OTX-015 OTX-015
CAS 202590-98-5 MFCD02590985
化学结构图
SMILES: Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=NC(CC(=O)Nc1ccc(O)cc1)c1nnc(C)n1-2
化学属性
| Mol. Weight | 491.99248 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name Translation | OTX-015 |
|---|---|
| Chemical Name | OTX-015 |
| PubChem Substance ID | 9936746 |
| 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 |
| Synonym | OTX015 OTX015; OTX-015; OTX 015; MK-8628; MK 8628; MK8628; Birabresib. |
| LabNetwork Molecule ID | LN01265369 |
| Formula | C25H22ClN5O2S |
| IUPAC 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. |
| InChIKey | GNMUEVRJHCWKTO-FQEVSTJZSA-N |
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产品应用
- Birabresib, also known as OTX015 and MK-8628, a potent BET bromodomian inhibitor, which targets the BET bromodomain proteins 2, 3, and 4 (BRD2/3/4). BRDs 2, 3, and 4 are considered potential cancer targets because of their pivotal role in regulating the transcription of growth-promoting genes and cell cycle regulators. OTX015 is the first BRD2/3/4 inhibitor to enter clinical trials. OTX015 showed antiproliferative activity in a large panel of cell lines derived from mature B-cell lymphoid tumors with median IC50 of 240 nmol/L, without significant differences among the different histotypes.
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