PI3K-IN-1 NEW
| Price | $30 | $43 | $68 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: PI3K-IN-1 | CAS No.: 1349796-36-6 |
| Purity: 98% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | PI3K-IN-1 |
| Description | PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR. |
| Cell Research | Cells are treated with XL765 24 hours after plating and harvested for apoptosis or autophagy assays at 24, 48, or 72 hours after XL765 treatment. Apoptosis is determined by total percentage of annexin V-positive cells by fluorescence-activated cell sorting (FACS). Acidic vesicular organelles (AVOs) are detected in XL765-treated cells by vital staining with acridine orange. The degree of AVO formation is expressed as fold increase of acridine orange fluorescence intensity (FL3) in XL765-treated cells versus control cells. (Only for Reference) |
| Kinase Assay | Radioligand Binding Assays: Each tube in the A3 AR competitive binding assay contains 100 μL of membrane suspension (20 μg of protein), 50 μL of [125I]4-amino-3-iodobenzyl)adenosine-5′-N-methyluronamide (0.5 nM), and 50 μL of increasing concentrations of the test ligands in Tris-HCl buffer (50 mM, pH 7.4) containing 10 mM MgCl2 and 1 mM EDTA. Nonspecific binding is determined using 10 mM 5′-N-ethylcarboxamidoadenosine in the buffer. The mixtures are incubated at 25°C for 60 min. Binding reactions are terminated by filtration through Whatman GF/B filters under reduced pressure using a MT-24 cell harvester. Filters are washed three times with 9 mL of ice-cold buffer. Radioactivity is determined using a Beckman γ-counter, and the percent inhibition is calculated. |
| In vitro | In the GBM 39-luc xenografted nude mice model, oral administration of XL765 was able to inhibit the growth of tumor cells while also enhancing survival rates. In the BxPC-3 xenograft mouse model, combining XL765 (30 mg/kg) with chloroquine (50 mg/kg) demonstrated the capability to suppress tumor cell growth. |
| In vivo | XL765 inhibits Class I PI3K, specifically targeting p110α (IC50=39 nM), p110β (IC50=113 nM), p110γ (IC50=9 nM), and p110δ (IC50=43 nM). It also suppresses mTOR (IC50 = 157 nM) by significantly reducing the phosphorylation of mTOR targets, including S6, S6K, and 4EBP1. In MIAPaCa-2 cells, treatment with XL765 leads to the accumulation of autophagic vacuoles. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 1 mg/ml, Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
| Keywords | Phosphoinositide 3-kinase | muscle | XL-147 derivative 1 | cancer | PI-3K-IN-1 | SRC | SAR 245409 | PI3K | XL-765 | fibrosis | inhibit | extraocular | thyroid | PI3K IN 1 | Inhibitor | PI3K-IN-1 | SAR-245409 | ophthalmopathy | XL 765 | PI3KIN1 | gene |
| Inhibitors Related | Myricetin | Erucic acid | Sapanisertib | (2S,3R,4S)-4-Hydroxyisoleucine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Quercetin | GDC0084 | Quercetin Dihydrate | Apilimod | LY294002 | Idelalisib |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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