Description
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. RK-287107 blocks colorectal cancer cell growth.
Product information
CAS Number: 2171386-10-8
Molecular Weight: 416.46
Formula: C22H26F2N4O2
Chemical Name: 2-[4,6-difluoro-1-(2-hydroxyethyl)-1,2-dihydrospiro[indole-3,4'-piperidin]-1'-yl]-3,4,5,6,7,8-hexahydroquinazolin-4-one
Smiles: OCCN1CC2(CCN(CC2)C2NC(=O)C3CCCCC=3N=2)C2=C1C=C(F)C=C2F
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (300.15 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
RK-87107 (0.01-10 μM; 12 hours) shows an antiproliferative effect on colorectal cancer cells harboring short adenomatous polyposis coli (APC) mutations. The 50% growth inhibition (GI50) value of RK-287107 on COLO-320DM cells is 0.449 μM. RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2. RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells.
In Vivo:
RK-287107 (100 and 300 mg/kg; i.p. administration; once per day; 5-days on/ 2-days off schedule for 2 weeks) inhibits tumor growth in a mouse xenograft model.
Products are for research use only. Not for human use.
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