ETP-46321
ETP-46321(ETP-46321)
CAS: 1252594-99-2
化学式: C20H27N9O3S
| 中文名 | ETP-46321 |
| 英文名 | ETP-46321 |
| 别名 | 化合物ETP-46321 |
| 英文别名 | CS-2500 ETP46321 ETP-46321 ETP 46321 5-(2-((4-methylsulfonylpiperazin-1-yl)methyl)-8-morpholinoimidazo[1,2-a]pyrazin-6-yl)pyrimidin-2-amine 2-Pyrimidinamine, 5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-8-(4-morpholinyl)imidazo[1,2-a]pyrazin-6-yl]- |
| CAS | 1252594-99-2 |
| 化学式 | C20H27N9O3S |
| 分子量 | 473.55 |
| 密度 | 1.59±0.1 g/cm3(Predicted) |
| 溶解度 | DMSO: ≥ 33 mg/mL |
| 酸度系数 | 5.86±0.30(Predicted) |
| 存储条件 | -20℃ |
| 产品用途 | ETP-46321 is a potent and orally bioavailable PI3K α, δ inhibitor with potent biochemical and cellular activity and good pharmacokinetic properties (PK) after oral dosing. ETP-46321 PK/PD studies showed time dependent downregulation of AKT(Ser473) phosphorylation, which correlates with compound levels in tumor tissue and demonstrating to be efficacious in a GEMM mouse tumor model driven by a K-Ras(G12V) oncogenic mutation. Treatment with ETP-46321 resulted in significant tumor growth inhibition. |
| 参考资料 展开查看 | 1: MartÃnez González S, Hernández AI, Varela C, RodrÃguez-ArÃstegui S, Lorenzo M, RodrÃguez A, Rivero V, MartÃn JI, Saluste CG, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán M, Alfonso P, GarcÃa-Serelde B, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Pastor J. Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. Bioorg Med Chem Lett. 2012 May 15;22(10):3460-6. doi: 10.1016/j.bmcl.2012.03.090. Epub 2012 Mar 29. PubMed PMID: 22520259. |
ETP-46321 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.112 ml | 10.559 ml | 21.117 ml |
| 5 mM | 0.422 ml | 2.112 ml | 4.223 ml |
| 10 mM | 0.211 ml | 1.056 ml | 2.112 ml |
| 5 mM | 0.042 ml | 0.211 ml | 0.422 ml |
最后更新：2024-01-02 23:10:35
ETP-46321 - 动物实验
BALB/C mice are treated daily with ETP-46321 (50 mg/kg, p.o.) for three weeks. Tumor volumes of four mice in each treatment group are measured and compared to the starting volume at the beginning of the treatment.
最后更新：2023-08-16 21:32:38
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