Description Features In vitro In vivo
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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
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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
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Safety

HS Code 
2934.99.3900
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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.

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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
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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

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OTX015 Suppliers

Americas 1 China 141 Europe 1 India 2 Japan 1 United Kingdom 2 United States 17 Global 165
TCI AMERICA
Tel
800-4238616
Fax
+1-888-520-1075 / +1-503-283-1987
Email
sales@tciamerica.com
Country
Americas
ProdList
23662
Advantage
75
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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