PF-06939999(PRMT5-IN-3)是一种口服有效的、S-腺苷甲硫氨酸(SAM)竞争性的蛋白精氨酸甲基转移酶5(PRMT5)抑制剂,在A427细胞中抑制对称二甲基精氨酸(SDMA)蛋白表达的IC50值为1.1nM,并表现出抗肿瘤活性。
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-25~-15℃避光保存,有效期3年。
[1] Jensen-Pergakes K, Tatlock J, Maegley KA, McAlpine IJ, McTigue M, Xie T, Dillon CP, Wang Y, Yamazaki S, Spiegel N, Shi M, Nemeth A, Miller N, Hendrickson E, Lam H, Sherrill J, Chung CY, McMillan EA, Bryant SK, Palde P, Braganza J, Brooun A, Deng YL, Goshtasbi V, Kephart SE, Kumpf RA, Liu W, Patman RL, Rui E, Scales S, Tran-Dube M, Wang F, Wythes M, Paul TA. SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance. Mol Cancer Ther. 2022 Jan;21(1):3-15. doi: 10.1158/1535-7163.MCT-21-0620. Epub 2021 Nov 4. PMID: 34737197.





