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Chemical Structure : RK-287107
CAS No.: 2171386-10-8
Catalog No.: PC-35703Not For Human Use, Lab Use Only.
RK-287107 (RK287107) is a novel potent, tankyrase-specific inhibitor with IC50 of 14.3 and 10.6 nM for tankyrase-1 (TNKS1) and tankyrase-2 (TNKS2) respectively, shows no activity against PARP-1.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $158 | In stock | |
| 10 mg | $258 | In stock | |
| 25 mg | $428 | In stock | |
| 50 mg | $728 | In stock | |
| 100 mg | Get quote |
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RK-287107 (RK287107) is a novel potent, tankyrase-specific inhibitor with IC50 of 14.3 and 10.6 nM for tankyrase-1 (TNKS1) and tankyrase-2 (TNKS2) respectively, shows no activity against PARP-1.
RK-287107 shows 4-8-fold more potency than G007-LK; causes Axin2 accumulation and downregulates β-catenin, T-cell factor/lymphoid enhancer factor reporter activity and the target gene expression in colorectal cancer cells harboring the shortly truncated APC mutations.
RK-287107 inhibits the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells but not the APC-wild (β-catenin-independent) colorectal cancer RKO cells.
RK-287107 suppresses COLO-320DM tumor growth in NOD-SCID mice (intraperitoneal or oral administration).
| M.Wt | 416.473 | |
| Formula | C22H26F2N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-(4,6-difluoro-1-(2-hydroxyethyl)spiro[indoline-3,4'-piperidin]-1'-yl)-5,6,7,8-tetrahydroquinazolin-4(3H)-one |
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1. Mizutani A, et al. Cancer Sci. 2018 Sep 20. doi: 10.1111/cas.13805.
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