ZSTK474 is an ATP-competitive pan-class IPI3Kinhibitor withIC₅₀s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα,PI3Kβ,PI3KδandPI3Kγ, respectively.

Lineweaver-Burk plot analysis revealed that ZSTK474 inhibits all four PI3K isoforms in an ATP-competitive manner. The K_ivalues determined for the four PI3K isoforms showed that ZSTK474 inhibited the PI3Kδ isoform most effectively with a K_iof 1.8 nM, whereas the other isoforms are inhibited with 4-10-fold higher K_ivalues. Therefore, ZSTK474 should be regarded as a pan-PI3K inhibitor. We also determined the IC₅₀values for inhibiting the four PI3K isoforms with ZSTK474 and LY294002. The IC₅₀values of ZSTK474 (16, 44, 4.6 and 49 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively) are shown to be consistent with the K_ivalues (6.7, 10.4, 1.8 and 11.7 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively), which further supported the idea that ZSTK474 inhibits PI3Kδ most potently. Even at a concentration of 100 μM, ZSTK474 inhibits mTOR activity rather weakly^[1].

In mice subjected to MCAO, treatment with ZSTK474 is tested at dosages of 50, 100, 200, and 300 mg/kg. Since the 200 mg/kg dose produces significant improvement and no obvious toxic effects (P<0.01), mice are treated with ZSTK474 at a dose of 200 mg/kg/day daily for three post-MCAO days during the remaining experiments of this study. Neurological function is examined in mice suffered from MCAO followed by 24, 48, and 72 h of reperfusion. In the ZSTK474 group, neurological function scores are significantly better than the control group except the corner test^[2].

417.41

Solid

C₁₉H₂₁F₂N₇O₂

475110-96-4

Room temperature in continental US; may vary elsewhere.

DMSO : 2 mg/mL(4.79 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

• 1.

  ZSTK474 is suspended in 5% hydroxypropyl cellulose^[3].