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ZSTK474
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ZSTK474图片
CAS NO:475110-96-4
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议

产品介绍
ZSTK474 是一种 ATP 竞争性的泛 I 类PI3K抑制剂,抑制 PI3Kα,PI3Kβ,PI3Kδ 和 PI3Kγ,IC50分别为 16 nM,44 nM,4.6 nM 和 49 nM。
生物活性

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

IC50& Target[2]

PI3Kδ

4.6 nM (IC50)

PI3Kα

16 nM (IC50)

PI3Kβ

44 nM (IC50)

PI3Kγ

49 nM (IC50)

Autophagy

 

体外研究
(In Vitro)

Lineweaver-Burk plot analysis revealed that ZSTK474 inhibits all four PI3K isoforms in an ATP-competitive manner. The Kivalues determined for the four PI3K isoforms showed that ZSTK474 inhibited the PI3Kδ isoform most effectively with a Kiof 1.8 nM, whereas the other isoforms are inhibited with 4-10-fold higher Kivalues. 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 Kivalues (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].

体内研究
(In Vivo)

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].

Clinical Trial
分子量

417.41

性状

Solid

Formula

C19H21F2N7O2

CAS 号

475110-96-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3957 mL11.9786 mL23.9573 mL
5 mM---------
10 mM---------
*

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。

In Vivo:
  • 1.

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