PF-4708671
| 中文名稱 | PF-4708671 |
|---|---|
| 中文同義詞 | 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;2-((4-(5-乙基嘧啶-4-基)哌嗪-1-基)甲基)-6-(三氟甲基)-1H-苯并[D]咪唑;PF-4708671,S6K1抑制劑;化合物PF-4708671,10 MM DMSO 溶液;P70核糖體S6激酶1抑制劑(S6K1抑制劑)(PF-4708671);PF-4708671 |CAS 1255517-76-0;抑制劑PF-4708671;PF-4708671試劑 |
| 英文名稱 | PF-4708671 |
| 英文同義詞 | 2-[[4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-5-(trifluoromethyl)-1H-benzo[d]imidazole;PF 4708671;PF4708671/PF-4708671;2-[[4-(5-ethyl-4-pyriMidinyl)-1-piperazinyl]Methyl]-6-(trifluoroMethyl)-1H-benziMidazole;PF-04708671;1H-Benzimidazole, 2-[[4-(5-ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-;2-[[4-(5-Ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-1H-benzimidazole PF-4708671;2-[[4-(5-ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-6-(trifluoromethyl)-1H-benzimidazole |
| CAS號 | 1255517-76-0 |
| 分子式 | C19H21F3N6 |
| 分子量 | 390.41 |
| EINECS號 | |
| 相關(guān)類別 | 小分子抑制劑;小分子抑制劑，天然產(chǎn)物;細胞生物學(xué)試劑;Akt;mTOR;PI3K;PI3K/Akt/mTOR;Amines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals;API |
| Mol文件 | 1255517-76-0.mol |
| 結(jié)構(gòu)式 |  |
PF-4708671 性質(zhì)
| 沸點 | 572.8±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.348±0.06 g/cm3(Predicted) |
| 儲存條件 | room temp |
| 溶解度 | 二甲基亞砜：≥20mg/mL |
| 形態(tài) | 粉末 |
| 酸度系數(shù)(pKa) | 10.20±0.10(Predicted) |
| 顏色 | 米白色 |
| InChI | 1S/C19H21F3N6/c1-2-13-10-23-12-24-18(13)28-7-5-27(6-8-28)11-17-25-15-4-3-14(19(20,21)22)9-16(15)26-17/h3-4,9-10,12H,2,5-8,11H2,1H3,(H,25,26) |
| InChIKey | FBLPQCAQRNSVHB-UHFFFAOYSA-N |
| SMILES | CCC(C=NC=N1)=C1N2CCN(CC3=NC4=C(C=CC(C(F)(F)F)=C4)N3)CC2 |
| Target | Value |
|
p70 S6K1
(Cell-free assay) | 160 nM |
PF-4708671是一種哌嗪基嘧啶類似物，是第一個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（胰島素樣生長因子1）的S6蛋白的磷酸化，對PMA-誘導(dǎo)的底物磷酸化沒有作用效果，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.
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2026/07/06 | S2163 | PF-4708671 PF-4708671 | 1255517-76-0 | 10mg | 1179.06元 |
| 2026/07/06 | S2163 | PF-4708671 PF-4708671 | 1255517-76-0 | 10mM (1mL in DMSO) | 1574.66元 |