EZM0414

Product Name: EZM0414
CAS No.: 2411748-50-8
Chemical Name: EZM0414
Synonyms: EZM0414
CBNumber: CB110828961
Molecular Formula: C22H29FN4O2
Formula Weight: 400.5
MOL File: 2411748-50-8.mol

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EZM0414 Property

storage temp.: Store at -20°C
form: Solid
color: Off-white to light yellow
InChIKey: PGNLXEBQMQHFNK-XGTFWIOGNA-N
SMILES: FC1C=CC(C)=C2NC(C(=O)N[C@@H]3CCC[C@H](N4CCN(C(=O)C)CC4)C3)=CC=12 |&1:12,16,r|

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Hazard and Precautionary Statements (GHS)

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EZM0414 Chemical Properties,Usage,Production

Uses

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].

in vivo

EZM0414 (15 and 30 mg/kg, p.o., BID, daily, ) inhibits tumor growth in NOD SCID mouse xenograft model implanted with human KMS-11 cells, and is well-tolerated^[3].
EZM0414 (50 mg/kg, p.o.) shows almost 100% oral bioavailability in rats and mice, t_1/2 of 1.8 h (mice)and 3.8 h (rats)^[3].

IC 50

SETD2/KMT3A

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. DOI:10.1021/acsmedchemlett.2c00167

EZM0414 Preparation Products And Raw materials

Raw materials

Preparation Products

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EZM0414 Suppliers

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