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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Epigenetics >Histone Methyltransferase Inhibitors >Tazemetostat (EPZ-6438)

Tazemetostat (EPZ-6438)

Tazemetostat (EPZ-6438)  Structure
  • ₹0
  • Product name: Tazemetostat (EPZ-6438)
  • CAS: 1403254-99-8
  • MF: C34H44N4O4
  • MW: 572.74
  • EINECS:
  • MDL Number:MFCD24849415
  • Synonyms:E-7438;EPZ-7438;N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-[1,1'-biphenyl]-3-carboxamide;[1,1'-Biphenyl]-3-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-;N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-[1,1'-biphenyl]-3-carboxamide EPZ6438;Henagliflozin Proline;Tazemetostat EPZ-6438;EPZ-6438(E7438)
Manufacturer Product number Product description Packaging Price Updated Buy

Properties

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).
pka :11.92±0.10(Predicted)
form :solid
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.

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 Causes skin irritation Skin corrosion/irritation Category 2 Warning GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 May cause respiratory irritation Specific target organ toxicity, single exposure;Respiratory tract irritation Category 3 Warning GHS hazard pictograms
Precautionary statements:
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P264 Wash hands thoroughly after handling.
P264 Wash skin thouroughly after handling.
P270 Do not eat, drink or smoke when using this product.
P271 Use only outdoors or in a well-ventilated area.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312 IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352 IF ON SKIN: wash with plenty of soap and water.
P304+P340 IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321 Specific treatment (see … on this label).
P330 Rinse mouth.
P332+P313 IF SKIN irritation occurs: Get medical advice/attention.
P337+P313 IF eye irritation persists: Get medical advice/attention.
P403+P233 Store in a well-ventilated place. Keep container tightly closed.
P405 Store locked up.
P501 Dispose of contents/container to..…

Description

EPZ6438 is an orally bioavailable, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 2.5 nM), the enzymatic subunit of polycomb repressive complex 2. It displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other histone methyltransferases. EPZ6438 blocks histone H3 lysine 27 trimethylation in both wild-type and mutant lymphoma cells (IC50s range from 2-90 nM). EPZ6438 has been shown to induce apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and to promote their regression in xenograft-bearing mice.

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