EZM0414 (TFA)

EZM0414 (SETD2-IN-1) TFA is the TFA salt form of EZM0414 (HY-144858) . EZM0414 TFA is a potent, selective, orally active inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay) . EZM0414 TFA can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma[1].

Product Specifications

CAS Number

[2411759-92-5]

Product Name Alternative

SETD2-IN-1 (TFA)

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-tfa.html

Purity

97.20

Solubility

DMSO : 200 mg/mL (ultrasonic) |H2O : 6.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C(N1)=CC2=C1C(C)=CC=C2F)N[C@H]3C[C@@H](N4CCN(C(C)=O)CC4)CCC3.O=C(O)C(F)(F)F

Molecular Formula

C24H30F4N4O4

Molecular Weight

514.51

References & Citations

[1]John Lampe, et al. Substituted indoles and methods of use thereof. WO2020037079A1.|[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