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EZM0414

CAT: 0804-HY-144858-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-144858-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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.

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