PI3Kδ-IN-10 NEW
| Price | $1520 | $1980 | $2500 |
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: PI3Kδ-IN-10 | CAS No.: 2409725-49-9 |
| Supply Ability: 10g | Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | PI3Kδ-IN-10 |
| Description | PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor (IC50 = 2 nM) that robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models. |
| In vitro | PI3Kδ-IN-10 (compound 9x) significantly inhibits cell proliferation in HCC (Hepatocellular Carcinoma) cell lines (Bel-7402, HepG2, Hep3B) with IC50 values between 0.53 and 1.36 μM over 72 hours at concentrations up to 10 μM. At concentrations up to 50 μM for 24 hours, it also increases cleaved PARP and cleaved caspase-3 expression and decreases phosphorylation of Akt at Ser473 and Thr308 in a dose-dependent manner, indicating apoptosis induction and reduced Akt 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. |
| Storage | Shipping with blue ice. |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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United States- Since: 2011-01-07
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