2171388-28-4
Chemical Structure
RK-582
- CAS No.: 2171388-28-4
- Formula:C27H35FN6O3
- Molecular Weight:510.60
IUPAC Name: 6-((2R,6S)-2,6-dimethylmorpholino)-4-fluoro-1-methyl-1'-(8-methyl-4-oxo-1,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-2-yl)spiro[indoline-3,4'-piperidin]-2-one
InChIKey: KZUPFZKALLNBBV-CALCHBBNSA-N
SMILES: O=C(N1C)C2(CCN(C(NC3=C4CCCN3C)=NC4=O)CC2)C(C1=CC(N(C[C@@H]5C)C[C@H](O5)C)=C6)=C6F
Biological Activity: RK-582 is a tankyrase inhibitor, antitumor agent, and orally bioavailable growth inhibitor, with an IC50 of 36.1 nM against human tankyrase-1 and an IC50 of 39.2 nM against human tankyrase-2. In APC-mutated colorectal cancer cells, the sensitivity to RK-582 correlates with the level of active β-catenin, while drug resistance associates with PIK3CA mutation. RK-582 can be used for the research of colorectal cancer[1][2].
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RK-582 | 98.05% | RK-582 is a tankyrase inhibitor, antitumor agent, and orally bioavailable growth inhibitor, with an IC50 of 36.1 nM against human tankyrase-1 and an IC50 of 39.2 nM against human tankyrase-2. In APC-mutated colorectal cancer cells, the sensitivity to RK-582 correlates with the level of active β-catenin, while drug resistance associates with PIK3CA mutation. RK-582 can be used for the research of colorectal cancer. | ||||||||||||||||||||
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- [1]. Chen M, et al. APC/PIK3CA mutations and β-catenin status predict tankyrase inhibitor sensitivity of patient-derived colorectal cancer cells. Br J Cancer. 2024;130(1):151-162. [Content Brief]
- [2]. Shirai F, et al. Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer. J Med Chem. 2020;63(8):4183-4204. [Content Brief]
Keywords
