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EZM0414
$850 – $6,950
Products Details
Product 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].
Web ID
– HY-144858
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture and light)
Shipping
– Room Temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C22H29FN4O2
References
– [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.
CAS Number
– 2411748-50-8
Molecular Weight
– 400.49
Compound Purity
– 99.45
SMILES
– FC1=C2C(NC(C(N[C@H]3C[C@](N4CCN(CC4)C(C)=O)([H])CCC3)=O)=C2)=C(C=C1)C
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– DMSO : 120 mg/mL (ultrasonic;warming;heat to 60°C)|H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Histone Methyltransferase
Isoform
– SETD2/KMT3A
Pathway
– Epigenetics
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
