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PF-4708671是一種細胞滲透性p70 ribosomal S6 kinase(S6K1亞型)抑制劑,在無細胞試驗中Ki/IC50為20 nM/160 nM,作用于S6K1比作用于S6K2選擇性高400倍,作用于S6K1比作用于MSK1和RSK1/2選擇性分別高4和20倍以上,是第一個報道的S6K1特異性抑制劑。
PF-4708671 Chemical Structure
CAS: 1255517-76-0
相關(guān)靶點 | p70 S6K p70 S6K1 RSK1 RSK2 RSK3 RSK4 | 點擊展開 |
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相關(guān)產(chǎn)品 | BI-D1870 LY2584702 LY2584702 Tosylate LJI308 LJH685 Phospho-S6K1(T421/S424) Rabbit Recombinant mAb | 點擊展開 |
相關(guān)化合物庫 | 激酶抑制劑庫 PI3K/Akt 抑制劑庫 凋亡分子化合物庫 細胞周期化合物庫 NF-κB信號通路庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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BHT-101 | Growth Inhibition Assay | IC50=0.82024 μM | SANGER | ||
UACC-893 | Growth Inhibition Assay | IC50=5.19886 μM | SANGER | ||
A427 | Growth Inhibition Assay | IC50=5.72567 μM | SANGER | ||
OCUB-M | Growth Inhibition Assay | IC50=6.66102 μM | SANGER | ||
SW684 | Growth Inhibition Assay | IC50=7.52268 μM | SANGER | ||
SK-LMS-1 | Growth Inhibition Assay | IC50=9.01302 μM | SANGER | ||
CP50-MEL-B | Growth Inhibition Assay | IC50=9.30419 μM | SANGER | ||
NCI-H1651 | Growth Inhibition Assay | IC50=10.0276 μM | SANGER | ||
ABC-1 | Growth Inhibition Assay | IC50=10.1037 μM | SANGER | ||
OE19 | Growth Inhibition Assay | IC50=10.1733 μM | SANGER | ||
DSH1 | Growth Inhibition Assay | IC50=10.8879 μM | SANGER | ||
SW13 | Growth Inhibition Assay | IC50=11.9319 μM | SANGER | ||
MDA-MB-453 | Growth Inhibition Assay | IC50=12.1603 μM | SANGER | ||
647-V | Growth Inhibition Assay | IC50=12.3582 μM | SANGER | ||
NCI-H2342 | Growth Inhibition Assay | IC50=12.3995 μM | SANGER | ||
LB2241-RCC | Growth Inhibition Assay | IC50=12.5779 μM | SANGER | ||
UACC-257 | Growth Inhibition Assay | IC50=13.4453 μM | SANGER | ||
NCI-H661 | Growth Inhibition Assay | IC50=13.6449 μM | SANGER | ||
FADU | Growth Inhibition Assay | IC50=13.6992 μM | SANGER | ||
A2780 | Growth Inhibition Assay | IC50=13.8041 μM | SANGER | ||
NCI-H1793 | Growth Inhibition Assay | IC50=14.4085 μM | SANGER | ||
TE-8 | Growth Inhibition Assay | IC50=15.3465 μM | SANGER | ||
HGC-27 | Growth Inhibition Assay | IC50=16.1644 μM | SANGER | ||
MMAC-SF | Growth Inhibition Assay | IC50=17.3727 μM | SANGER | ||
Calu-6 | Growth Inhibition Assay | IC50=18.1513 μM | SANGER | ||
HUTU-80 | Growth Inhibition Assay | IC50=18.3959 μM | SANGER | ||
SAS | Growth Inhibition Assay | IC50=18.6455 μM | SANGER | ||
IST-MES1 | Growth Inhibition Assay | IC50=18.6508 μM | SANGER | ||
C3A | Growth Inhibition Assay | IC50=18.7919 μM | SANGER | ||
ES3 | Growth Inhibition Assay | IC50=18.8364 μM | SANGER | ||
HSC-2 | Growth Inhibition Assay | IC50=19.6541 μM | SANGER | ||
T47D | Growth Inhibition Assay | IC50=20.1485 μM | SANGER | ||
EW-7 | Growth Inhibition Assay | IC50=20.8588 μM | SANGER | ||
LN-405 | Growth Inhibition Assay | IC50=20.8965 μM | SANGER | ||
U031 | Growth Inhibition Assay | IC50=21.4802 μM | SANGER | ||
A549 | Growth Inhibition Assay | IC50=21.8491 μM | SANGER | ||
RMG-I | Growth Inhibition Assay | IC50=22.2668 μM | SANGER | ||
BT-474 | Growth Inhibition Assay | IC50=22.6551 μM | SANGER | ||
NB69 | Growth Inhibition Assay | IC50=23.152 μM | SANGER | ||
NB7 | Growth Inhibition Assay | IC50=24.188 μM | SANGER | ||
HCC1569 | Growth Inhibition Assay | IC50=24.6125 μM | SANGER | ||
MEL-JUSO | Growth Inhibition Assay | IC50=24.6908 μM | SANGER | ||
MDA-MB-175-VII | Growth Inhibition Assay | IC50=25.2517 μM | SANGER | ||
HCC1419 | Growth Inhibition Assay | IC50=25.6003 μM | SANGER | ||
Ca9-22 | Growth Inhibition Assay | IC50=25.6432 μM | SANGER | ||
KGN | Growth Inhibition Assay | IC50=25.7547 μM | SANGER | ||
LB373-MEL-D | Growth Inhibition Assay | IC50=26.1938 μM | SANGER | ||
NCI-H1755 | Growth Inhibition Assay | IC50=26.8841 μM | SANGER | ||
D-423MG | Growth Inhibition Assay | IC50=27.0715 μM | SANGER | ||
DK-MG | Growth Inhibition Assay | IC50=28.7846 μM | SANGER | ||
NCI-H1623 | Growth Inhibition Assay | IC50=28.8342 μM | SANGER | ||
KU-19-19 | Growth Inhibition Assay | IC50=28.995 μM | SANGER | ||
C-33-A | Growth Inhibition Assay | IC50=29.2198 μM | SANGER | ||
SCC-4 | Growth Inhibition Assay | IC50=30.3354 μM | SANGER | ||
MG-63 | Growth Inhibition Assay | IC50=30.5994 μM | SANGER | ||
LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=31.4921 μM | SANGER | ||
CAPAN-1 | Growth Inhibition Assay | IC50=31.5286 μM | SANGER | ||
GI-ME-N | Growth Inhibition Assay | IC50=31.5353 μM | SANGER | ||
RERF-LC-MS | Growth Inhibition Assay | IC50=32.6747 μM | SANGER | ||
KLE | Growth Inhibition Assay | IC50=33.4334 μM | SANGER | ||
KNS-81-FD | Growth Inhibition Assay | IC50=33.5008 μM | SANGER | ||
DOK | Growth Inhibition Assay | IC50=34.6612 μM | SANGER | ||
ACHN | Growth Inhibition Assay | IC50=35.1588 μM | SANGER | ||
KYSE-520 | Growth Inhibition Assay | IC50=35.2361 μM | SANGER | ||
SBC-5 | Growth Inhibition Assay | IC50=35.5116 μM | SANGER | ||
NCI-H28 | Growth Inhibition Assay | IC50=35.6695 μM | SANGER | ||
ES7 | Growth Inhibition Assay | IC50=36.2249 μM | SANGER | ||
A172 | Growth Inhibition Assay | IC50=36.4187 μM | SANGER | ||
UM-UC-3 | Growth Inhibition Assay | IC50=37.8746 μM | SANGER | ||
LXF-289 | Growth Inhibition Assay | IC50=38.0047 μM | SANGER | ||
KP-4 | Growth Inhibition Assay | IC50=38.4739 μM | SANGER | ||
TE-1 | Growth Inhibition Assay | IC50=39.6589 μM | SANGER | ||
G-402 | Growth Inhibition Assay | IC50=40.061 μM | SANGER | ||
786-0 | Growth Inhibition Assay | IC50=40.9096 μM | SANGER | ||
K5 | Growth Inhibition Assay | IC50=41.3686 μM | SANGER | ||
SK-N-DZ | Growth Inhibition Assay | IC50=41.3823 μM | SANGER | ||
OVCAR-4 | Growth Inhibition Assay | IC50=41.7568 μM | SANGER | ||
T84 | Growth Inhibition Assay | IC50=42.1263 μM | SANGER | ||
GCIY | Growth Inhibition Assay | IC50=43.0803 μM | SANGER | ||
BB49-HNC | Growth Inhibition Assay | IC50=43.3348 μM | SANGER | ||
SNU-C2B | Growth Inhibition Assay | IC50=43.6436 μM | SANGER | ||
TE-6 | Growth Inhibition Assay | IC50=43.8894 μM | SANGER | ||
23132-87 | Growth Inhibition Assay | IC50=44.2978 μM | SANGER | ||
DMS-53 | Growth Inhibition Assay | IC50=44.3384 μM | SANGER | ||
ONS-76 | Growth Inhibition Assay | IC50=44.7661 μM | SANGER | ||
DMS-273 | Growth Inhibition Assay | IC50=44.943 μM | SANGER | ||
COLO-824 | Growth Inhibition Assay | IC50=45.8775 μM | SANGER | ||
DMS-114 | Growth Inhibition Assay | IC50=45.8927 μM | SANGER | ||
YKG-1 | Growth Inhibition Assay | IC50=46.0355 μM | SANGER | ||
RH-18 | Growth Inhibition Assay | IC50=46.3733 μM | SANGER | ||
NCI-H1355 | Growth Inhibition Assay | IC50=46.618 μM | SANGER | ||
NCI-H2170 | Growth Inhibition Assay | IC50=47.7584 μM | SANGER | ||
OC-314 | Growth Inhibition Assay | IC50=47.8478 μM | SANGER | ||
NCI-H2030 | Growth Inhibition Assay | IC50=47.8906 μM | SANGER | ||
22RV1 | Growth Inhibition Assay | IC50=47.9015 μM | SANGER | ||
G-401 | Growth Inhibition Assay | IC50=48.4415 μM | SANGER | ||
YAPC | Growth Inhibition Assay | IC50=49.8073 μM | SANGER | ||
SW1573 | Growth Inhibition Assay | IC50=50.2435 μM | SANGER | ||
COLO-792 | Growth Inhibition Assay | IC50=50.6237 μM | SANGER | ||
KNS-62 | Growth Inhibition Assay | IC50=50.7508 μM | SANGER | ||
NB5 | Growth Inhibition Assay | IC50=51.4509 μM | SANGER | ||
CP66-MEL | Growth Inhibition Assay | IC50=51.6408 μM | SANGER | ||
CaR-1 | Growth Inhibition Assay | IC50=52.0606 μM | SANGER | ||
CAL-54 | Growth Inhibition Assay | IC50=52.1102 μM | SANGER | ||
8305C | Growth Inhibition Assay | IC50=52.315 μM | SANGER | ||
Calu-3 | Growth Inhibition Assay | IC50=52.3733 μM | SANGER | ||
AU565 | Growth Inhibition Assay | IC50=52.5509 μM | SANGER | ||
CW-2 | Growth Inhibition Assay | IC50=52.8654 μM | SANGER | ||
BEN | Growth Inhibition Assay | IC50=53.7862 μM | SANGER | ||
NCI-H1975 | Growth Inhibition Assay | IC50=53.8966 μM | SANGER | ||
HCT-116 | Growth Inhibition Assay | IC50=54.0327 μM | SANGER | ||
SH-4 | Growth Inhibition Assay | IC50=54.138 μM | SANGER | ||
NCI-H1693 | Growth Inhibition Assay | IC50=54.2103 μM | SANGER | ||
BPH-1 | Growth Inhibition Assay | IC50=55.2892 μM | SANGER | ||
CAMA-1 | Growth Inhibition Assay | IC50=55.8116 μM | SANGER | ||
A388 | Growth Inhibition Assay | IC50=56.0985 μM | SANGER | ||
C2BBe1 | Growth Inhibition Assay | IC50=56.2634 μM | SANGER | ||
GAMG | Growth Inhibition Assay | IC50=56.5955 μM | SANGER | ||
MKN28 | Growth Inhibition Assay | IC50=56.8013 μM | SANGER | ||
VA-ES-BJ | Growth Inhibition Assay | IC50=56.8745 μM | SANGER | ||
HuCCT1 | Growth Inhibition Assay | IC50=57.0492 μM | SANGER | ||
BFTC-905 | Growth Inhibition Assay | IC50=57.2898 μM | SANGER | ||
LS-123 | Growth Inhibition Assay | IC50=57.5668 μM | SANGER | ||
LB996-RCC | Growth Inhibition Assay | IC50=58.0287 μM | SANGER | ||
NCI-H1048 | Growth Inhibition Assay | IC50=58.2188 μM | SANGER | ||
COR-L105 | Growth Inhibition Assay | IC50=58.7337 μM | SANGER | ||
OVCAR-8 | Growth Inhibition Assay | IC50=59.1716 μM | SANGER | ||
SK-N-FI | Growth Inhibition Assay | IC50=59.3207 μM | SANGER | ||
MES-SA | Growth Inhibition Assay | IC50=59.4509 μM | SANGER | ||
SCC-9 | Growth Inhibition Assay | IC50=59.4753 μM | SANGER | ||
EFO-27 | Growth Inhibition Assay | IC50=59.943 μM | SANGER | ||
GT3TKB | Growth Inhibition Assay | IC50=60.6048 μM | SANGER | ||
HCC38 | Growth Inhibition Assay | IC50=61.4379 μM | SANGER | ||
MLMA | Growth Inhibition Assay | IC50=61.6163 μM | SANGER | ||
D-566MG | Growth Inhibition Assay | IC50=63.5224 μM | SANGER | ||
SF295 | Growth Inhibition Assay | IC50=63.6655 μM | SANGER | ||
ES4 | Growth Inhibition Assay | IC50=64.4719 μM | SANGER | ||
CAKI-1 | Growth Inhibition Assay | IC50=64.5721 μM | SANGER | ||
OAW-28 | Growth Inhibition Assay | IC50=64.9647 μM | SANGER | ||
NCI-H460 | Growth Inhibition Assay | IC50=65.0897 μM | SANGER | ||
JAR | Growth Inhibition Assay | IC50=65.5516 μM | SANGER | ||
SNU-449 | Growth Inhibition Assay | IC50=65.7616 μM | SANGER | ||
D-392MG | Growth Inhibition Assay | IC50=65.9434 μM | SANGER | ||
EW-22 | Growth Inhibition Assay | IC50=66.395 μM | SANGER | ||
GCT | Growth Inhibition Assay | IC50=67.0443 μM | SANGER | ||
NOS-1 | Growth Inhibition Assay | IC50=67.6867 μM | SANGER | ||
RH-1 | Growth Inhibition Assay | IC50=68.5559 μM | SANGER | ||
HuH-7 | Growth Inhibition Assay | IC50=69.1002 μM | SANGER | ||
NUGC-3 | Growth Inhibition Assay | IC50=70.9644 μM | SANGER | ||
IST-SL1 | Growth Inhibition Assay | IC50=71.2324 μM | SANGER | ||
SHP-77 | Growth Inhibition Assay | IC50=72.119 μM | SANGER | ||
SW1116 | Growth Inhibition Assay | IC50=72.1407 μM | SANGER | ||
LK-2 | Growth Inhibition Assay | IC50=72.8612 μM | SANGER | ||
U-2-OS | Growth Inhibition Assay | IC50=73.1828 μM | SANGER | ||
KYSE-150 | Growth Inhibition Assay | IC50=73.6118 μM | SANGER | ||
U251 | Growth Inhibition Assay | IC50=73.8168 μM | SANGER | ||
HT-1080 | Growth Inhibition Assay | IC50=74.2574 μM | SANGER | ||
NCI-H1437 | Growth Inhibition Assay | IC50=74.6326 μM | SANGER | ||
HPAF-II | Growth Inhibition Assay | IC50=74.6415 μM | SANGER | ||
Becker | Growth Inhibition Assay | IC50=75.1105 μM | SANGER | ||
PANC-10-05 | Growth Inhibition Assay | IC50=75.2865 μM | SANGER | ||
TYK-nu | Growth Inhibition Assay | IC50=75.3102 μM | SANGER | ||
SKG-IIIa | Growth Inhibition Assay | IC50=75.3341 μM | SANGER | ||
NCI-H1993 | Growth Inhibition Assay | IC50=75.7397 μM | SANGER | ||
S-117 | Growth Inhibition Assay | IC50=75.755 μM | SANGER | ||
HuO9 | Growth Inhibition Assay | IC50=76.0048 μM | SANGER | ||
CAL-51 | Growth Inhibition Assay | IC50=76.1006 μM | SANGER | ||
BT-20 | Growth Inhibition Assay | IC50=76.2168 μM | SANGER | ||
LB831-BLC | Growth Inhibition Assay | IC50=76.3217 μM | SANGER | ||
LB1047-RCC | Growth Inhibition Assay | IC50=76.7619 μM | SANGER | ||
ES8 | Growth Inhibition Assay | IC50=78.0073 μM | SANGER | ||
UMC-11 | Growth Inhibition Assay | IC50=78.0884 μM | SANGER | ||
NCI-H226 | Growth Inhibition Assay | IC50=78.1315 μM | SANGER | ||
IGROV-1 | Growth Inhibition Assay | IC50=78.555 μM | SANGER | ||
BHY | Growth Inhibition Assay | IC50=79.596 μM | SANGER | ||
MKN45 | Growth Inhibition Assay | IC50=80.3174 μM | SANGER | ||
IA-LM | Growth Inhibition Assay | IC50=80.3511 μM | SANGER | ||
WM-115 | Growth Inhibition Assay | IC50=81.4114 μM | SANGER | ||
VMRC-RCZ | Growth Inhibition Assay | IC50=81.4425 μM | SANGER | ||
NCI-H2291 | Growth Inhibition Assay | IC50=81.6842 μM | SANGER | ||
MCF7 | Growth Inhibition Assay | IC50=83.2897 μM | SANGER | ||
639-V | Growth Inhibition Assay | IC50=84.6129 μM | SANGER | ||
RT4 | Growth Inhibition Assay | IC50=85.2403 μM | SANGER | ||
NCI-H2405 | Growth Inhibition Assay | IC50=85.2997 μM | SANGER | ||
CAL-33 | Growth Inhibition Assay | IC50=85.6315 μM | SANGER | ||
BT-549 | Growth Inhibition Assay | IC50=85.9382 μM | SANGER | ||
HT-1197 | Growth Inhibition Assay | IC50=88.1077 μM | SANGER | ||
G-361 | Growth Inhibition Assay | IC50=88.1474 μM | SANGER | ||
LS-411N | Growth Inhibition Assay | IC50=89.3388 μM | SANGER | ||
HT-144 | Growth Inhibition Assay | IC50=89.5992 μM | SANGER | ||
DJM-1 | Growth Inhibition Assay | IC50=89.8845 μM | SANGER | ||
CAL-12T | Growth Inhibition Assay | IC50=90.7895 μM | SANGER | ||
MKN7 | Growth Inhibition Assay | IC50=91.3551 μM | SANGER | ||
HuP-T3 | Growth Inhibition Assay | IC50=96.1004 μM | SANGER | ||
SK-MG-1 | Growth Inhibition Assay | IC50=96.1348 μM | SANGER | ||
NCI-H2347 | Growth Inhibition Assay | IC50=98.1042 μM | SANGER | ||
SW872 | Growth Inhibition Assay | IC50=100.456 μM | SANGER | ||
COLO-829 | Growth Inhibition Assay | IC50=100.553 μM | SANGER | ||
MC-IXC | Growth Inhibition Assay | IC50=100.615 μM | SANGER | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | PF-4708671是一種細胞滲透性p70 ribosomal S6 kinase(S6K1亞型)抑制劑,在無細胞試驗中Ki/IC50為20 nM/160 nM,作用于S6K1比作用于S6K2選擇性高400倍,作用于S6K1比作用于MSK1和RSK1/2選擇性分別高4和20倍以上,是第一個報道的S6K1特異性抑制劑。 | ||
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | 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。[1] | |||
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實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
Western blot | pS6 / S6 / pS6K / S6K1 / pAKT / AKT p-mTOR / mTOR / p-p70S6K / p70S6K |
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28626016 | |
Growth inhibition assay | Cell viability |
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30423811 |
分子量 | 390.41 | 分子式 | C19H21F3N6 |
CAS號 | 1255517-76-0 | SDF | Download PF-4708671 SDF |
Smiles | CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
Ethanol : 40 mg/mL (102.45 mM) DMSO : 30 mg/mL ( (76.84 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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問題 1:
Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for S2163 is suitable for i.p. or not?
回答:
The formula "30% PEG400+0.5% Tween80+5% Propylene glycol" on our website is an oral one. It is a suspension.