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.
For research use only. We do not sell to patients.
| Name | ETP-46321 |
|---|---|
| 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 |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | crystalline solid |
|---|---|
| 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 |