Description Features In vitro In vivo
ChemicalBook > CAS DataBase List > OTX015

OTX015

Description Features In vitro In vivo
Product Name
OTX015
CAS No.
202590-98-5
Chemical Name
OTX015
Synonyms
MK8628;OTX015;MK 8628;MK-8628;OXT-015;CS-1013;OTX 015;OTX-015;Birabresib;OTX015(OTX-015)
CBNumber
CB42666673
Molecular Formula
C25H22ClN5O2S
Formula Weight
491.99
MOL File
202590-98-5.mol
More
Less

OTX015 Property

Melting point:
220 °C
Density 
1.45±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
≥24.6 mg/mL in DMSO; insoluble in H2O; ≥106 mg/mL in EtOH with gentle warming
form 
powder
pka
10.05±0.26(Predicted)
color 
white to light brown
More
Less

Safety

HS Code 
2934.99.3900
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

More
Less

N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1605
Product name
OTX015
Purity
≥98% (HPLC)
Packaging
5MG
Price
$146.4
Updated
2024/03/01
Sigma-Aldrich
Product number
SML1605
Product name
OTX015
Purity
≥98% (HPLC)
Packaging
25MG
Price
$951
Updated
2024/03/01
TCI Chemical
Product number
O0482
Product name
OTX 015
Packaging
10MG
Price
$171
Updated
2024/03/01
TCI Chemical
Product number
O0482
Product name
OTX 015
Packaging
50MG
Price
$594
Updated
2024/03/01
Cayman Chemical
Product number
15947
Product name
OTX 015
Purity
≥95%
Packaging
1mg
Price
$49
Updated
2024/03/01
More
Less

OTX015 Chemical Properties,Usage,Production

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.

Features

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

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.

Description

The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM). It displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias, downregulating c-Myc expression and inducing cell cycle arrest and apoptosis. At 100 mg/kg, OTX015 has been shown to inhibit the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79%.

Uses

(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 is an orally bioavailable, inhibitor of BRD2, BRD3, and BRD4 to AcH4 and shows anti-tumor activity in vitro and in vivo tumor models.

Definition

ChEBI: 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)- is an organonitrogen heterocyclic compound and an organosulfur heterocyclic compound.

Biochem/physiol Actions

It binds to bromodomain and extra-terminal domain (BET) proteins and inhibits their binding to the chromatin. This in turn prevents gene transcription. OTX015 has been shown to inhibit proliferation of cells in haematological malignancies.

target

BRD2

storage

Store at -20°C

OTX015 Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

OTX015 Suppliers

Americas 1 China 142 Europe 1 India 2 Japan 1 United Kingdom 2 United States 18 Global 167
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
Target molecule Corp.
Tel
857-239-0968
Fax
857-239-8801
Email
service1@targetmol.com
Country
United States
ProdList
2559
Advantage
60
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
32161
Advantage
58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
Email
inquiry@bocsci.com
Country
United States
ProdList
19553
Advantage
58
Cato Research Chemicals Inc.
Tel
020-81215950 4000-868-328
Email
customer@uwalab.com
Country
United States
ProdList
10404
Advantage
58
Aladdin Scientific
Tel
+1-+1(833)-552-7181
Email
sales@aladdinsci.com
Country
United States
ProdList
57505
Advantage
58
TargetMol Chemicals Inc.
Tel
Email
support@targetmol.com
Country
United States
ProdList
38631
Advantage
58
ApexBio Technology
Tel
--
Fax
--
Email
sales@apexbt.com
Country
United States
ProdList
6251
Advantage
58
ChemieTek
Tel
--
Fax
--
Email
info@chemietek.com
Country
United States
ProdList
219
Advantage
50
LKT Laboratories, Inc.
Tel
--
Fax
--
Email
info@lktlabs.com
Country
United States
ProdList
2164
Advantage
64
Cayman Chemical Company
Tel
--
Fax
--
Email
cayman@caymanchem.com
Country
United States
ProdList
6213
Advantage
81
ChemShuttle. Inc.
Tel
--
Fax
--
Email
Sales@ChemShuttle.com
Country
United States
ProdList
6695
Advantage
58
MedChemExpress
Tel
--
Fax
--
Email
sales@medchemexpress.com
Country
United States
ProdList
6398
Advantage
58
Matrix Scientific
Tel
--
Fax
--
Email
sales@matrixscientific.com
Country
United States
ProdList
6632
Advantage
80
More
Less

View Lastest Price from OTX015 manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
OTX015 202590-98-5
Price
US $0.00/mg
Min. Order
1mg
Purity
98%min
Supply Ability
50mg
Release date
2021-08-26
Career Henan Chemical Co
Product
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)?- 202590-98-5
Price
US $1.00/KG
Min. Order
1g
Purity
Min98% HPLC
Supply Ability
g/kg /ton
Release date
2019-12-20

202590-98-5, OTX015Related Search:

PFI-1 I-BET151 (GSK1210151A) (+)-JQ1 RVX-208 CPI-203 I-BET-762

  • CS-1013
  • OXT-015
  • OTX 015; OTX015;MK-8628; MK 8628; MK8628;OTX-015
  • OTX015(OTX-015)
  • 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)-
  • MK 8628
  • MK8628
  • MK-8628
  • OTX015;OTX 015;OTX-015
  • 2-((6S)-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
  • Birabresib
  • OTX-015 (Birabresib)
  • OTX015(MK-8628,Birabresib)
  • OTX015; OTX-015; OTX 015; MK-8628; MK 8628; MK8628; BIRABRESIB.
  • OTX 015
  • OTX015
  • OTX-015
  • (S)-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
  • (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
  • (S)-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
  • Birabresib(OTX-015)
  • OTX015 USP/EP/BP
  • Venadaparib Impurity 93
  • 202590-98-5
  • 2202590-98-5
  • Inhibitors