1255517-76-0

基本信息
2-[[4-(5-乙基-4-嘧啶基)-1-哌嗪基]甲基]-6-(三氟甲基)-1H-苯并咪唑
PF 4708671
PF-04708671
PF4708671/PF-4708671
PF-4708671 USP/EP/BP
PF 4708671 - PF 04708671
2-[[4-(5-ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-6-(trifluoromethyl)-1H-benzimidazole
2-[[4-(5-ethyl-4-pyriMidinyl)-1-piperazinyl]Methyl]-6-(trifluoroMethyl)-1H-benziMidazole
1H-Benzimidazole, 2-[[4-(5-ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-
2-[[4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-5-(trifluoromethyl)-1H-benzo[d]imidazole
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱(chēng) | CAS號(hào) | 包裝 | 價(jià)格 |
2025/05/22 | HY-15773 | PF-4708671 | 1255517-76-0 | 1 mg | 184元 |
2025/05/22 | HY-15773 | PF-4708671 | 1255517-76-0 | 5 mg | 368元 |
2025/05/22 | HY-15773 | PF-4708671 PF-4708671 | 1255517-76-0 | 10mg | 590元 |
常見(jiàn)問(wèn)題列表
Target | Value |
p70 S6K1
(Cell-free assay) | 160 nM |
PF-4708671是一種哌嗪基嘧啶類(lèi)似物,是第一個(gè)S6K1特異性抑制劑。PF-4708671不顯著抑制緊密相關(guān)的S6K2亞型或一組其他AGC激酶 (Akt1, Akt2, PKA, PKCα, PKC?, PRK2, ROCK2, RSK1, RSK2 或SGK1)的活性。PF-4708671抑制S6K1介導(dǎo)的響應(yīng)IGF-1(胰島素樣生長(zhǎng)因子1)的S6蛋白的磷酸化,對(duì)PMA-誘導(dǎo)的底物磷酸化沒(méi)有作用效果,底物與RSK (p90核糖體S6激酶)和MSK(絲分裂原和應(yīng)激活化蛋白激酶)激酶高度相關(guān)。PF-4708671誘導(dǎo)S6K1的T型環(huán)和疏水性基序磷酸化,這種作用依賴(lài)于mTORC1 (mTOR復(fù)合體1)。PF-4708671不影響mTORC1的活性。
The tumor growth rate in mice treated with the combination of OSI-906+PF-4708671 is significantly slower than that of OSI-906 alone (P=0.0189) or PF4708671 alone (P=0.0165) treated mice. The average tumor volume in the OSI-906+PF-4708671-treated mice is approximately 50% of that in mice treated with OSI-906 (P=0.0056) or PF-4708671 alone (P<0.001) at the end of a 15-day treatment.