PI3K-IN-1

SKU: orb1307368

Description

PI3K-IN-1

Research Area

Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 1349796-36-6
• MW: 599.66
• Purity: 97.07%
• Formula: C₃₁H₂₉N₅O₆S
• SMILES: COc1cc(Nc2nc3ccccc3nc2NS(=O)(=O)c2ccc(NC(=O)c3ccc(OC)c(C)c3)cc2)cc(OC)c1
• Target: DNA-PK,PI3K
• Solubility: DMSO:1 mg/mL (1.67 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.67 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PI3Kγ:9 nM|PI3Kβ:113 nM|DNA-PK:150 nM|PI3Kα:39 nM|PI3Kδ:43 nM
• 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.
• 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PI3Kγ, PI3Kβ, PI3Kδ, PI3Kα, PI3K, PI3K IN 1, PI3KIN1, PI-3K-IN-1, PI3K-IN-1, XL 765, XL-147 derivative 1, XL765, XL-765, thyroid, SAR245409, SAR-245409, SAR 245409, Voxtalisib Analogue, DNA-PK, DNAPK, fibrosis, extraocular, ophthalmopathy

Compound Identifiers

PubChem CID

91895223