AZD 6482

SKU: orb1301085

Description

AZD 6482

Research Area

Cell Biology, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 1173900-33-8
• MW: 408.45
• Purity: 99.87%
• Formula: C₂₂H₂₄N₄O₄
• SMILES: C[C@@H](Nc1ccccc1C(O)=O)c1cc(C)cn2c1nc(cc2=O)N1CCOCC1
• Target: PI3K,Autophagy,DNA-PK
• 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). Stud 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 bloc 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 o the proliferation of U87 and U118 cells. Results AZD 6482 inhibite 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 o 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 accordin the formula: [(R1-R2)/R1] × 100 = % aggregation. Spontaneous aggregation or pro-aggregatory effect o the inhibitor is evaluated b 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 o 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.
• 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