OTX015 --- BET Inhibitor

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


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.

Product information

CAS Number: 202590-98-5

Molecular Weight: 491.99

Formula: C25H22ClN5O2S




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

Smiles: CC1=NN=C2[C@H](CC(=O)NC3C=CC(O)=CC=3)N=C(C3=C(SC(C)=C3C)N12)C1C=CC(Cl)=CC=1


InChi: InChI=1S/C25H22ClN5O2S/c1-13-14(2)34-25-22(13)23(16-4-6-17(26)7-5-16)28-20(24-30-29-15(3)31(24)25)12-21(33)27-18-8-10-19(32)11-9-18/h4-11,20,32H,12H2,1-3H3,(H,27,33)/t20-/m0/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

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.


  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.


Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed