| Identification | Back Directory | [Name]
Tulmimetostat | [CAS]
2567686-02-4 | [Synonyms]
Tulmimetostat
Tulmimetostat (CPI-0209)
1,3-Benzodioxole-5-carboxamide, 7-chloro-N-[[1,2-dihydro-6-methyl-4-(methylthio)-2-oxo-3-pyridinyl]methyl]-2-[trans-4-(3-methoxy-1-azetidinyl)cyclohexyl]-2,4-dimethyl-, (2R)- | [Molecular Formula]
C28H36ClN3O5S | [MOL File]
2567686-02-4.mol | [Molecular Weight]
562.12 |
| Chemical Properties | Back Directory | [Boiling point ]
653.6±55.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
10.89±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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].
| [IC 50]
EZH2; EZH1 | [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. DOI:10.1016/j.blre.2022.100988
[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. DOI:10.4155/fmc-2020-0072
[5] Rentian Wu, et al. Abstract 2126: Therapeutic potential of CPI-0209. Cancer Res 1 July 2021; 81 (13_Supplement): 2126. |
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