OTX015

Catalog No.S7360

OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Phase 1.

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OTX015 Chemical Structure

OTX015 Chemical Structure
Molecular Weight: 491.99

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Phase 1.
Targets BRDs [1]
(Cell-free assay)
IC50 10-19 nM(EC50)
In vitro OTX015 inhibits the binding of BRD2, BRD3, and BRD4 to AcH4 with IC50 ranging from 92 to 112 nM, and inhibits the growth of a variety of human cancer cell lines with GI50 ranging from 60 to 200 nM. [1] 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. [2]
In vivo OTX015 (p.o.) significantly inhibits the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79% at 100 mg/kg qd and 61% at 10 mg/kg bid, respectively. [1]
Features Orally bioavailable BRD2/3/4-selective inhibitor that has been tested in Phase I clinical trials for treatment of Haematological Malignancies.

Protocol(Only for Reference)

Kinase Assay: [1]

TR-FRET Assay [1] To assess binding of OTX015 to BRD2, BRD3, and BRD4, BRD-expressing CHO cell lysate (from CHO cells transfected with expression plasmids for Flag-tagged BRD2, BRD3, or BRD4 or vector alone), europium-conjugated anti-Flag antibody, XL-665-conjugated streptavidin, and biotinylated OTX015 are incubated at room temperature for 0.2 to 2 h. Fluorescence is measured by TR-FRET using an EnVision 2103 Multilabel Reader and EC50 for binding is calculated by nonlinear regression using PRISM version 5.02.

Cell Assay: [1]

Cell lines Human tumor cells
Concentrations ~2 μM
Incubation Time 72 hours
Method Effects of OTX015 on cancer cell proliferation are evaluated by incubating human tumor cells for 72 h with increasing concentrations of OTX015 and assessing proliferation using a tetrazolium salt (WST-8)-based colorimetric assay.

Animal Study: [1]

Animal Models BLAB/c-nu/nu mice bearing established Ty82 BRD-NUT midline carcinoma xenografts.
Formulation
Dosages ~100 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Noel JK, et al. Mol Cancer Ther. 2013, 12, C244.

[2] Boi M, et al. Mol Cancer Ther. 2013, 12, A219.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02303782 Withdrawn Acute Myeloid Leukemia Oncoethix GmbH January 2015 Phase 1|Phase 2
NCT02296476 Terminated Glioblastoma Multiforme Oncoethix GmbH October 2014 Phase 1|Phase 2
NCT02259114 Active, not recruiting NUT Midline Carcinoma|Triple Negative Breast Cancer|Non-small Cell Lung Cancer With Rearranged ALK Gene/Fusion Protein or KRAS Mutation|Castrate-re  ...more NUT Midline Carcinoma|Triple Negative Breast Cancer|Non-small Cell Lung Cancer With Rearranged ALK Gene/Fusion Protein or KRAS Mutation|Castrate-resistant Prostate Cancer (CRPC)|Pancreatic Ductal Adenocarcinoma Oncoethix GmbH October 2014 Phase 1
NCT01713582 Active, not recruiting Acute Myeloid Leukemia|Diffuse Large B-cell Lymphoma|Acute Lymphoblastic Leukemia|Multiple Myeloma Oncoethix GmbH December 2012 Phase 1

Chemical Information

Download OTX015 SDF
Molecular Weight (MW) 491.99
Formula

C25H22ClN5O2S

CAS No. 202590-98-5
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 98 mg/mL (199.19 mM)
Ethanol 98 mg/mL (199.19 mM)
Water <1 mg/mL (<1 mM)
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name (6S)-​4-​(4-​chlorophenyl)-​N-​(4-​hydroxyphenyl)-​2,​3,​9-​trimethyl-​6H-​thieno[3,​2-​f][1,​2,​4]triazolo[4,​3-​a][1,​4]diazepine-​6-​acetamide

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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