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

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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
InChIKey: GNMUEVRJHCWKTO-FQEVSTJZSA-N
SMILES: N12C(C)=NN=C1[C@H](CC(NC1=CC=C(O)C=C1)=O)N=C(C1=CC=C(Cl)C=C1)C1C(C)=C(C)SC=12

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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: $175.7
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML1605
Product name: OTX015
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $978
Updated: 2025/07/31

TCI Chemical

Product number: O0482
Product name: OTX 015
Packaging: 10MG
Price: $171
Updated: 2025/07/31

TCI Chemical

Product number: O0482
Product name: OTX 015
Packaging: 50MG
Price: $594
Updated: 2025/07/31

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

References

[1] J. NOEL. Abstract C244: Development of the BET bromodomain inhibitor OTX015.[J]. Molecular Cancer Therapeutics, 2013, 12 1. DOI: 10.1158/1535-7163.targ-13-c244
[2] M. COUDE?. Preclinical Study Of The Bromodomain Inhibitor OTX015 In Acute Myeloid (AML) and Lymphoid (ALL) Leukemias[J]. Blood, 2013, 122 1: 4218-4218. DOI: 10.1182/blood.v122.21.4218.4218
[3] M. BOI. Abstract A219: OTX015, a bromodomain and extraterminal inhibitor, represents a novel agent for ALK positive anaplastic large cell lymphoma.[J]. Molecular Cancer Therapeutics, 2013, 12 1. DOI: 10.1158/1535-7163.targ-13-a219

OTX015 Preparation Products And Raw materials

Raw materials

Preparation Products

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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:

(+)-JQ-1 PFI-1 I-BET151 (GSK1210151A) 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

Birabresib, 10 mM in DMSO

202590-98-5

2202590-98-5

Inhibitors