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基本描述
| 英文名称 | itacnosertib |
|---|---|
| 别名 | example 11 [WO2014151871A9];TP-0184;TP0184 |
| 英文别名 | example 11 [WO2014151871A9];TP-0184;TP0184 |
名称和标识符
| IUPAC Name | 2-N-[3-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-N-(2-pyridin-2-ylpyridin-3-yl)pyrimidine-2,4-diamine |
|---|---|
| INCHI | InChI=1S/C26H28N8O/c1-33-14-16-34(17-15-33)22-9-8-19(18-23(22)35-2)30-26-29-13-10-24(32-26)31-21-7-5-12-28-25(21)20-6-3-4-11-27-20/h3-13,18H,14-17H2,1-2H3,(H2,29,30,31,32) |
| InChi Key | XSQKEVGTZSBVBR-UHFFFAOYSA-N |
| Canonical SMILES | COc1cc(ccc1N1CCN(CC1)C)Nc1nccc(n1)Nc1cccnc1c1ccccn1 |
| PubChem CID | 86290265 |
数据库链接
| PubChem CID | 86290265 |
|---|---|
| CAS Registry No. | 1628870-27-8 |
关联配体
| Ligand ID | 10632 |
|---|---|
| 名称 | itacnosertib |
| 别名 | example 11 [WO2014151871A9] |
| 类别 | Synthetic organic |
| 学名 | 2-N-[3-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-N-(2-pyridin-2-ylpyridin-3-yl)pyrimidine-2,4-diamine |
| 生物活性评价 |
The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in |
| 评价 |
The chemical structure that was submitted to the WHO for the INN itacnosertib is identical to the structure of example 11 that is claimed in Tolero Pharmaceuticals' patent WO2014151871A9 |
| 临床描述 |
TP-0184 is a potent inhibitor of ALK2 or ACRV1 kinase, a constitutively active
serine/threonine receptor kinase due to activating mutations or upregulated upstream
signaling pathways. This is a Phase 1, open-label, dose-escalation, safety, pharmacokinetics,
and pharmacodynamic study, with a purpose of determining the maximum tolerated dose (MTD) and
dose-limiting toxicities (DLTs) of oral TP-0184 administered once weekly for 4 weeks in
patients with advanced solid tumors.
This study will evaluate preliminary safety and efficacy of TP-0184 to treat anemia when administered to adult patients with Revised International Prognostic Scoring System (IPSS-R) low or intermediate risk MDS. The recommended Phase 2 dose (RP2D) will be determined by the maximum tolerated dose (MTD) or maximum administered dose (MAD) in the Phase 1 portion of the study. |
| 来源公司 |
Sumitomo Dainippon Pharma Oncology, Inc Sumitomo Dainippon Pharma Oncology, Inc |
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