AZD 6482

SKU: orb1301085

Description

AZD 6482 (KIN-193) is a highly potent and selective p110β/PI3Kβ inhibitor, demonstrating IC50 values of 0.69 nM and 10 nM, respectively. It effectively suppresses AKT signaling and inhibits tumor growth in models driven by p110β activation or PTEN deficiency, making it a valuable tool for oncology research in both cellular and animal studies.

Research Area

Cell Biology, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 1173900-33-8
• MW: 408.45
• Purity: 99.95% (May vary between batches)
• Formula: C₂₂H₂₄N₄O₄
• SMILES: C[C@@H](Nc1ccccc1C(O)=O)c1cc(C)cn2c1nc(cc2=O)N1CCOCC1
• Target: DNA-PK,Autophagy,PI3K
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.9 mM);DMSO:45 mg/mL (110.17 mM)

Bioactivity

• Target IC50:
  PI3Kα:136 nM|DNA-PK:53.7 nM|PI3Kβ:10 nM|hVps34:3390 nM|PI3Kγ:47.8 nM|mTOR:3930 nM|p110β:0.69 nM|PI3Kδ:13.6 nM|PI4Kα:8830 nM|PI3KC2β:54.1 nM
• In Vivo:
  METHODS: Mice with HCC70, PC3, and HCC1954 xenograft tumors were treated with AZD 6482 (KIN-193) (20 mg/kg, i.p., twice daily) or GDC-0941 (150 mg/kg, orally, once daily). Study the in vivo effects of KIN-193 on PTEN-deficient tumors. RESULTS AZD 6482 significantly inhibited tumor growth of HCC70 and PC3 tumors but failed to block the growth of HCC1954 tumors.
• In Vitro:
  METHODS: U87 and U118 cells were treated with AZD 6482 (KIN-193) (0.625, 1.25, 2.5, 5, 10, 20, 40 μM, 48 hours), and CCK8 was used to measure its inhibitory effect on the proliferation of U87 and U118 cells. RESULTS AZD 6482 inhibited the viability of both cell lines in a dose-dependent manner, with U118 cells being more sensitive than U87 cells, with IC50 values ​​of 7.989 and 9.061 μM, respectively.
• Cell Research:
  For assay of washed platelet aggregation (WPA), the platelet pellets are isolated from human blood and re-suspended to 2 × 1015/L in Tyrodes buffer (TB) containing 1 μM hirudin and 0.02 U/mL apyrase. Then, the platelet suspension is left to rest at room temperature for 30 min. Just prior to time for assay, CaCl2 is added to a final concentration of 2 mM. AZD6482, dissolved in DMSO, is added to a 96-well plate prior to the addition of the washed platelet suspension. The platelet suspension is preincubated with AZD6482 for 5 min. Light absorption at 650 nm is recorded before and after a 5 min plate shake and referred to as recording 0 (R0) and Rl. A mouse anti-human CD9 antibody is added (at a donor specific concentration) to each well prior to next 10 min plate shake and light absorption recording; R2. For data analysis, light absorbance in wells with TB are subtracted from all readings before percent aggregation is calculated according the formula: [(R1-R2)/R1] × 100 = % aggregation. Spontaneous aggregation or pro-aggregatory effect of the inhibitor is evaluated by the same formula, [(R0-Rl)/R0] × 100 = % aggregation. IC50 values are calculated according to the equation, y = {a+[(b-a)/(l+(x/IC50)s)]}, where y = % inhibition; a = 0%; b = 100%; s = the slope of the concentration-response curve; x = AZD6482 concentration. (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

Phosphoinositide 3-kinase, PI3Kβ, PI3Kγ, PI3Kδ, PI3K, PI3Kα, KIN193, KIN-193, KIN 193, Inhibitor, inhibit, AZD 6482, AZD6482, AZD-6482, Autophagy, DNA-PK, DNAPK

Compound Identifiers

PubChem CID

44137675