ETP-46321 is a potent and orally bioavailable PI3K / inhibitor with IC50 of 2.3/14.2 nM for p110/p110; exhibits potency on mutated p110(IC50=1.77-2.33 nM, p110a E542K; E545K; H1047R).
ETP-46321, has been pro?led and shown to be a potent PI3K a and d inhibitor, highly selective versus mTOR and 288 representative kinases. The compound demonstrated a good pharmacokinetic profile in mice and was selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-Ras G12V oncogenic mutation, showing significant tumor growth inhibition (ca. 51%), and reduction of the tumor metabolic activity as measured by PET techniques.
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Name | ETP-46321 |
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Iupac Chemical Name | ETP-46321 |
Synonyms | ETP 46321; ETP46321 |
Molecular Formula | C20H27N9O3S |
Molecular Weight | 473.55 |
InChiKey | |
InChi | |
CAS Number | 1252594-99-2 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Formulation | crystalline solid |
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Purity | 98% |
Storage | 3 years -20ºCpowder |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |