Tazemetostat (EPZ-6438)
- Product Name
- Tazemetostat (EPZ-6438)
- CAS No.
- 1403254-99-8
- Chemical Name
- Tazemetostat (EPZ-6438)
- Synonyms
- Tazemetostat;EPZ-6438;E-7438;CS-971;CPDB1064;EPZ-7438;EPZ-6438(E7438);E7438, Tazemetostat;Tazemetostat EPZ-6438;Henagliflozin Proline
- CBNumber
- CB82655404
- Molecular Formula
- C34H44N4O4
- Formula Weight
- 572.74
- MOL File
- 1403254-99-8.mol
Tazemetostat (EPZ-6438) Property
- Melting point:
- >162°C (dec.)
- Boiling point:
- 750.8±60.0 °C(Predicted)
- Density
- 1.163±0.06 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- Soluble in DMSO (up to at least 25 mg/ml).
- form
- solid
- pka
- 11.92±0.10(Predicted)
- color
- Off-white
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 16174
- Product name
- EPZ6438
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 16174
- Product name
- EPZ6438
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $130
- Updated
- 2024/03/01
- Product number
- 16174
- Product name
- EPZ6438
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $235
- Updated
- 2024/03/01
- Product number
- 16174
- Product name
- EPZ6438
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $745
- Updated
- 2024/03/01
- Product number
- E592250
- Product name
- EPZ6438
- Packaging
- 1mg
- Price
- $50
- Updated
- 2021/12/16
Tazemetostat (EPZ-6438) Chemical Properties,Usage,Production
Description
Tazemetostat (1403254-99-8) is a potent (Ki = 2.5nM wild type human PRC2-containing) and selective SAM-competitive inhibitor of the lysine methyltransferase EZH2.1?Tazemetostat displayed strong antiproliferative effects against SMARCB1-deleted malignant rhabdoid tumor (MRT) cell lines?in vitro. This antitumor activity was also observed in SMARTCB1 mutant mouse xenografts. It displayed potent antitumor activity in various cancer models including non-Hodgkins lymphoma2, pediatric glioma3, small-cell carcinoma of the ovary4, and synovial sarcomas5. Tazemetostat has also been shown to control inflammatory genes by modulating IRF1, IRF8, and STAT1 levels suggesting therapeutic potential for the treatment of neuroinflammatory diseases associated with microglial activation.6
Uses
EPZ 6438 is a potent and selective inhibitor of EZH2.
Biological Activity
Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with K i and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMT.
target
EZH2(Cell-free assay)
References
1) Knutson?et al.?(2013),?Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2;?Proc. Natl. Acad. Sci. USA?110?7922 2) Knutson?et al.?(2014),?Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma; Mol.Cancer Ther.?13?842 3) Mohammad?et al. (2017),?EZH2 is a potential therapeutic target for H3K27M-mutant pediatric gliomas; Nat. Med.?23?483 4) Chan-Penebre?et al.?(2017),?Selective killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models; Mol. Cancer Ther.?16?850 5) Kawano?et al.?(2016),?Preclinical Evidence of Anti-Tumor Activity by EZH2 Inhibition in Human Models of Synovial Sarcoma; PLoS One?11?e0158888 6) Arifuzzaman?et al.?(2017),?Selective inhibition of EZH2 by a small molecule inhibitor regulates microglial gene expression essential for inflammation; Biochem. Pharmacol.?137?61
Tazemetostat (EPZ-6438) Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Tazemetostat (EPZ-6438) manufacturers
- Product
- Tazemetostat (EPZ-6438) 1403254-99-8
- Price
- US $60.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 1000
- Release date
- 2024-03-25
- Product
- Tazemetostat (EPZ-6438) 1403254-99-8
- Price
- US $5.90/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 500000kg
- Release date
- 2024-10-29
- Product
- Tazemetostat (EPZ-6438) 1403254-99-8
- Price
- US $0.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 50000KG/month
- Release date
- 2023-11-30