| Company Name: |
Shanghai Synchem Pharma Co., ltd Gold |
| Tel: |
21-619849051-1 18521059765 |
| Email: |
synchempharma@aliyun.com |
| Products Intro: |
Product Name:OTX015
CAS:202590-98-5
Purity:98%+ Package:1g/
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| Company Name: |
Twochem Co.Ltd Gold |
| Tel: |
021-021-58111628 15800915896 |
| Email: |
sales@twochem.com |
| Products Intro: |
Product Name:OTX015
CAS:202590-98-5
Purity:>98% HPLC Package:1g;10g;100g
|
| Company Name: |
Chembest Research Laboratories Limited |
| Tel: |
021-20908456 |
| Email: |
sales@BioChemBest.com |
| Products Intro: |
Product Name:OTX-015 (MK-8628
CAS:202590-98-5
Purity:98%+ HPLC Package:50mg;100mg;500mg;1g;5g;10g Remarks:Biochemical Reagents; Pharmaceutical Intermediates
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- OTX015
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2026-09-11
- CAS:202590-98-5
- Min. Order: 1mg
- Purity: 98%min
- Supply Ability: 50mg
- Birabresib
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- $41.00
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2026-07-14
- CAS:202590-98-5
- Purity: 99.80%
- Supply Ability: 10g
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| Product Name: | OTX015 | | Synonyms: | 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;OTX015;OTX 015;OTX-015 | | CAS: | 202590-98-5 | | MF: | C25H22ClN5O2S | | MW: | 491.99 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 202590-98-5.mol |  |
| | OTX015 Chemical Properties |
| 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 |
| WGK Germany | WGK 3 | | HS Code | 2934.99.3900 | | Storage Class | 11 - Combustible Solids |
| | OTX015 Usage And Synthesis |
| 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 |
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