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

EEDi-5285 

Cat. No.: HY-136977 Purity: 98.66%
COA 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

CAS No. : 2488952-40-3

Size Price Stock Quantity
5 mg USD 580 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1900 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

CAS No.
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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (260.67 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0854 mL 10.4269 mL 20.8538 mL
5 mM 0.4171 mL 2.0854 mL 4.1708 mL
10 mM 0.2085 mL 1.0427 mL 2.0854 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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