OTX015 --- BET Inhibitor

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

Synonym:

Birabresib

MK-8628

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

InChiKey: GNMUEVRJHCWKTO-FQEVSTJZSA-N

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.

References:

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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