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ETP-45658

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Chemical Structure| 1198357-79-7 同义名 : -
CAS号 : 1198357-79-7
货号 : A952617
分子式 : C16H17N5O2
纯度 : 99%+
分子量 : 311.339
MDL号 : MFCD29081201
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(802.98 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 ETP-45658 is a potent PI3K nhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 had modest, but significant activity toward the class IV PI3-related kinase mTOR and DNA PK with IC50 values of 152 nM and 70.6 nM, respectively. ETP-45658 inhibits the proliferation of MCF7, PC3, 786-O, HTC116, and U251 cells, with EC50s of 0.48 μM, 0.49 μM, 2.62 μM, 3.53 μM, and 5.56 μM, respectively. Treatment with ETP-45658 at 10μM for 4h decreased in the phosphorylation of FOXO3a, Gsk3-β and p70 S6K in U2OS cells. ETP-45658 was a potent inducer of GFP-FOXO nuclear translocation with EC50 value of 45 nM. Treatment with ETP-45658 from 5 nM to 11.1μM. 11.1μM for 1 h induced a dose-dependent increase of GFP-FOXO nuclear translocation in U2foxRELOC cells. Treatment with ETP-45658 at 10μM for 24 h induced a clear G1 arrest of PC3 cells. Treatment with ETP-45658 at 10 μM for 1h decreased the expression of cyclin D1 and p-Akt on serine 473 in U2OS cells[1]. ETP-45658 potently inhibited cell proliferation within a broad range of human cancer cells, most potently suppressing the growth of breast cancer cells via inhibiting cell cycle[2]. ETP 45658 also reduced glucolipotoxicity-induced β-cell death. It decreased markers of glucolipotoxicity including caspase activation, mitochondrial depolarization, and increased calcium flux[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.06mL

3.21mL

1.61mL

32.12mL

6.42mL

3.21mL
参考文献

[1]Link W, Oyarzabal J, Serelde BG, Albarran MI, Rabal O, Cebriá A, Alfonso P, Fominaya J, Renner O, Peregrina S, Soilán D, Ceballos PA, Hernández AI, Lorenzo M, Pevarello P, Granda TG, Kurz G, Carnero A, Bischoff JR. Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. J Biol Chem. 2009 Oct 9;284(41):28392-28400.

[2]Hill R, Kalathur RK, Callejas S, Colaço L, Brandão R, Serelde B, Cebriá A, Blanco-Aparicio C, Pastor J, Futschik M, Dopazo A, Link W. A novel phosphatidylinositol 3-kinase (PI3K) inhibitor directs a potent FOXO-dependent, p53-independent cell cycle arrest phenotype characterized by the differential induction of a subset of FOXO-regulated genes. Breast Cancer Res. 2014 Dec 9;16(6):482.

[3]Small JC, Joblin-Mills A, Carbone K, Kost-Alimova M, Ayukawa K, Khodier C, Dancik V, Clemons PA, Munkacsi AB, Wagner BK. Phenotypic Screening for Small Molecules that Protect β-Cells from Glucolipotoxicity. ACS Chem Biol. 2022 May 20;17(5):1131-1142.