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PRMT5/EGFR-IN-1

PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors[1].

Product Specifications

UNSPSC

12352005

Target

EGFR; Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/prmt5-egfr-in-1.html

Solubility

10 mM in DMSO

Smiles

COC1=CC(C2NCCC3=C2NC4=CC=CC=C43)=CC=C1OCC5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5

Molecular Formula

C27H22F6N2O2

Molecular Weight

520.47

References & Citations

[1]Zhang J, et al. Synthesis and biological evaluation of 1-phenyl-tetrahydro-β-carboline-based first dual PRMT5/EGFR inhibitors as potential anticancer agents. Eur J Med Chem. 2024 Mar 18;269:116341.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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