For research use only. Not for therapeutic Use.
EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma[1].
EZM0414 inhibits proliferation of a panel of MM and DLBCL cell lines, with IC50s of 0.24 μM for t(4;14) cell, 0.023 μM- >10 μM for DLBCL cell lines[2].
EZM0414 (15 and 30 mg/kg, p.o., BID, daily, ) inhibits tumor growth in NOD SCID mouse xenograft model implanted with human KMS-11 cells, and is well-tolerated[3].
EZM0414 (50 mg/kg, p.o.) shows almost 100% oral bioavailability in rats and mice, t1/2 of 1.8 h (mice)and 3.8 h (rats)[3].
| Catalog Number | I044038 |
| CAS Number | 2411748-50-8 |
| Synonyms | N-[(1R,3S)-3-(4-acetylpiperazin-1-yl)cyclohexyl]-7-fluoro-4-methyl-1H-indole-2-carboxamide |
| Molecular Formula | C22H29FN4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H29FN4O2/c1-14-6-7-19(23)21-18(14)13-20(25-21)22(29)24-16-4-3-5-17(12-16)27-10-8-26(9-11-27)15(2)28/h6-7,13,16-17,25H,3-5,8-12H2,1-2H3,(H,24,29)/t16-,17+/m1/s1 |
| InChIKey | ZGFOQXUCQAEQHH-SJORKVTESA-N |
| SMILES | CC1=C2C=C(NC2=C(C=C1)F)C(=O)NC3CCCC(C3)N4CCN(CC4)C(=O)C |
| Reference | [1]. Jennifer Totman, et al. Pharmacologic Inhibition of the Histone Methyltransferase SETD2 with EZM0414 As a Novel Therapeutic Strategy in Relapsed or Refractory Multiple Myeloma and Diffuse Large B-cell Lymphoma. [2]. Jennifer Totman, et al. Pharmacologic Inhibition of the Histone Methyltransferase SETD2 with EZM0414 As a Novel Therapeutic Strategy in Relapsed or Refractory Multiple Myeloma and Diffuse Large B-Cell Lymphoma. Blood. Volume 138, Supplement 1, 23 November 2021, Page 1142. [3]. Alford JS, et al. Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies. ACS Med Chem Lett. 2022 Jun 7;13(7):1137-1143. |
