RP-6306是一种 PKMYT1 抑制剂 ｜ MedChemExpress (MCE)

RP-6306

CAS：2719793-90-3

品牌：MedChemExpress (MCE)

存储条件：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是一种PKMYT1抑制剂，提取自专利WO2021195781A1化合物182。RP-6306可用于癌症的研究[1]。

体外：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[2]。 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[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：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[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

参考文献：

[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.