OTX015
- CAS No.
- 202590-98-5
- Chemical Name:
- OTX015
- Synonyms
- MK8628;OTX015;OTX 015;OTX-015;MK 8628;MK-8628;CS-1013;OXT-015;Birabresib;OTX015(OTX-015)
- CBNumber:
- CB42666673
- Molecular Formula:
- C25H22ClN5O2S
- Molecular Weight:
- 491.99
- MDL Number:
- MFCD26960949
- MOL File:
- 202590-98-5.mol
- MSDS File:
- SDS
| 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 |
| pka | 10.05±0.26(Predicted) |
| form | powder |
| color | white to light brown |
| FDA UNII | X40LKS49S3 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
| HS Code | 2934.99.3900 |
OTX015 price More Price(43)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML1605 | OTX015 ≥98% (HPLC) | 202590-98-5 | 5MG | $146.4 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML1605 | OTX015 ≥98% (HPLC) | 202590-98-5 | 25MG | $951 | 2024-03-01 | Buy |
| TCI Chemical | O0482 | OTX 015 | 202590-98-5 | 10MG | $171 | 2024-03-01 | Buy |
| TCI Chemical | O0482 | OTX 015 | 202590-98-5 | 50MG | $594 | 2024-03-01 | Buy |
| Cayman Chemical | 15947 | OTX 015 ≥95% | 202590-98-5 | 1mg | $49 | 2024-03-01 | Buy |
OTX015 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Zhejiang ZETian Fine Chemicals Co. LTD | 18957127338 | stella@zetchem.com | China | 2141 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Jilin Chinese Academy of Sciences - Yanshen Technology Co., Ltd. | 0431-80514535 13634302652 | Extension@chemextension.com | CHINA | 967 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Shanghai Daeyeon Chemicals Co., Ltd | 021-64478606 +8615900664856 | daeyeon001@vip.163.com | China | 2062 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29220 | 58 |
| Wuhan Fortuna Chemical Co., Ltd | +86-27-59207850 +86-13986145403 | info@fortunachem.com | China | 5988 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
View Lastest Price from OTX015 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2021-09-29 | OTX015
202590-98-5
|
US $0.00 / mg | 1mg | 98%min | 50mg | WUHAN FORTUNA CHEMICAL CO., LTD | |
![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)?- pictures](https://img.chemicalbook.com/ProductImageEN/2019-12/Small/b2f8639f-3ce0-41ed-982d-01ee7f83faea.png) |
2019-12-23 | 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
|
US $1.00 / KG | 1g | Min98% HPLC | g/kg /ton | Career Henan Chemical Co |
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- OTX015
202590-98-5
- US $0.00 / mg
- 98%min
- WUHAN FORTUNA CHEMICAL CO., LTD
-
- 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
- US $1.00 / KG
- Min98% HPLC
- Career Henan Chemical Co