| Identification | Back Directory | [Name]
ETP-46321 | [CAS]
1252594-99-2 | [Synonyms]
CS-2500
ETP-46321
ETP46321;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]- | [Molecular Formula]
C20H27N9O3S | [MOL File]
1252594-99-2.mol | [Molecular Weight]
473.55 |
| Chemical Properties | Back Directory | [density ]
1.59±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMSO: 10 mg/ml | [form ]
A solid | [pka]
5.86±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively. | [in vivo]
ETP-46321, is selected for in vivo studies based on its appealing pharmacokinetic profile in BALB-C mice, low in vivo Clearance (0.6 L/h/Kg) and good oral bioavailability (90%). ETP-46321 demonstrates a good pharmacokinetic profile in mice and is selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation, showing significant tumor growth inhibition, and reduction of the tumor metabolic activity as measured by positron emission tomography (PET) techniques[1]. | [IC 50]
p110α: 2.3 nM (Ki); PI3Kα-E545K: 1.77 nM (Ki); PI3Kα-E542K: 1.89 nM (Ki); PI3Kα-H1047R: 2.33 nM (Ki); p110δ: 14.2 nM (Ki); p110β: 170 nM (Ki); p110γ: 179 nM (Ki) | [storage]
Store at -20°C | [References]
[1] Martínez González S, et al. 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 |
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