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

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

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5 mg USD 480 In-stock
10 mg USD 720 In-stock
25 mg USD 1250 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

EEDi-5285 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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]
Cellular Effect
Cell Line Type Value Description References
KARPAS-422 IC50
0.5 nM
Compound: 28; EEDi-5285
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
[PMID: 32580550]
Pfeiffer IC50
0.02 nM
Compound: 28; EEDi-5285
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
[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.

EEDi-5285 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the 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.

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.98%

SDS (251 KB)

COA (253 KB) HNMR (284 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

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
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EEDi-5285 Related Classifications

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.

Keywords:

EEDi-52852488952-40-3EEDi5285EEDi 5285Histone MethyltransferaseEEDanti-cancerorallyembryonicectodermdevelopmentH3K27me3Inhibitorinhibitorinhibit

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