PI3Kα-IN-9
Catalog No. T61654 CAS
2715287-67-3
PI3Kα-IN-9 (compound 27) is a highly specific, orally active, and long-lasting inhibitor of PI3Kα, demonstrating potent inhibitory effects with IC50 values of 4.4, 128, 146, and 153 nM against PI3Kα, PI3Kγ, PI3Kδ, and PI3Kβ, respectively. Additionally, PI3Kα-IN-9 exhibits antiproliferative properties and effectively induces apoptosis. Given its characteristics, PI3Kα-IN-9 holds great potential for cancer research [1].
All TargetMol products are for research or drug registration purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose in violation of laws and regulations.
PI3Kα-IN-9, CAS 2715287-67-3
Please contact us for prices and availability for the specification of product you are interested at.
Product consultation
Contact us for more batch information
Biological Description
Chemical Properties
Storage
& Solubility Information
Description |
PI3Kα-IN-9 (compound 27) is a highly specific, orally active, and long-lasting inhibitor of PI3Kα, demonstrating potent inhibitory effects with IC50 values of 4.4, 128, 146, and 153 nM against PI3Kα, PI3Kγ, PI3Kδ, and PI3Kβ, respectively. Additionally, PI3Kα-IN-9 exhibits antiproliferative properties and effectively induces apoptosis. Given its characteristics, PI3Kα-IN-9 holds great potential for cancer research [1]. |
In vitro |
PI3Kα-IN-9 (compound 27) demonstrated antiproliferative effects and induced apoptosis across various cancer cell lines, including gastric, ovarian, prostate, breast (with a focus on triple-negative), liver, multiple myeloma, chronic myeloid leukemia, glioma, and acute lymphoblastic leukemia, when administered at concentrations ranging from 0-8 μM over 72 hours. Specifically, in MGC-803 gastric cancer cells, PI3Kα-IN-9 reduced the expression of PI3Kα protein and its downstream proteins, p-AKT and p-P70S6 K. Cell viability assays showed that this compound inhibited the growth of these cancer cells, yielding IC 50 values between 0.43 to 1.33 μM. Further apoptosis analysis in MGC-803 cells revealed a dose-dependent increase in apoptotic cell percentage from 12.07% to 61.69% following treatment with varying concentrations of 0, 2, 4, and 8 μM over 36 hours.
|
In vivo |
PI3Kα-IN-9 (compound 27) demonstrated favorable pharmacokinetics and therapeutic potential in preclinical studies. Administered to male Sprague-Dawley rats at doses of 1-10 mg/kg, either orally (p.o.) or intravenously (i.v.) for 24 hours, the compound exhibited notable stability (T 1/2 >10 h) and high bioavailability (130%) [1]. Further evaluation in male BALB/c nude mice at a dose of 30 mg/kg, administered orally once daily for 3 weeks, revealed its significant antitumor activity accompanied by minimal cytotoxicity [1]. The pharmacokinetic analysis in rats highlighted a dose-dependent increase in exposure, with parameters indicating efficient absorption and sustained plasma levels. In the tumor inhibition study with mice, the compound achieved a tumor growth inhibition (TGI) rate of 41.5%, underscoring its potential as a therapeutic agent with favorable pharmacokinetic properties and efficacy in cancer models.
|
Molecular Weight |
383.4
|
Formula |
C18H21N7O3 |
CAS No. |
2715287-67-3 |
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
More
In vivo Formulation Calculator (Clear solution)
Step One: Enter information below
Step Two: Enter the in vivo formulation
Calculator
Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
bottom
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Keywords
PI3Kα-IN-9
2715287-67-3
inhibitor
inhibit