Res 1 July 2021; 81 (13_Supplement): 2126. |
