EZM0414

• Description :

  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].

• CAS Number :

  [2411748-50-8]

• UNSPSC :

  12352005

• Target :

  Histone Methyltransferase

• Type :

  Reference compound

• Related Pathways :

  Epigenetics

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/ezm0414.html

• Purity :

  99.11

• Solubility :

  DMSO : 120 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles :

  FC1=C2C(NC(C(N[C@H]3C[C@](N4CCN(CC4)C(C)=O)([H])CCC3)=O)=C2)=C(C=C1)C

• Molecular Formula :

  C22H29FN4O2

• Molecular Weight :

  400.49

• References & Citations :

  [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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  4°C (Powder, sealed storage, away from moisture and light)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 1

• Isoform :

  SETD2/KMT3A

• Citation 01 :

  Int J Biol Macromol. 2024 Oct 28:136767.|Sci Rep. 2024 Jun 3;14 (1) :12728.|Cell Rep. 2025 Jan 15;44 (1) :115219.|Cell Stem Cell. 2023 Apr 6;30 (4) :450-459.e9.|Nat Chem Biol. 2023 Sep;19 (9) :1105-1115.|Research Square Preprint. 2023 May 26.