Synonym
RK-287107; RK 287107; RK287107;
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
InChi Key
FZQYCOUBRJEYBC-UHFFFAOYSA-N
InChi Code
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)
SMILES Code
O=C1NC(N2CCC3(CC2)CN(CCO)C4=C3C(F)=CC(F)=C4)=NC5=C1CCCC5
Purity
>98% (or refer to the Certificate of Analysis)
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.
Storage Condition
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
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively.
In vitro activity:
To be determined
In vivo activity:
RK-287107 exerts an antitumor effect and may have potential for tankyrase-directed molecular cancer therapy. RK-287107 inhibits the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells. RK-287107 suppresses COLO-320DM tumor growth in NOD-SCID mice.
Reference: Cancer Sci. 2018 Dec;109(12):4003-4014. https://pubmed.ncbi.nlm.nih.gov/30238564/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
125.0 |
300.15 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
416.47
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. 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. PMID: 30238564; PMCID: PMC6272098.
2. Shirai F, Mizutani A, Yashiroda Y, Tsumura T, Kano Y, Muramatsu Y, Chikada T, Yuki H, Niwa H, Sato S, Washizuka K, Koda Y, Mazaki Y, Jang MK, Yoshida H, Nagamori A, Okue M, Watanabe T, Kitamura K, Shitara E, Honma T, Umehara T, Shirouzu M, Fukami T, Seimiya H, Yoshida M, Koyama H. Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer. J Med Chem. 2020 Apr 23;63(8):4183-4204. doi: 10.1021/acs.jmedchem.0c00045. Epub 2020 Apr 1. PMID: 32202790.
In vitro protocol:
To be determined
In vivo protocol:
1. 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. PMID: 30238564; PMCID: PMC6272098.
2. Shirai F, Mizutani A, Yashiroda Y, Tsumura T, Kano Y, Muramatsu Y, Chikada T, Yuki H, Niwa H, Sato S, Washizuka K, Koda Y, Mazaki Y, Jang MK, Yoshida H, Nagamori A, Okue M, Watanabe T, Kitamura K, Shitara E, Honma T, Umehara T, Shirouzu M, Fukami T, Seimiya H, Yoshida M, Koyama H. Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer. J Med Chem. 2020 Apr 23;63(8):4183-4204. doi: 10.1021/acs.jmedchem.0c00045. Epub 2020 Apr 1. PMID: 32202790.
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.
