RP-6306

MCE 國際站：RP-6306

CAS：2719793-90-3

品牌：MedChemExpress (MCE)

存儲條件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：RP-6306是一種PKMYT1抑制劑，提取自WO2021195781A1化合物182。RP-6306可用于癌癥的研究
^[1]。

體外：RP-6306（500nM；持續(xù) 24h）處理在 HCC1569 乳腺癌細胞系中誘導(dǎo) pan-γH2AX，表明腫瘤衍生的 CCNE1 擴增也使細胞在 PKMYT1 抑制后容易受到 DNA 損傷誘導(dǎo)
[2]。 RP-6306 處理會在 CCNE1 過表達細胞中選擇性地意外激活 CDK1，從而促進正在進行 DNA 合成的細胞的早期有絲分裂
[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內(nèi)：在 CCNE1 擴增的卵巢異種移植模型 (OVCAR3) 中，RP-6306 (15, 50, and 300 ppm; oral; daily; for 21 days) 導(dǎo)致 OVCAR3 腫瘤生長顯著減少且呈劑量依賴性
[1] 。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: OVCAR3-bearing mice
[1] 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. Clinical Trial

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研究領(lǐng)域：Cell Cycle/DNA Damage

作用靶點：Wee1

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參考文獻：
[1]. Janek Szychowski, et al. Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem. 2022 Aug 11;65(15):10251-10284.
[2]. David Gallo, et al. CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. Nature. 2022 Apr;604(7907):749-756.