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.
For research use only. We do not sell to patients.
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; |
| 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 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | 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 |
| Handling | |
| 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. |
| HS Code |
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| 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.
Chemical Structure
