IF 17
PMID: 35840558 ↗EPZ-6438
Catalog No.: GC14062Purity:>99.00%Synonyms: E-7438,Tazemetostat
EPZ-6438 is a potent and bio-available inhibitor of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of lysine 27 of histone H3 (H3K27), that inhibits the activity of human PRC2-containing wild-type EZH2 with a value of inhibition constant Ki of 2.5 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1403254-99-8
10mM (in 1mL DMSO)In Stock
$56.00
1
5mgIn Stock
$42.00
1
20mgIn Stock
$80.00
1
50mgIn Stock
$110.00
1
100mgIn Stock
$185.00
1
500mgIn Stock
$651.00
1
1gIn Stock
$1,008.00
1
3gIn Stock
$1,785.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $56.00 | In Stock | 1 | |
| 5mg | $42.00 | In Stock | 1 | |
| 20mg | $80.00 | In Stock | 1 | |
| 50mg | $110.00 | In Stock | 1 | |
| 100mg | $185.00 | In Stock | 1 | |
| 500mg | $651.00 | In Stock | 1 | |
| 1g | $1,008.00 | In Stock | 1 | |
| 3g | $1,785.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citations
7 publicationsPublications from researchers using this productIF 16
PMID: 40695784 ↗IF 15
PMID: 33208750 ↗IF 13
PMID: 34210752 ↗IF 11
PMID: 35878022 ↗Description
EPZ-6438 is a potent and bio-available inhibitor of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of lysine 27 of histone H3 (H3K27), that inhibits the activity of human PRC2-containing wild-type EZH2 with a value of inhibition constant Ki of 2.5 nM. EPZ-6438 competitively binds to the S-adenosylmethionine (SAM) binding site of EZH2 and also non-competitively binds to the binding sites of peptide or nucleosome substrate. EPZ-6438 selectively inhibits EZH2 with selectivity 35-fold greater than EZH1. Study results have suggested that EPZ-6438 exhibits dramatic and permanent anti-tumor activity in MRT models through synergistic effects of EPZ-6438-mediated EZH2 inhibition on several cancer pathways.
Reference
[1].Sarah K. Knutson1, Natalie M. Warholic, Tim J. Wigle, Christine R. Klaus, Christina J. Allain, Alejandra Raimondi, Margaret Porter Scott, Richard Chesworth, Mikel P. Moyer, Robert A. Copeland, Victoria M. Richon, Roy M. Pollock, Kevin W. Kuntz, and Heike Keilhack. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. PNAS 2013; 110(19): 7922-7927
Protocol
| Cell experiment [1]: | |
|
Cell lines |
SMARCB1-deficient MRT cells |
|
Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reaction Conditions |
4-7 days |
|
Applications |
EPZ-6438 induces a reduction of global H3K27Me3 level in a concentration-dependent manner. In addition, EPZ-6438 leads to a substantial antiproliferative effects as IC50 values within nanomolar range. Treatment of EPZ-6438 results in expression of CD133, DOCK4, and PTPRK and up-regulates CDKN1A and CDKN2A and BIN1in a time-dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
SCID mice bearing EZH2-mutant lymphoma xenografts. |
|
Dosage form |
3 times daily every 8 hours, 2 times a day every 12 hours, or once a day schedules for either 7 or 28 days by oral gavage. |
|
Applications |
EPZ-6438 dose-dependently causes a reduction of tumor H3K27Me3 levels (EC50 =23 nmol/L). EPZ-6438 also shows a remarkable antitumor effects in a dose dependent manner with 2 cycles of 7-day on/7-day off and 21-day on/7-day off schedules. All EPZ-6438 dose groups except the lowest one leads to complete tumor regressions. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: 1. Knutson SK, Warholic NM, Wigle TJ et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7. 2. Knutson SK, Kawano S, Minoshima Y et al. Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma. Mol Cancer Ther. 2014 Apr;13(4):842-54. |
|
Product Documents
Purity:>99.00%Appearance:A solid
Biological Data
1 / 4
Chemical Properties
CAS No.
1403254-99-8
Synonyms
E-7438,Tazemetostat
Chemical Name
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide
SMILES
CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5
Molecular Formula
C34H44N4O4
Molecular Weight
572.74
Solubility
≥ 28.637mg/mL in DMSO
Storage
Desiccate at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
Reviews
Review for EPZ-6438
Rating: 5
- 5 Star100%
- 4 Star0%
- 3 Star0%
- 2 Star0%
- 1 Star0%