6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶

6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶

中文名称6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶
中文同义词6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶;MTOR抑制剂(WAY-600
英文名称WAY-600
英文同义词WAY-600;6-(1H-Indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine;6-(1H-indol-5-yl)-4-morpholino-1-(1-(pyridin-3-ylmethyl)piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidine;WAY-600;WAY 600;4-[6-(1H-indol-5-yl)-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-4-yl]morpholine;1H-Pyrazolo[3,4-d]pyrimidine, 6-(1H-indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-;WAY-600 USP/EP/BP
CAS号1062159-35-6
分子式C28H30N8O
分子量494.59
EINECS号
相关类别小分子抑制剂,天然产物;细胞生物学试剂;Inhibitors;Akt;mTOR;PI3K;PI3K/Akt/mTOR
Mol文件1062159-35-6.mol
结构式6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶 结构式

6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶 性质

密度1.43
储存条件Store at -20°C
溶解度溶于 DMSO > 10 mM
形态粉末
酸度系数(pKa)16.08±0.30(Predicted)

6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶 用途与合成方法

WAY-600 是有效,ATP 竞争型,选择性的 mTOR 抑制剂,抑制重组 mTOR 酶的 IC50 值为 9 nM。WAY-600 阻断 mTOR 复合物 1/2 (mTORC1/2) 组装和激活。

mTOR

9 nM (IC 50 )

mTORC1

mTORC2

PI3K alpha

1.96 μM (IC 50 )

PI3K gamma

8.45 μM (IC 50 )

WAY-600 exhibits a concentration-dependent and time-dependent inhibition of f HepG2 and Huh-7 cells viability. Following WAY-600 (1-1000 nM) treatment, the number of HepG2 cell colonies is dramatically decreased. Meanwhile, BrdU incorporation in HepG2 cells is also inhibited with WAY-600 treatment. WAY-600 dose-dependently increases the activity of caspase-3 and caspase-9 in HepG2 cells. WAY-600 disrupts assemble of mTORC1 (mTOR-Raptor association) and mTORC2 (mTOR-Rictor association). Activation of mTORC1 (indicated by p-S6K1 and p-4E-BP1) and mTORC2 is almost blocked by WAY-600 (100 nM).

Administration of WAY-600 (10 mg/kg, daily) inhibits HepG2 tumor growth in nude mice. Daily HepG2 tumor growth of WAY-600-administrated mice is significantly lower than that of vehicle control mice. Importantly, the in vivo anti-cancer activity by WAY-600 is further potentiated with the co-administration of MEK-162 (2.5 mg/kg, p.o. daily).

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-152726-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶
WAY-600
1062159-35-62mg1100元
2024/01/25HY-152726-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶
WAY-600
1062159-35-65mg1900元

6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶 上下游产品信息

"6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶"相关产品信息
SAM-315 N-[4-(2-溴-4,5-二氟苯氧基)苯基]-L-天冬酰胺 5-(苯磺酰基)-N-(哌啶-4-基)-2-(三氟甲基)苯磺酰胺 WAY-100635;WAY100635;WAY100635 WAY208466dihydrochloride 796854-35-8 MAY-262611 220460-92-4 7-溴-2-(4-羟基苯基)苯并[D]恶唑-5-醇 4-[6-[4-[(甲氧羰基)氨基]苯基]-4-(4-吗啉基)-1H-吡唑并[3,4-D]嘧啶-1-基]-1-哌啶羧酸甲酯 TENOVIN-1 培利替尼 KU-0063794 阿法替尼 卡奈替尼
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