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EEDi-5273

EEDi-5273 (APG-5918) is a potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 of 0.2 nM. EEDi-5273 can inhibit the polycomb repressive complex 2 (PRC2) activity and block trimethylation of histone H3 lysine 27. EEDi-5273 can be used for the research of cancer, such as ovarian cancer[1].

Product Specifications

CAS Number

[2585648-55-9]

Product Name Alternative

APG-5918

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/eedi-5273.html

Concentration

10mM

Purity

99.09

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

CC(N1CC2=CC(C(F)(F)F)=NC=C2C3=CN=C(N4C=NC(C1=O)=C34)NCC5=C6CCOC6=CC=C5F)C

Molecular Formula

C26H22F4N6O2

Molecular Weight

526.49

References & Citations

[1]Rej RK, et al. Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression. J Med Chem. 2021 Oct 14;64 (19) :14540-14556.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 1

Available Sizes

Curated Selection

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