RK-287107
RK-287107 is a potent TNKS/TNKS2 inhibitor (IC50 = 14.4 nM) with >7000-fold selectivity against the PARP1 enzyme, which inhibits WNT-responsive TCF reporter activity and proliferation of human colorectal cancer cell line COLO-320DM. RK-287107 also demonstrated dose-dependent tumor growth inhibition in a mouse xenograft model. RK-287107 is a promising lead compound for the development of novel tankyrase inhibitors as anticancer agents.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | RK-287107 |
|---|---|
| Iupac 化学名称 | 2-(4,6-difluoro-1-(2-hydroxyethyl)spiro[indoline-3,4'-piperidin]-1'-yl)-5,6,7,8-tetrahydroquinazolin-4(3H)-one |
| 同义词 | RK-287107; RK 287107; RK287107; |
| 英文同义词 | RK-287107; RK 287107; RK287107; |
| 分子式 | C22H26F2N4O2 |
| 分子量 | 416.4728 |
| Smile | O=C1NC(N2CCC3(CC2)CN(CCO)C4=C3C(F)=CC(F)=C4)=NC5=C1CCCC5 |
| InChiKey | FZQYCOUBRJEYBC-UHFFFAOYSA-N |
| InChi | InChI=1S/C22H26F2N4O2/c23-14-11-16(24)19-18(12-14)28(9-10-29)13-22(19)5-7-27(8-6-22)21-25-17-4-2-1-3-15(17)20(30)26-21/h11-12,29H,1-10,13H2,(H,25,26,30) |
| Cas号 | 2171386-10-8 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Shirai F, Tsumura T, Yashiroda Y, Yuki H, Niwa H, Sato S, Chikada T, Koda Y,
Washizuka K, Yoshimoto N, Abe M, Onuki T, Mazaki Y, Hirama C, Fukami T, Watanabe
H, Honma T, Umehara T, Shirouzu M, Okue M, Kano Y, Watanabe T, Kitamura K,
Shitara E, Muramatsu Y, Yoshida H, Mizutani A, Seimiya H, Yoshida M, Koyama H.
Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors. J
Med Chem. 2019 Apr 1. doi: 10.1021/acs.jmedchem.8b01888. [Epub ahead of print]
PubMed PMID: 30883102.
2: Mizutani A, Yashiroda Y, Muramatsu Y, Yoshida H, Chikada T, Tsumura T, Okue M,
Shirai F, Fukami T, Yoshida M, Seimiya H. RK-287107, a potent and specific
tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model.
Cancer Sci. 2018 Dec;109(12):4003-4014. doi: 10.1111/cas.13805. Epub 2018 Oct 20.
PubMed PMID: 30238564.
