Eganelisib

SKU: orb1301794

Description

Eganelisib

Research Area

Signal Transduction

Key Properties

• CAS Number: 1693758-51-8
• MW: 528.56
• Purity: 99.04%
• Formula: C₃₀H₂₄N₈O₂
• SMILES: C[C@H](NC(=O)c1c(N)nn2cccnc12)c1cc2cccc(C#Cc3cnn(C)c3)c2c(=O)n1-c1ccccc1
• Target: PI3K
• Solubility: DMSO:20 mg/mL (37.84 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.89 mM)

Bioactivity

• Target IC50:
  PI3Kα:3.2 μM|PI3Kβ:3.5 μM|PI3Kγ:16 nM
• In Vivo:
  IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo.
• In Vitro:
  IPI-549 sensitizes doxorubicin-resistant SW620/Ad300 cells to P-glycoprotein (P-gp) substrates, such as paclitaxel (IC50s = 710 and 6.7 nM for paclitaxel alone and in combination with IPI-549, respectively), and increases the level of intracellular paclitaxel in SW620/Ad300 cells.
• Animal Research:
  SW620 (4 X 10^6 ) and SW620/Ad300 (5 X 10^6 ) cells were injected subcutaneously at the flank near the armpits of athymic nude mice. When the subcutaneous tumors were approximately 0.5 x 0.5 cm in size (day 0), the mice were randomized into four treatment groups. The vehicle used to deliver the IPI-549 and paclitaxel by intraperitoneal (i.p.) injection was ethanol/Cremophor ELP/saline (10%/10%/80%). Group one received the vehicle only; group two received vehicle plus 3 mg/kg IPI-549; group three received vehicle plus 15 mg/kg paclitaxel; group four, the combination group, received vehicle plus 3 mg/kg IPI-549 one h prior to administration of vehicle plus 15 mg/kg paclitaxel. The drug doses were administered every 3 days with a total of 4 doses. Tumor volume was measured using calipers, and body weights were recorded prior to each dosing.

Storage & Handling

• Storage: store at low temperature | 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

Phosphoinositide 3-kinase, PI3Kγ, PI3Kβ, PI3Kα, PI3K, Inhibitor, IPI 549, IPI549, IPI-549, inhibit, Eganelisib

Compound Identifiers

PubChem CID

91933883