Free shipping on all orders over $ 500

OTX015

Cat. No. M2903
OTX015 Structure
Size Price Availability Quantity
10mg USD 150 In stock
50mg USD 480 In stock
100mg USD 800 In stock
Bulk Inquiry?

Quality Control
Biological Activity

OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4.

Protocol
Cell Experiment
Cell lines 33 cell lines from mature B-cell lymphoid tumors
Preparation method We first evaluated the anti-proliferative activity of the BET Bromodomain-inhibitor OTX015 in a panel of 33 cell lines derived from mature B-cell lymphoid tumors. As assessed by MTT assays performed after 72 hours of drug exposure, OTX015 was active in a dose-dependent manner in almost all the cell lines (Fig. 1A), at concentrations achievable in the clinical setting.
Concentrations 70nM~15µM
Incubation time 72h
Animal Experiment
Animal models anti-lymphoma activity NOD-SCID mice
Formulation unknown
Dosages 25 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 491.99
Formula C25H22ClN5O2S
CAS Number 202590-98-5
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
Related Epigenetic Reader Domain Products
666-15

666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.

JQ-1 carboxylic acid

(+)-JQ1 carboxylic acid is the carboxylic acid form of (+)-JQ1 for derivative synthesis.

AZD9496

AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.

GSK6853

GSK6853 is a selective benzimidazolone BRPF1 inhibitor with pIC50 of 8.1(TR-FRET) showing greater than 1600-fold selectivity over all other bromodomains tested.

Mivebresib

Mivebresib(ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4)

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: OTX015 supplier, Epigenetic Reader Domain, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.