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基本描述
| 英文名称 | samuraciclib |
|---|---|
| 别名 | CT7001;ICEC-0942;ICEC0942;PPDA-001 |
| 英文别名 | CT7001;ICEC-0942;ICEC0942;PPDA-001 |
名称和标识符
| IUPAC Name | (3R,4R)-4-[[[7-(benzylamino)-3-propan-2-ylpyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]piperidin-3-ol |
|---|---|
| INCHI | InChI=1S/C22H30N6O/c1-15(2)18-13-26-28-21(25-11-16-6-4-3-5-7-16)10-20(27-22(18)28)24-12-17-8-9-23-14-19(17)29/h3-7,10,13,15,17,19,23,25,29H,8-9,11-12,14H2,1-2H3,(H,24,27)/t17-,19+/m1/s1 |
| InChi Key | YCVGLKWJKIKVBI-MJGOQNOKSA-N |
| Canonical SMILES | O[C@H]1CNCC[C@@H]1CNc1cc(NCc2ccccc2)n2c(n1)c(cn2)C(C)C |
| PubChem CID | 91844733 |
关联配体
| Ligand ID | 9903 |
|---|---|
| 名称 | samuraciclib |
| 别名 | PPDA-001 |
| 类别 | Synthetic organic |
| 学名 | (3R,4R)-4-[[[7-(benzylamino)-3-propan-2-ylpyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]piperidin-3-ol |
| 生物活性评价 |
CDK4, CDK6 and CDK8 are not substantially inhibited by ICEC0942 |
| 评价 |
Samuraciclib (ICEC0942, a.k.a. CT7001) is an orally available, non-covalent, selective inhibitor of cyclin dependent kinase 7 (CDK7) that was developed as a new transcription-targeting approach for potential cancer therapy |
| 临床描述 |
This is a modular, Phase I/II, multicentre study to investigate the optimal monotherapy dose of CT7001 in advanced solid malignancies (Module 1A) and to further investigate the monotherapy dose of CT7001 in specific participant groups (Module 1B). Further modules will be added as substantial protocol amendments. A food-effect study of CT7001 monotherapy in advanced solid malignancies (Module 4) is ongoing. A study of combination doses of CT7001 with fulvestrant in hormone receptor-positive (HR+ve) / human epidermal growth factor-2 negative (HER2-ve) breast cancer (Module 2) is planned to start in 2019. |
| 来源公司 |
Carrick Therapeutics Limited |
产品问答
产品问答
参考文献
| 1. Patel H, Periyasamy M, Sava GP, Bondke A, Slafer BW, Kroll SHB, Barbazanges M, Starkey R, Ottaviani S, Harrod A et al.. (2018) ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment.. Mol Cancer Ther, 17 (6): (1156-1166). [PMID:29545334] |
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