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1062159-35-6

中文名稱 6-(1H-吲哚-5-基)-4-(4-嗎啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶
英文名稱 WAY-600
CAS 1062159-35-6
分子式 C28H30N8O
分子量 494.59
MOL 文件 1062159-35-6.mol
更新日期 2025/01/07 08:45:03
1062159-35-6 結(jié)構(gòu)式 1062159-35-6 結(jié)構(gòu)式

基本信息

中文別名
MTOR抑制劑(WAY-600
6-(1H-吲哚-5-基)-4-(4-嗎啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶
英文別名
WAY-600
WAY-600
WAY 600
WAY-600 USP/EP/BP
6-(1H-indol-5-yl)-4-morpholino-1-(1-(pyridin-3-ylmethyl)piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidine
4-[6-(1H-indol-5-yl)-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-4-yl]morpholine
6-(1H-Indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine
1H-Pyrazolo[3,4-d]pyrimidine, 6-(1H-indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-
所屬類別
生物化工:mTOR 抑制劑

物理化學性質(zhì)

密度1.43
儲存條件-20°C儲存
溶解度Soluble in DMSO > 10 mM
酸度系數(shù)(pKa)16.08±0.30(Predicted)
形態(tài)粉末
顏色White to off-white
6-(1H-吲哚-5-基)-4-(4-嗎啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-152726-(1H-吲哚-5-基)-4-(4-嗎啉基)-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
2024/11/08HY-152726-(1H-吲哚-5-基)-4-(4-嗎啉基)-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
2024/11/08HY-152726-(1H-吲哚-5-基)-4-(4-嗎啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶
WAY-600
1062159-35-610mM * 1mLin DMSO2067元

常見問題列表

生物活性
WAY-600 是有效,ATP 競爭型,選擇性的 mTOR 抑制劑,抑制重組 mTOR 酶的 IC50 值為 9 nM。WAY-600 阻斷 mTOR 復合物 1/2 (mTORC1/2) 組裝和激活。
靶點

mTOR

9 nM (IC 50 )

mTORC1

mTORC2

PI3K alpha

1.96 μM (IC 50 )

PI3K gamma

8.45 μM (IC 50 )

體外研究

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).

體內(nèi)研究

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).

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