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Igermetostat

Chemical Structure : Igermetostat

CAS No.: 2409538-60-7

Igermetostat (XNW-5004, XNW5004)

Catalog No.: PC-23098Not For Human Use, Lab Use Only.

Igermetostat (XNW5004) is a potent, selective EZH2 inhibitor which potently inhibits both wild type and mutant EZH2.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Igermetostat (XNW5004) is a potent, selective EZH2 inhibitor which potently inhibits both wild type and mutant EZH2.
XNW5004 significantly suppresses level of H3K27Me3, arrests cell cycle in G1/S phase and promotes apoptosis in tumor.
XNW5004 exhibits strong antitumor activity in EZH2-mutant lymphoma xenograft models, such as Karpas422 (Y641N), Pfeiffer (A677G) and SU-DHL-10 (Y641F).
XNW5004 exhibits dose-dependent efficacy in solid tumor models such as G401 (SMARCB1 deficient) and COV434 (SMARCA2/SMARCA4 deficient) cancer cell lines and xenografts.

Physicochemical Properties

M.Wt 550.74
Formula C32H46N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-2-methyl-5-[[trans-3-(1-piperidinyl)cyclobutyl]oxy]benzamide

References

1. Yonghan Hu, et al. Cancer Res (2023) 83 (7_Supplement): 3089.

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