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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 6-8 weeks | |
50 mg | $1,980 | 6-8 weeks | |
100 mg | $2,500 | 6-8 weeks |
Description | PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor (IC50= 2 nM). In hepatocellular carcinoma models, PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis. |
In vitro | PI3Kδ-IN-10 (compound 9x), at concentrations ranging from 0 to 10 μM over 72 hours, significantly inhibits cell proliferation in HCC (Hepatocellular Carcinoma) cell lines, including Bel-7402, HepG2, and Hep3B, with IC50 values between 0.53 and 1.36 μM. Furthermore, when applied at concentrations from 0 to 50 μM for 24 hours, PI3Kδ-IN-10 notably increases the expression of cleaved PARP and cleaved caspase-3 and decreases Akt phosphorylation levels at Ser473 and Thr308 in a dose-dependent manner. This indicates not only an inhibition of cell proliferation but also an induction of apoptosis and a reduction in Akt signaling pathway activity in HCC cell lines. |
In vivo | PI3Kδ-IN-10 demonstrated favorable pharmacokinetics and efficacy in female Balb/c (nu/nu) mice, achieving an acceptable half-life (T 1/2), moderate distribution volume, and oral bioavailability when administered at 5 mg/kg orally (PO) and 1 mg/kg intravenously (IV). Additionally, 12-day intravenous treatments at dosages of 40 mg/kg and 20 mg/kg effectively reduced the growth of liver cancer xenografts, with inhibition ratios of 76.02% and 59.15%, respectively. This compound's pharmacokinetic parameters further illustrate its potential, showing significant area under the curve (AUC), volume of distribution adjusted by bioavailability (Vz/F), and drug absorption times (T max) across the examined dosages and methods of administration, underscoring its efficacy in the tested animal model. |
Molecular Weight | 405.84 |
Formula | C19H16ClN9 |
Cas No. | 2409725-49-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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