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PF-4708671

PF-4708671是一種細(xì)胞滲透性p70 ribosomal S6 kinase(S6K1亞型)抑制劑，在無細(xì)胞試驗(yàn)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(gè)報(bào)道的S6K1特異性抑制劑。

PF-4708671 Chemical Structure

PF-4708671 Chemical Structure

CAS: 1255517-76-0

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1574.66 現(xiàn)貨
10mg 1179.06 現(xiàn)貨
50mg 3415.23 現(xiàn)貨
1g 24488.1 現(xiàn)貨
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PF-4708671相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

S6 Kinase Signaling Pathways

S6 Kinase信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
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
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生物活性

產(chǎn)品描述 PF-4708671是一種細(xì)胞滲透性p70 ribosomal S6 kinase(S6K1亞型)抑制劑，在無細(xì)胞試驗(yàn)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(gè)報(bào)道的S6K1特異性抑制劑。
靶點(diǎn)
p70 S6K1 [1]
(Cell-free assay)
160 nM
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(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]
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot pS6 / S6 / pS6K / S6K1 / pAKT / AKT p-mTOR / mTOR / p-p70S6K / p70S6K 28626016
Growth inhibition assay Cell viability 30423811

化學(xué)信息&溶解度

分子量 390.41 分子式

C19H21F3N6
CAS號(hào) 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(chǔ)存條件(自收到貨起)

體外溶解度
批次：

Ethanol : 40 mg/mL (102.45 mM)

DMSO : 30 mg/mL ( (76.84 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)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(qǐng)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(jìn)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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常見問題及建議解決方法

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.

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