Bulk Inquiry
OTX 015
- Optical Purity: Optically pure
- Soluble in DMSO and EtOH
- MF: C25H22ClN5O2S
- MW: 491.99
Description
Potent inhibitor of BRD2, BRD3, and BRD4 (Ki values ranging from 3.2 to 24.7 nM, considering BDs 1 and 2), with clear anti-proliferative activity on a large number of diffuse large B-cell lymphoma (DLBCL) cell lines. OTX 015 inhibits the growth of hematologic malignances through directly regulating MYC expression and activity.
More Information
| Parent CAS No. | 202590-98-5 |
|---|---|
| Chemical Name | (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 |
| 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 |&1:6,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C25H22ClN5O2S/c1-13-14(2)34-25-22(13)23(16-4-6-17(26)7-5-16)28-20(24-30-29-15(3)31(24)25)12-21(33)27-18-8-10-19(32)11-9-18/h4-11,20,32H,12H2,1-3H3,(H,27,33)/t20-/m0/s1 |
| InChiKey | GNMUEVRJHCWKTO-FQEVSTJZSA-N |
| CID | 9936746 |
| Short Description | BET-BRD inhibitor |
References
- M. Boi et al. The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs.Clin Cancer Res. 2015 Apr 1;21(7):1628-38.
- J. Lu et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.
- X. Ran et al. Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. J Med Chem. 2015 Jun 25;58(12):4927-39.
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