EEDi-5285
Based on 1 publication(s) in Google Scholar
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.
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- Pureté : 99.87%
- CAS No.: 2488952-40-3
- Formule: C24H22FN5O3S
- Masse moléculaire:479.53
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) EEDi-5285
MoreVoir tous les produits spécifiques à Isoform Histone Methyltransferase
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Activité biologique
Description
IC50 & Target
IC50: 0.2 nM (Embryonic ectoderm development (EED))[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KARPAS-422 | IC50 |
0.5 nM
Compound: 28; EEDi-5285
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Growth inhibition of human KARPAS422 cells incubated for 7 days by WST8 assay
Growth inhibition of human KARPAS422 cells incubated for 7 days by WST8 assay
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[PMID: 32580550] |
| Pfeiffer | IC50 |
0.02 nM
Compound: 28; EEDi-5285
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Growth inhibition of human Pfeiffer cells incubated for 7 days by WST8 assay
Growth inhibition of human Pfeiffer cells incubated for 7 days by WST8 assay
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[PMID: 32580550] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice injected with KARPAS422 cells[1]
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Dosage:50 mg/kg, 100 mg/kg
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Administration:Oral gavage; daily; for 28 days
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Result:Showed highly efficacious and capable of achieving complete and long-lasting tumor regression in the KARPAS422 xenograft model in mice with oral administration.
Chemical Information
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CAS No. 2488952-40-3
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Appearance Solid
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Masse moléculaire 479.53
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Formule C24H22FN5O3S
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Color White to off-white
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SMILES
CS(C1=C2C(C3=CC=C(C4CC4)N=C3)=CN=C(NCC5=C(F)C=CC6=C5CCO6)N2C=N1)(=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Dual EZH1/2 inhibition enhances DNMT inhibitor efficacy in colon cancer through targeting H3K27me1. [Abstract]2025 Sep 18:2025.09.16.676613. PMID: 41000734
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (260.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0854 mL | 10.4269 mL | 20.8538 mL | 52.1344 mL |
| 5 mM | 0.4171 mL | 2.0854 mL | 4.1708 mL | 10.4269 mL | |
| 10 mM | 0.2085 mL | 1.0427 mL | 2.0854 mL | 5.2134 mL | |
| 15 mM | 0.1390 mL | 0.6951 mL | 1.3903 mL | 3.4756 mL | |
| 20 mM | 0.1043 mL | 0.5213 mL | 1.0427 mL | 2.6067 mL | |
| 25 mM | 0.0834 mL | 0.4171 mL | 0.8342 mL | 2.0854 mL | |
| 30 mM | 0.0695 mL | 0.3476 mL | 0.6951 mL | 1.7378 mL | |
| 40 mM | 0.0521 mL | 0.2607 mL | 0.5213 mL | 1.3034 mL | |
| 50 mM | 0.0417 mL | 0.2085 mL | 0.4171 mL | 1.0427 mL | |
| 60 mM | 0.0348 mL | 0.1738 mL | 0.3476 mL | 0.8689 mL | |
| 80 mM | 0.0261 mL | 0.1303 mL | 0.2607 mL | 0.6517 mL | |
| 100 mM | 0.0209 mL | 0.1043 mL | 0.2085 mL | 0.5213 mL |
EEDi-5285 Related Classifications
HY-136977 Related Classifications
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