PI3Kα-IN-9

Research use only, not for human use.

PI3Kα-IN-9 is an orally available, selective and potent PI3Kα inhibitor with antiproliferative activity, inhibits PI3Kα, PI3Kγ, PI3Kδ, and PI3Kβ, induces apoptosis, and can be used in the study of cancer.

PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research.

PI3Kα-IN-9 (compound 27) (0-8 μM; 72 hours; cancer cell lines) has antiproliferative activity and induces apoptosis.PI3Kα-IN-9 (compound 27) (0-8 μM; MGC-803 cells) down-regulates the expression of PI3Kα protein, the proteins of PI3K downstream, p-AKT and p-P70S6 K.Cell Viability Assay Cell Line:MGC-803 (gastric cancer), SKOV-3 (ovarian cancer), PC-3(prostate cancer), MCF-7 (breast cancer), MDA-MB-231 (triple-negative breast cancer), HepG2 (liver cancer), RPMI8226 (multiple myeloma), K562 (chronic myeloid leukemia), U251 (glioma) and MOLT-4 (acute lymphoblastic leukemia) cell lines Concentration:0-2 μM Incubation Time:72 hours Result:Inhibited the growth of a variety of cancer cells with IC50 values ranging from 0.43 to 1.33 μM.Apoptosis Analysis Cell Line:MGC-803 cells Concentration:0, 2, 4 and 8 μM Incubation Time:36 hours Result:Increased the percentage of apoptotic cells from 12.07 to 61.69% in a dose-dependent manner.

PI3Kα-IN-9 (compound 27) (1-10 mg/kg; p.o. and i.v.; for 24 hours; male Sprague-Dawley rat) has favorable stability (T1/2>10 h) and high bioavailability (130%).PI3Kα-IN-9 (compound 27) (30 mg/kg; p.o.; daily, for 3 weeks; male BALB/c nude mice) has antitumor activity and low cytotoxicity.Animal Model:Male Sprague-Dawley ratDosage:1 and 10 mg/kg Administration:Oral administration and intravenous injection.Animal Model:Male BALB/c nude mice Dosage:30 mg/kg Administration:Oral administration; daily, for 3 weeks Result:Inhibited tumor growth with a tumor growth inhibition (TGI) rate of 41.5%.

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Apoptosis

Apoptosis

Apoptosis | PI3K

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2715287-67-3

383.4

C18H21N7O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (260.82 mM; Ultrasonic (<80°C)

N1=C(N=C(N=C1N2CCOCC2)N3CCOCC3)C4=CC=C5OC(=NC5=C4)N

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(-20℃)

With Ice Pack

≥ 2 years