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编 号:F754947
分子式:C18H20N4O2
分子量:324.38
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
RP-6306((S)-RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. RP-6306 shows a high degree of selectivity over other kinases in cellular binding assays. RP-6306 shows anticancer effects.

体内研究:
在 CCNE1 扩增的卵巢异种移植模型 (OVCAR3) 中,RP-6306(15, 50, and 300 ppm; oral; daily; for 21 days) 导致 OVCAR3 肿瘤生长显着减少且呈剂量依赖性 。Animal Model:OVCAR3-bearing mice
Dosage:15, 50, and 300 ppm (equivalent to approximately 3, 10, and 60 mg/kg/day)
Administration:Oral; daily; for 21 days
Result:Resulted in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth.

体外研究:
RP-6306(500nM;持续 24h)处理在 HCC1569 乳腺癌细胞系中诱导 pan-γH2AX,表明肿瘤衍生的 CCNE1 扩增也使细胞在 PKMYT1 抑制后容易受到 DNA 损伤诱导。RP-6306 处理会在 CCNE1 过表达细胞中选择性地意外激活 CDK1,从而促进正在进行 DNA 合成的细胞的早期有丝分裂。
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