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Formula | C22H26F2N4O2 |
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Molecular Weight | 416.46 | CAS No. | 2171386-10-8 | |
Solubility (25°C)* | In vitro | DMSO | 83 mg/mL (199.29 mM) | |
Water | ˂1 mg/mL | |||
Ethanol | ˂1 mg/mL | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM. | ||||
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In vitro | RK-287107 is a novel tankyrase-specific inhibitor that inhibits tankyrase-1 and -2. RK-287107 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. Consistently, 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.[1] |
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In vivo | Intraperitoneal or oral administration of RK-287107 suppresses COLO-320DM tumor growth in NOD-SCID mice. RK-287107 suppresses the Wnt/β-catenin pathway and tumor growth of the xenografted COLO-320DM cells in vivo.[1] |
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