1. Epigenetics
  2. Histone Methyltransferase
  3. EEDi-5285

EEDi-5285 

Cat. No.: HY-136977
Handling Instructions

EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.

For research use only. We do not sell to patients.

EEDi-5285 Chemical Structure

EEDi-5285 Chemical Structure

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Description

EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity[1].

IC50 & Target

IC50: 0.2 nM (Embryonic ectoderm development (EED))[1]

In Vitro

EEDi-5285 inhibits cell growth with IC50 values of 20 pM and 0.5 nM in the Pfeiffer and KARPAS422 lymphoma cell lines, respectively, carrying an EZH2 mutation[1].

In Vivo

EEDi-5285 (compound 28; 50-100 mg/kg; oral gavage; daily; for 28 days; SCID mice) treatment achieves complete and durable tumor regression in the KARPAS422 xenograft model in mice with oral administration[1].
A single 100 mg/kg oral administration of EEDi-5285 (compound 28) effectively reduces the level of H3K27me3 at 24 h in KARPAS422 tumor tissue in mice[1].
EEDi-5285 (compound 28) achieves a Cmax of 1.8 μM and an AUC of 6.0 h▪μg/ml with 10 mg/kg oral administration and has an oral bioavailability (F) of 75%. EEDi-5285 has a moderate volume of distribution of 1.4 L/kg and a terminal T1/2 of approximately 2 h[1].

Animal Model: SCID mice injected with KARPAS422 cells[1]
Dosage: 50 mg/kg, 100 mg/kg
Administration: Oral gavage; daily; for 28 days
Result: Showed highly efficacious and capable of achieving complete and long-lasting tumor regression in the KARPAS422 xenograft model in mice with oral administration.
Molecular Weight

479.53

Formula

C₂₄H₂₂FN₅O₃S

SMILES

CS(C1=C2C(C3=CC=C(C4CC4)N=C3)=CN=C(NCC5=C(F)C=CC6=C5CCO6)N2C=N1)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

EEDi-5285EEDi5285EEDi 5285Histone MethyltransferaseEEDanti-cancerorallyembryonicectodermdevelopmentH3K27me3Inhibitorinhibitorinhibit

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Product Name:
EEDi-5285
Cat. No.:
HY-136977
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