OTX015, BET Inhibitor


Catalog No. size PriceQuantity
M60193-2S 2 mg solid $89
M60193-10S 10 mg solid $356

Description

Product Information
Molecular Weight: 491.99
Formula: C25H22ClN5O2S
Purity: ≥98%
CAS#: 202590-98-5
Solubility: DMSO up to 100 mM
Chemical Name: (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

OTX015 is a novel, highly potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3 and BRD4 with IC50 of 10-19 nM. It inhibits the growth of a variety of human cancer cell lines with IC50 ranging from 60 to 200 nM. OTX015 results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines. In vivo studies using OTX015 have demonstrated efficacy in a range of oncology models. OTX015 is currently in phase I clinical development for oncology indication.

 

 


How to Use:

 

 

  • In vitro: OTX015 was used at 2-10 µM final concentration in various in vitro assays.
  • In vivo: OTX015 could be dosed to the mice by oral administration at 100 mg/kg once per day or 10 mg/kg twice per day.

 

 

 


Reference:

 

  1. Noel JK, et al. Development of the BET bromodomain inhibitor OTX015. (2013) Mol Cancer Ther. 12, C244.
  2. Boi M, et al. OTX015, a bromodomain and extraterminal inhibitor, represents a novel agent for ALK positive anaplastic large cell lymphoma. (2013) Mol Cancer Ther. 12, A219.

 



 

Products are for research use only. Not for human use.

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