ETP-46321
- Product Name
- ETP-46321
- CAS No.
- 1252594-99-2
- Chemical Name
- ETP-46321
- Synonyms
- CS-2500;ETP-46321;ETP46321;ETP 46321;ETP-46321, 10 mM in DMSO;Inhibitor,ETP-46321,Phosphoinositide 3-kinase,ETP46321,inhibit,PI3K,ETP 46321;5-(2-((4-methylsulfonylpiperazin-1-yl)methyl)-8-morpholinoimidazo[1,2-a]pyrazin-6-yl)pyrimidin-2-amine;5-{2-[(4-methanesulfonylpiperazin-1-yl)methyl]-8-(morpholin-4-yl)imidazo[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]-
- CBNumber
- CB02715627
- Molecular Formula
- C20H27N9O3S
- Formula Weight
- 473.55
- MOL File
- 1252594-99-2.mol
ETP-46321 Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-3350
- Product name
- ETP-46321
- Purity
- 99.65%
- Packaging
- 5mg
- Price
- $320
- Updated
- 2021/12/16
- Product number
- CS-3350
- Product name
- ETP-46321
- Purity
- 99.65%
- Packaging
- 10mg
- Price
- $480
- Updated
- 2021/12/16
- Product number
- CS-3350
- Product name
- ETP-46321
- Purity
- 99.65%
- Packaging
- 50mg
- Price
- $1400
- Updated
- 2021/12/16
- Product number
- CS-3350
- Product name
- ETP-46321
- Purity
- 99.65%
- Packaging
- 100mg
- Price
- $2520
- Updated
- 2021/12/16
- Product number
- CD31004096
- Product name
- ETP-46321
- Purity
- 98+%
- Packaging
- 5mg
- Price
- $243
- Updated
- 2021/12/16
ETP-46321 Chemical Properties,Usage,Production
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)
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
ETP-46321 Preparation Products And Raw materials
Raw materials
Preparation Products
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