ETP-46321

小分子

ETP-46321

E647504-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with K iapp s of 2.3 and 14.2 nM, respectively. In Vitro ETP-46321 is selected to be screened against other PI3K isoforms. ETP-46321 is more potent against isoform α (K iapp =2.3 nM). ETP-4632, has been profiled and shown to be a potent PI3K α and δ inhibitor, highly selective versus mTOR and 288 representative kinases. ETP-46321 is also tested against three of the p110α mutant enzymes detected in human cancers (E542K, E545K and H1047R), being equipotent against these mutants when compared to the wild type protein (K iapp =2.33, 1.77 and 1.89 nM for PI3Kα-H1047R, PI3Kα-E545K and PI3Kα-E542K, respectively). ETP-46321 inhibits the phosphorilation of AKT in U2OS cell line with an IC 50 of 8.3 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target: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)

ETP-46321 是一种强效的口服生物活性 PI3Kα 和 PI3Kδ 抑制剂，其 K iapp s 分别为 2.3 和 14.2 nM。

1252594-99-2

C20H27N9O3S

473.55 g/mol

46927938

CS(=O)(=O)N1CCN(CC1)CC2=CN3C=C(N=C(C3=N2)N4CCOCC4)C5=CN=C(N=C5)N

5-[2-[(4-methylsulfonylpiperazin-1-yl)methyl]-8-morpholin-4-ylimidazo[1,2-a]pyrazin-6-yl]pyrimidin-2-amine

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)

OHKDVDMWRKFZRB-UHFFFAOYSA-N

CS(=O)(=O)N1CCN(CC1)CC2=CN3C=C(N=C(C3=N2)N4CCOCC4)C5=CN=C(N=C5)N

46927938

ETP-46321

DMSO : ≥ 33 mg/mL (69.69 mM)

1

11

5

473.196 Da

473.196 Da

143.000 Ų

33

0

746

0

1

-0.7