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.
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Chemical Information
| Name | RK-287107 |
|---|---|
| Iupac Chemical Name | 2-(4,6-difluoro-1-(2-hydroxyethyl)spiro[indoline-3,4'-piperidin]-1'-yl)-5,6,7,8-tetrahydroquinazolin-4(3H)-one |
| Synonyms | RK-287107; RK 287107; RK287107; |
| 英文同义词 | RK-287107; RK 287107; RK287107; |
| Molecular Formula | C22H26F2N4O2 |
| Molecular Weight | 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 Number | 2171386-10-8 |
| 相关CAS号 |
Ordering Information
| 包装 | Price | 库存 | Purity | 备货期 |
|---|---|---|---|---|
| 大货 | Enquiry | Enquiry | Enquiry |
| 外观性状 | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| 处理方式 | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| 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.
