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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-ZSTK474
ZSTK474

Chemical Structure : ZSTK474

CAS No.: 475110-96-4

ZSTK474 (ZSTK 474, ZSTK 474)

货号: PC-45869Not For Human Use, Lab Use Only.

ZSTK474 (ZSTK-474) is a potent inhibitor of class I PI3K isoforms with IC50 of 17 nM, 53 nM, and 6 nM for p110β, p110γ, and p110δ, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ZSTK474 (ZSTK-474) is a potent inhibitor of class I PI3K isoforms with IC50 of 17 nM, 53 nM, and 6 nM for p110β, p110γ, and p110δ, respectively.
ZSTK474 (ZSTK474) shows potent antiproliferative activity against a panel of 39 human cancer cell lines with mean GI50 of 0.32 uM.
ZSTK474 (ZSTK474) is more effectively than that of LY294002 or wortmannin.
ZSTK474 (ZSTK474) induces apoptosis in OVCAR3 cells, and induces complete G1-phase arrest but not apoptosis in A549 cells at 10 uM.
ZSTK474 (ZSTK474) completely inhibits the growth of A549, PC-3, and WiDr xenografts in mice at 400mg/kg; and induces the regression of A549 xenograft tumors.

物理化学性质&存储条件

分子量 417.4125
分子式 C19H21F2N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Benzimidazole, 2-(difluoromethyl)-1-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-

参考文献

1. Yaguchi S, et al. J Natl Cancer Inst, 2006, 98(8), 545-556.

2. Kong D, et al. Cancer Sci, 2007, 98(10), 1638-1642.

3. Kong D, et al. Eur J Cancer, 2009, 45(5), 857-865.

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