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

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PRODUCTS SPECIFICATIONS [202590-98-5]

Catalog

SLK-S7360

Brand

Selleck

CAS

202590-98-5

DESCRIPTION [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