Welcome to Arctom, sign up to enjoy up to 20% OFF

Search in Small Molecules Search in Biologics

Structure Search

Cart - 0 item(s)
$0.00

Your shopping cart is empty!

Chemistry
Bioactive Molecules
Natural Products
ADCs
Antibodies
- Primary Antibodies
- Secondary Antibodies
Multiplex IHC
Material Science
Others

[CAS NO. 202590-98-5] Birabresib (OTX015)

Ships within

Stock

Price

Qty

Total

SDS

COA

Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.

Catalog:	SLK-S7360
Brand:	Selleck
CAS:	202590-98-5

Overview

MDL	MFCD26960949
Molecular Weight	491.99
Molecular Formula	C25H22ClN5O2S
SMILES	CC=1C2=C(N3C([C@H](CC(NC4=CC=C(O)C=C4)=O)N=C2C5=CC=C(Cl)C=C5)=NN=C3C)SC1C

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.0326 mL	10.1628 mL	20.3256 mL
5 mM	0.4065 mL	2.0326 mL	4.0651 mL
10 mM	0.2033 mL	1.0163 mL	2.0326 mL
50 mM	0.0407 mL	0.2033 mL	0.4065 mL

Description

Birabresib (OTX015, MK 8628) is a potent inhibitor with ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of target genes.

Features

Orally bioavailable BRD2/3/4-selective inhibitor that has been tested in Phase I clinical trials for treatment of Haematological Malignancies.

Targets

BRDs ^[1]
(Cell-free assay)

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. 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

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.

References

[1] Noel JK, et al. Mol Cancer Ther. 2013, 12, C244.
[2] Boi M, et al. Mol Cancer Ther. 2013, 12, A219.

Synonyms

6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6S)-

6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-(4-hydroxyphenyl)-2,3,9-trimethyl-, (S)-

(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

OTX 015

MK 8628

Birabresib

(-)-OTX 015

(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

OXT 015

Request a Quote

Please fill in your details below to request a COA for our product. We will send the COA to the provided email address promptly.

Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.

Information

Shipping
Privacy notice
Terms of Service
About us
Contact us

Customer service

Search
Custom Synthesis

My account

My account
Orders
Addresses
Shopping cart