solo per uso di ricerca
PF-4708671 S6 Kinase inibitore
N. Cat.S2163
Struttura chimica
Peso molecolare: 390.41
Controllo Qualità
| Target correlati | PI3K Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A |
|---|---|
| Altro S6 Kinase Inibitori | BI-D1870 LY2584702 LY2584702 Tosylate LJH685 LJI308 S6K-18 3'-Hydroxypterostilbene L-Norvaline BRD7389 Gingerenone A |
Coltura cellulare, trattamento e concentrazione di lavoro
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dellattività | PMID |
|---|---|---|---|---|---|---|
| BHT-101 | Growth Inhibition Assay | IC50=0.82024 μM | ||||
| UACC-893 | Growth Inhibition Assay | IC50=5.19886 μM | ||||
| A427 | Growth Inhibition Assay | IC50=5.72567 μM | ||||
| OCUB-M | Growth Inhibition Assay | IC50=6.66102 μM | ||||
| SW684 | Growth Inhibition Assay | IC50=7.52268 μM | ||||
| SK-LMS-1 | Growth Inhibition Assay | IC50=9.01302 μM | ||||
| CP50-MEL-B | Growth Inhibition Assay | IC50=9.30419 μM | ||||
| NCI-H1651 | Growth Inhibition Assay | IC50=10.0276 μM | ||||
| ABC-1 | Growth Inhibition Assay | IC50=10.1037 μM | ||||
| OE19 | Growth Inhibition Assay | IC50=10.1733 μM | ||||
| DSH1 | Growth Inhibition Assay | IC50=10.8879 μM | ||||
| SW13 | Growth Inhibition Assay | IC50=11.9319 μM | ||||
| MDA-MB-453 | Growth Inhibition Assay | IC50=12.1603 μM | ||||
| 647-V | Growth Inhibition Assay | IC50=12.3582 μM | ||||
| NCI-H2342 | Growth Inhibition Assay | IC50=12.3995 μM | ||||
| LB2241-RCC | Growth Inhibition Assay | IC50=12.5779 μM | ||||
| UACC-257 | Growth Inhibition Assay | IC50=13.4453 μM | ||||
| NCI-H661 | Growth Inhibition Assay | IC50=13.6449 μM | ||||
| FADU | Growth Inhibition Assay | IC50=13.6992 μM | ||||
| A2780 | Growth Inhibition Assay | IC50=13.8041 μM | ||||
| NCI-H1793 | Growth Inhibition Assay | IC50=14.4085 μM | ||||
| TE-8 | Growth Inhibition Assay | IC50=15.3465 μM | ||||
| HGC-27 | Growth Inhibition Assay | IC50=16.1644 μM | ||||
| MMAC-SF | Growth Inhibition Assay | IC50=17.3727 μM | ||||
| Calu-6 | Growth Inhibition Assay | IC50=18.1513 μM | ||||
| HUTU-80 | Growth Inhibition Assay | IC50=18.3959 μM | ||||
| SAS | Growth Inhibition Assay | IC50=18.6455 μM | ||||
| IST-MES1 | Growth Inhibition Assay | IC50=18.6508 μM | ||||
| C3A | Growth Inhibition Assay | IC50=18.7919 μM | ||||
| ES3 | Growth Inhibition Assay | IC50=18.8364 μM | ||||
| HSC-2 | Growth Inhibition Assay | IC50=19.6541 μM | ||||
| T47D | Growth Inhibition Assay | IC50=20.1485 μM | ||||
| EW-7 | Growth Inhibition Assay | IC50=20.8588 μM | ||||
| LN-405 | Growth Inhibition Assay | IC50=20.8965 μM | ||||
| U031 | Growth Inhibition Assay | IC50=21.4802 μM | ||||
| A549 | Growth Inhibition Assay | IC50=21.8491 μM | ||||
| RMG-I | Growth Inhibition Assay | IC50=22.2668 μM | ||||
| BT-474 | Growth Inhibition Assay | IC50=22.6551 μM | ||||
| NB69 | Growth Inhibition Assay | IC50=23.152 μM | ||||
| NB7 | Growth Inhibition Assay | IC50=24.188 μM | ||||
| HCC1569 | Growth Inhibition Assay | IC50=24.6125 μM | ||||
| MEL-JUSO | Growth Inhibition Assay | IC50=24.6908 μM | ||||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=25.2517 μM | ||||
| HCC1419 | Growth Inhibition Assay | IC50=25.6003 μM | ||||
| Ca9-22 | Growth Inhibition Assay | IC50=25.6432 μM | ||||
| KGN | Growth Inhibition Assay | IC50=25.7547 μM | ||||
| LB373-MEL-D | Growth Inhibition Assay | IC50=26.1938 μM | ||||
| NCI-H1755 | Growth Inhibition Assay | IC50=26.8841 μM | ||||
| D-423MG | Growth Inhibition Assay | IC50=27.0715 μM | ||||
| DK-MG | Growth Inhibition Assay | IC50=28.7846 μM | ||||
| NCI-H1623 | Growth Inhibition Assay | IC50=28.8342 μM | ||||
| KU-19-19 | Growth Inhibition Assay | IC50=28.995 μM | ||||
| C-33-A | Growth Inhibition Assay | IC50=29.2198 μM | ||||
| SCC-4 | Growth Inhibition Assay | IC50=30.3354 μM | ||||
| MG-63 | Growth Inhibition Assay | IC50=30.5994 μM | ||||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=31.4921 μM | ||||
| CAPAN-1 | Growth Inhibition Assay | IC50=31.5286 μM | ||||
| GI-ME-N | Growth Inhibition Assay | IC50=31.5353 μM | ||||
| RERF-LC-MS | Growth Inhibition Assay | IC50=32.6747 μM | ||||
| KLE | Growth Inhibition Assay | IC50=33.4334 μM | ||||
| KNS-81-FD | Growth Inhibition Assay | IC50=33.5008 μM | ||||
| DOK | Growth Inhibition Assay | IC50=34.6612 μM | ||||
| ACHN | Growth Inhibition Assay | IC50=35.1588 μM | ||||
| KYSE-520 | Growth Inhibition Assay | IC50=35.2361 μM | ||||
| SBC-5 | Growth Inhibition Assay | IC50=35.5116 μM | ||||
| NCI-H28 | Growth Inhibition Assay | IC50=35.6695 μM | ||||
| ES7 | Growth Inhibition Assay | IC50=36.2249 μM | ||||
| A172 | Growth Inhibition Assay | IC50=36.4187 μM | ||||
| UM-UC-3 | Growth Inhibition Assay | IC50=37.8746 μM | ||||
| LXF-289 | Growth Inhibition Assay | IC50=38.0047 μM | ||||
| KP-4 | Growth Inhibition Assay | IC50=38.4739 μM | ||||
| TE-1 | Growth Inhibition Assay | IC50=39.6589 μM | ||||
| G-402 | Growth Inhibition Assay | IC50=40.061 μM | ||||
| 786-0 | Growth Inhibition Assay | IC50=40.9096 μM | ||||
| K5 | Growth Inhibition Assay | IC50=41.3686 μM | ||||
| SK-N-DZ | Growth Inhibition Assay | IC50=41.3823 μM | ||||
| OVCAR-4 | Growth Inhibition Assay | IC50=41.7568 μM | ||||
| T84 | Growth Inhibition Assay | IC50=42.1263 μM | ||||
| GCIY | Growth Inhibition Assay | IC50=43.0803 μM | ||||
| BB49-HNC | Growth Inhibition Assay | IC50=43.3348 μM | ||||
| SNU-C2B | Growth Inhibition Assay | IC50=43.6436 μM | ||||
| TE-6 | Growth Inhibition Assay | IC50=43.8894 μM | ||||
| 23132-87 | Growth Inhibition Assay | IC50=44.2978 μM | ||||
| DMS-53 | Growth Inhibition Assay | IC50=44.3384 μM | ||||
| ONS-76 | Growth Inhibition Assay | IC50=44.7661 μM | ||||
| DMS-273 | Growth Inhibition Assay | IC50=44.943 μM | ||||
| COLO-824 | Growth Inhibition Assay | IC50=45.8775 μM | ||||
| DMS-114 | Growth Inhibition Assay | IC50=45.8927 μM | ||||
| YKG-1 | Growth Inhibition Assay | IC50=46.0355 μM | ||||
| RH-18 | Growth Inhibition Assay | IC50=46.3733 μM | ||||
| NCI-H1355 | Growth Inhibition Assay | IC50=46.618 μM | ||||
| NCI-H2170 | Growth Inhibition Assay | IC50=47.7584 μM | ||||
| OC-314 | Growth Inhibition Assay | IC50=47.8478 μM | ||||
| NCI-H2030 | Growth Inhibition Assay | IC50=47.8906 μM | ||||
| 22RV1 | Growth Inhibition Assay | IC50=47.9015 μM | ||||
| G-401 | Growth Inhibition Assay | IC50=48.4415 μM | ||||
| YAPC | Growth Inhibition Assay | IC50=49.8073 μM | ||||
| SW1573 | Growth Inhibition Assay | IC50=50.2435 μM | ||||
| COLO-792 | Growth Inhibition Assay | IC50=50.6237 μM | ||||
| KNS-62 | Growth Inhibition Assay | IC50=50.7508 μM | ||||
| NB5 | Growth Inhibition Assay | IC50=51.4509 μM | ||||
| CP66-MEL | Growth Inhibition Assay | IC50=51.6408 μM | ||||
| CaR-1 | Growth Inhibition Assay | IC50=52.0606 μM | ||||
| CAL-54 | Growth Inhibition Assay | IC50=52.1102 μM | ||||
| 8305C | Growth Inhibition Assay | IC50=52.315 μM | ||||
| Calu-3 | Growth Inhibition Assay | IC50=52.3733 μM | ||||
| AU565 | Growth Inhibition Assay | IC50=52.5509 μM | ||||
| CW-2 | Growth Inhibition Assay | IC50=52.8654 μM | ||||
| BEN | Growth Inhibition Assay | IC50=53.7862 μM | ||||
| NCI-H1975 | Growth Inhibition Assay | IC50=53.8966 μM | ||||
| HCT-116 | Growth Inhibition Assay | IC50=54.0327 μM | ||||
| SH-4 | Growth Inhibition Assay | IC50=54.138 μM | ||||
| NCI-H1693 | Growth Inhibition Assay | IC50=54.2103 μM | ||||
| BPH-1 | Growth Inhibition Assay | IC50=55.2892 μM | ||||
| CAMA-1 | Growth Inhibition Assay | IC50=55.8116 μM | ||||
| A388 | Growth Inhibition Assay | IC50=56.0985 μM | ||||
| C2BBe1 | Growth Inhibition Assay | IC50=56.2634 μM | ||||
| GAMG | Growth Inhibition Assay | IC50=56.5955 μM | ||||
| MKN28 | Growth Inhibition Assay | IC50=56.8013 μM | ||||
| VA-ES-BJ | Growth Inhibition Assay | IC50=56.8745 μM | ||||
| HuCCT1 | Growth Inhibition Assay | IC50=57.0492 μM | ||||
| BFTC-905 | Growth Inhibition Assay | IC50=57.2898 μM | ||||
| LS-123 | Growth Inhibition Assay | IC50=57.5668 μM | ||||
| LB996-RCC | Growth Inhibition Assay | IC50=58.0287 μM | ||||
| NCI-H1048 | Growth Inhibition Assay | IC50=58.2188 μM | ||||
| COR-L105 | Growth Inhibition Assay | IC50=58.7337 μM | ||||
| OVCAR-8 | Growth Inhibition Assay | IC50=59.1716 μM | ||||
| SK-N-FI | Growth Inhibition Assay | IC50=59.3207 μM | ||||
| MES-SA | Growth Inhibition Assay | IC50=59.4509 μM | ||||
| SCC-9 | Growth Inhibition Assay | IC50=59.4753 μM | ||||
| EFO-27 | Growth Inhibition Assay | IC50=59.943 μM | ||||
| GT3TKB | Growth Inhibition Assay | IC50=60.6048 μM | ||||
| HCC38 | Growth Inhibition Assay | IC50=61.4379 μM | ||||
| MLMA | Growth Inhibition Assay | IC50=61.6163 μM | ||||
| D-566MG | Growth Inhibition Assay | IC50=63.5224 μM | ||||
| SF295 | Growth Inhibition Assay | IC50=63.6655 μM | ||||
| ES4 | Growth Inhibition Assay | IC50=64.4719 μM | ||||
| CAKI-1 | Growth Inhibition Assay | IC50=64.5721 μM | ||||
| OAW-28 | Growth Inhibition Assay | IC50=64.9647 μM | ||||
| NCI-H460 | Growth Inhibition Assay | IC50=65.0897 μM | ||||
| JAR | Growth Inhibition Assay | IC50=65.5516 μM | ||||
| SNU-449 | Growth Inhibition Assay | IC50=65.7616 μM | ||||
| D-392MG | Growth Inhibition Assay | IC50=65.9434 μM | ||||
| EW-22 | Growth Inhibition Assay | IC50=66.395 μM | ||||
| GCT | Growth Inhibition Assay | IC50=67.0443 μM | ||||
| NOS-1 | Growth Inhibition Assay | IC50=67.6867 μM | ||||
| RH-1 | Growth Inhibition Assay | IC50=68.5559 μM | ||||
| HuH-7 | Growth Inhibition Assay | IC50=69.1002 μM | ||||
| NUGC-3 | Growth Inhibition Assay | IC50=70.9644 μM | ||||
| IST-SL1 | Growth Inhibition Assay | IC50=71.2324 μM | ||||
| SHP-77 | Growth Inhibition Assay | IC50=72.119 μM | ||||
| SW1116 | Growth Inhibition Assay | IC50=72.1407 μM | ||||
| LK-2 | Growth Inhibition Assay | IC50=72.8612 μM | ||||
| U-2-OS | Growth Inhibition Assay | IC50=73.1828 μM | ||||
| KYSE-150 | Growth Inhibition Assay | IC50=73.6118 μM | ||||
| U251 | Growth Inhibition Assay | IC50=73.8168 μM | ||||
| HT-1080 | Growth Inhibition Assay | IC50=74.2574 μM | ||||
| NCI-H1437 | Growth Inhibition Assay | IC50=74.6326 μM | ||||
| HPAF-II | Growth Inhibition Assay | IC50=74.6415 μM | ||||
| Becker | Growth Inhibition Assay | IC50=75.1105 μM | ||||
| PANC-10-05 | Growth Inhibition Assay | IC50=75.2865 μM | ||||
| TYK-nu | Growth Inhibition Assay | IC50=75.3102 μM | ||||
| SKG-IIIa | Growth Inhibition Assay | IC50=75.3341 μM | ||||
| NCI-H1993 | Growth Inhibition Assay | IC50=75.7397 μM | ||||
| S-117 | Growth Inhibition Assay | IC50=75.755 μM | ||||
| HuO9 | Growth Inhibition Assay | IC50=76.0048 μM | ||||
| CAL-51 | Growth Inhibition Assay | IC50=76.1006 μM | ||||
| BT-20 | Growth Inhibition Assay | IC50=76.2168 μM | ||||
| LB831-BLC | Growth Inhibition Assay | IC50=76.3217 μM | ||||
| LB1047-RCC | Growth Inhibition Assay | IC50=76.7619 μM | ||||
| ES8 | Growth Inhibition Assay | IC50=78.0073 μM | ||||
| UMC-11 | Growth Inhibition Assay | IC50=78.0884 μM | ||||
| NCI-H226 | Growth Inhibition Assay | IC50=78.1315 μM | ||||
| IGROV-1 | Growth Inhibition Assay | IC50=78.555 μM | ||||
| BHY | Growth Inhibition Assay | IC50=79.596 μM | ||||
| MKN45 | Growth Inhibition Assay | IC50=80.3174 μM | ||||
| IA-LM | Growth Inhibition Assay | IC50=80.3511 μM | ||||
| WM-115 | Growth Inhibition Assay | IC50=81.4114 μM | ||||
| VMRC-RCZ | Growth Inhibition Assay | IC50=81.4425 μM | ||||
| NCI-H2291 | Growth Inhibition Assay | IC50=81.6842 μM | ||||
| MCF7 | Growth Inhibition Assay | IC50=83.2897 μM | ||||
| 639-V | Growth Inhibition Assay | IC50=84.6129 μM | ||||
| RT4 | Growth Inhibition Assay | IC50=85.2403 μM | ||||
| NCI-H2405 | Growth Inhibition Assay | IC50=85.2997 μM | ||||
| CAL-33 | Growth Inhibition Assay | IC50=85.6315 μM | ||||
| BT-549 | Growth Inhibition Assay | IC50=85.9382 μM | ||||
| HT-1197 | Growth Inhibition Assay | IC50=88.1077 μM | ||||
| G-361 | Growth Inhibition Assay | IC50=88.1474 μM | ||||
| LS-411N | Growth Inhibition Assay | IC50=89.3388 μM | ||||
| HT-144 | Growth Inhibition Assay | IC50=89.5992 μM | ||||
| DJM-1 | Growth Inhibition Assay | IC50=89.8845 μM | ||||
| CAL-12T | Growth Inhibition Assay | IC50=90.7895 μM | ||||
| MKN7 | Growth Inhibition Assay | IC50=91.3551 μM | ||||
| HuP-T3 | Growth Inhibition Assay | IC50=96.1004 μM | ||||
| SK-MG-1 | Growth Inhibition Assay | IC50=96.1348 μM | ||||
| NCI-H2347 | Growth Inhibition Assay | IC50=98.1042 μM | ||||
| SW872 | Growth Inhibition Assay | IC50=100.456 μM | ||||
| COLO-829 | Growth Inhibition Assay | IC50=100.553 μM | ||||
| MC-IXC | Growth Inhibition Assay | IC50=100.615 μM | ||||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
Informazioni chimiche, conservazione e stabilità
| Peso molecolare | 390.41 | Formula | C19H21F3N6 |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 1255517-76-0 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | N/A | Smiles | CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F | ||
Solubilità
|
In vitro |
DMSO
: 30 mg/mL
(76.84 mM)
Ethanol : 8 mg/mL Water : Insoluble |
Calcolatore di Molarità
|
In vivo |
|||||
Calcolatore di formulazione in vivo (Soluzione chiara)
Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.
Meccanismo dazione
| Targets/IC50/Ki |
p70 S6K1
(Cell-free assay) 160 nM
|
|---|---|
| In vitro |
PF-4708671 è un analogo piperazinil-pirimidinico e il primo inibitore specifico di S6K1. Questo composto non inibisce significativamente l'attività dell'isoforma S6K2 strettamente correlata o di un certo numero di altre chinasi AGC (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 o SGK1). Previene la fosforilazione della proteina S6 mediata da S6K1 in risposta a IGF-1 (fattore di crescita insulino-simile 1), pur non avendo alcun effetto sulla fosforilazione indotta da PMA dei substrati delle chinasi RSK (p90 ribosomal S6 kinase) e MSK (mitogen- and stress-activated kinase) altamente correlate. Si è anche riscontrato che questa sostanza chimica induce la fosforilazione del T-loop e del motivo idrofobico di S6K1, un effetto che dipende da mTORC1 (mTOR complex 1). Non influisce sull'attività di mTORC1.
|
Riferimenti |
Applicazioni
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | p-mTOR / mTOR / p-p70S6K / p70S6K pS6 / S6 / pS6K / S6K1 / pAKT / AKT |
|
30423811 |
| Growth inhibition assay | Cell viability |
|
30423811 |
Supporto tecnico
Istruzioni per la manipolazione
Tel: +1-832-582-8158 Ext:3
Per qualsiasi altra domanda, si prega di lasciare un messaggio.
Domande Frequenti
Domanda 1:
Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for it is suitable for i.p. or not?
Risposta:
The formula "30% PEG400+0.5% Tween80+5% Propylene glycol" on our website is an oral one for this compound. It is a suspension.
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