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EZM0414 (TFA)

CAT: 0804-HY-136328-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-136328-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
EZM0414 (SETD2-IN-1) TFA is the TFA salt form of EZM0414. 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].
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
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
SETD2/KMT3A
Citation 01
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.|Int J Biol Macromol. 2024 Oct 28:136767.|Sci Rep. 2024 Jun 3;14 (1) :12728.

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