ETP-46321
CAS 1252594-99-2 MFCD352594992
化学结构图
SMILES: CS(=O)(=O)N1CCN(Cc2cn3cc(-c4cnc(N)nc4)nc(N4CCOCC4)c3n2)CC1
化学属性
| Mol. Weight | 473.55 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | ETP-46321 |
|---|---|
| Formula | C20H27N9O3S |
| Synonym | ETP46321; ETP-46321; ETP 46321 |
| IUPAC Name | 5-(2-((4-(methylsulfonyl)piperazin-1-yl)methyl)-8-morpholinoimidazo[1,2-a]pyrazin-6-yl)pyrimidin-2-amine |
| InChIKey | OHKDVDMWRKFZRB-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H27N9O3S/c1-33(30,31)29-4-2-26(3-5-29)12-16-13-28-14-17(15-10-22-20(21)23-11-15)25-19(18(28)24-16)27-6-8-32-9-7-27/h10-11,13-14H,2-9,12H2,1H3,(H2,21,22,23) |
| Canonical SMILES | NC1=NC=C(C2=CN3C(C(N4CCOCC4)=N2)=NC(CN5CCN(S(=O)(C)=O)CC5)=C3)C=N1 |
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产品应用
- ETP-46321 is a potent and orally bioavailable PI3K α, δ inhibitor with potent biochemical and cellular activity and good pharmacokinetic properties (PK) after oral dosing. ETP-46321 PK/PD studies showed time dependent downregulation of AKT(Ser473) phosphorylation, which correlates with compound levels in tumor tissue and demonstrating to be efficacious in a GEMM mouse tumor model driven by a K-Ras(G12V) oncogenic mutation. Treatment with ETP-46321 resulted in significant tumor growth inhibition.
