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
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
Safety
- HS Code
- 2934.99.3900
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.
N-Bromosuccinimide Price
- Product number
- SML1605
- Product name
- OTX015
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $146.4
- Updated
- 2024/03/01
- Product number
- SML1605
- Product name
- OTX015
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $951
- Updated
- 2024/03/01
- Product number
- O0482
- Product name
- OTX 015
- Packaging
- 10MG
- Price
- $171
- Updated
- 2024/03/01
- Product number
- O0482
- Product name
- OTX 015
- Packaging
- 50MG
- Price
- $594
- Updated
- 2024/03/01
- Product number
- 15947
- Product name
- OTX 015
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $49
- Updated
- 2024/03/01
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-
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
OTX015 Suppliers
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View Lastest Price from OTX015 manufacturers
- Product
- OTX015 202590-98-5
- Price
- US $0.00/mg
- Min. Order
- 1mg
- Purity
- 98%min
- Supply Ability
- 50mg
- Release date
- 2021-08-26
- 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