Home Angiogenesis Src Inhibitor Saracatinib (AZD0530)

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Saracatinib (AZD0530) Src Inhibitor

Kat.-Nr.: S1006

Saracatinib (AZD0530) ist ein potenter Src-Inhibitor mit einer IC50 von 2,7 nM in zellfreien Assays und ist potent gegen c-Yes, Fyn, Lyn, Blk, Fgr und Lck; weniger aktiv für Abl und EGFR (L858R und L861Q). Es induziert Autophagy und befindet sich in Phase 2/3.
Saracatinib (AZD0530) Src Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 542.03

Springe zu

Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.99%
99.99

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
CTV-1 Growth Inhibition Assay IC50=0.06143 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.1599 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.23688 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.265 μM SANGER
TE-15 Growth Inhibition Assay IC50=0.27412 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=0.28116 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.3268 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=0.44196 μM SANGER
K-562 Growth Inhibition Assay IC50=0.44967 μM SANGER
D-336MG Growth Inhibition Assay IC50=0.50304 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.60529 μM SANGER
EW-24 Growth Inhibition Assay IC50=0.62693 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.65249 μM SANGER
NCCIT Growth Inhibition Assay IC50=0.73218 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=0.79049 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.86203 μM SANGER
TE-8 Growth Inhibition Assay IC50=0.87275 μM SANGER
A704 Growth Inhibition Assay IC50=0.8921 μM SANGER
TK10 Growth Inhibition Assay IC50=0.90669 μM SANGER
KS-1 Growth Inhibition Assay IC50=1.19779 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=1.20507 μM SANGER
RXF393 Growth Inhibition Assay IC50=1.2436 μM SANGER
KGN Growth Inhibition Assay IC50=1.27687 μM SANGER
NB69 Growth Inhibition Assay IC50=1.37497 μM SANGER
TE-11 Growth Inhibition Assay IC50=1.43418 μM SANGER
TE-1 Growth Inhibition Assay IC50=1.44105 μM SANGER
ST486 Growth Inhibition Assay IC50=1.45852 μM SANGER
HOP-62 Growth Inhibition Assay IC50=1.50246 μM SANGER
EW-16 Growth Inhibition Assay IC50=1.55083 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=1.55453 μM SANGER
TE-10 Growth Inhibition Assay IC50=1.66252 μM SANGER
RL95-2 Growth Inhibition Assay IC50=1.66902 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=1.71782 μM SANGER
MFH-ino Growth Inhibition Assay IC50=1.7787 μM SANGER
GB-1 Growth Inhibition Assay IC50=1.79833 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=1.84688 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=1.88574 μM SANGER
SW982 Growth Inhibition Assay IC50=1.92093 μM SANGER
KALS-1 Growth Inhibition Assay IC50=1.98722 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=2.05958 μM SANGER
GI-1 Growth Inhibition Assay IC50=2.16084 μM SANGER
SW962 Growth Inhibition Assay IC50=2.17178 μM SANGER
SW872 Growth Inhibition Assay IC50=2.18507 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=2.25714 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=2.29356 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=2.35723 μM SANGER
BL-70 Growth Inhibition Assay IC50=2.47422 μM SANGER
SW954 Growth Inhibition Assay IC50=2.57408 μM SANGER
SNB75 Growth Inhibition Assay IC50=2.68594 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=2.72379 μM SANGER
GCIY Growth Inhibition Assay IC50=2.87005 μM SANGER
KU812 Growth Inhibition Assay IC50=3.05299 μM SANGER
LXF-289 Growth Inhibition Assay IC50=3.12109 μM SANGER
ETK-1 Growth Inhibition Assay IC50=3.20767 μM SANGER
SF126 Growth Inhibition Assay IC50=3.31174 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=3.557 μM SANGER
KNS-42 Growth Inhibition Assay IC50=3.65 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=3.73433 μM SANGER
PF-382 Growth Inhibition Assay IC50=3.83698 μM SANGER
SH-4 Growth Inhibition Assay IC50=4.25259 μM SANGER
KM12 Growth Inhibition Assay IC50=4.32416 μM SANGER
NB5 Growth Inhibition Assay IC50=4.41864 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=4.65256 μM SANGER
Becker Growth Inhibition Assay IC50=4.66416 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=4.81344 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=4.82373 μM SANGER
LS-123 Growth Inhibition Assay IC50=5.49684 μM SANGER
SF268 Growth Inhibition Assay IC50=5.61262 μM SANGER
A388 Growth Inhibition Assay IC50=5.63667 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=6.01811 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=6.02075 μM SANGER
ES4 Growth Inhibition Assay IC50=6.53074 μM SANGER
SR Growth Inhibition Assay IC50=6.58807 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=6.73206 μM SANGER
KLE Growth Inhibition Assay IC50=6.78377 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=6.98466 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=7.82737 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=7.94904 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=8.42808 μM SANGER
GDM-1 Growth Inhibition Assay IC50=8.97292 μM SANGER
LC4-1 Growth Inhibition Assay IC50=9.00911 μM SANGER
MLMA Growth Inhibition Assay IC50=9.15006 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=9.30192 μM SANGER
BOKU Growth Inhibition Assay IC50=9.96466 μM SANGER
EVSA-T Growth Inhibition Assay IC50=10.6568 μM SANGER
D-283MED Growth Inhibition Assay IC50=10.9176 μM SANGER
NB1 Growth Inhibition Assay IC50=11.0242 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=11.178 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=11.1806 μM SANGER
NB7 Growth Inhibition Assay IC50=11.3297 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=12.9567 μM SANGER
697 Growth Inhibition Assay IC50=13.2701 μM SANGER
CTB-1 Growth Inhibition Assay IC50=13.5948 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=13.9234 μM SANGER
BE-13 Growth Inhibition Assay IC50=14.3915 μM SANGER
SKM-1 Growth Inhibition Assay IC50=14.4499 μM SANGER
TE-6 Growth Inhibition Assay IC50=14.7591 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=14.7898 μM SANGER
ECC4 Growth Inhibition Assay IC50=17.0277 μM SANGER
ES3 Growth Inhibition Assay IC50=17.4655 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=17.4949 μM SANGER
NB10 Growth Inhibition Assay IC50=18.5256 μM SANGER
L-540 Growth Inhibition Assay IC50=18.8109 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=19.51 μM SANGER
HH Growth Inhibition Assay IC50=20.0099 μM SANGER
MPP-89 Growth Inhibition Assay IC50=23.2289 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=23.8658 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=23.9255 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=24.5989 μM SANGER
EKVX Growth Inhibition Assay IC50=26.0203 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=26.434 μM SANGER
Daudi Growth Inhibition Assay IC50=27.0773 μM SANGER
ALL-PO Growth Inhibition Assay IC50=27.081 μM SANGER
NB6 Growth Inhibition Assay IC50=27.488 μM SANGER
ES6 Growth Inhibition Assay IC50=27.9123 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=28.0373 μM SANGER
K5 Growth Inhibition Assay IC50=28.1287 μM SANGER
ES1 Growth Inhibition Assay IC50=28.7773 μM SANGER
LC-1F Growth Inhibition Assay IC50=29.7346 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=30.7317 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=32.5598 μM SANGER
D-247MG Growth Inhibition Assay IC50=32.9773 μM SANGER
TE-5 Growth Inhibition Assay IC50=33.0362 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=33.5048 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=33.7666 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=33.7928 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=35.144 μM SANGER
A253 Growth Inhibition Assay IC50=35.7429 μM SANGER
HCC1599 Growth Inhibition Assay IC50=36.7053 μM SANGER
EB-3 Growth Inhibition Assay IC50=36.9518 μM SANGER
GOTO Growth Inhibition Assay IC50=37.3224 μM SANGER
SW684 Growth Inhibition Assay IC50=41.8495 μM SANGER
DEL Growth Inhibition Assay IC50=42.0522 μM SANGER
HT-144 Growth Inhibition Assay IC50=42.1676 μM SANGER
TE-9 Growth Inhibition Assay IC50=43.4596 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=44.3925 μM SANGER
HAL-01 Growth Inhibition Assay IC50=44.5034 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=44.7392 μM SANGER
CP67-MEL Growth Inhibition Assay IC50=45.6241 μM SANGER
NB17 Growth Inhibition Assay IC50=45.6643 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=45.9464 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=46.0119 μM SANGER
HCE-4 Growth Inhibition Assay IC50=46.5968 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=46.7682 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=47.0895 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=47.1622 μM SANGER
HCE-T Growth Inhibition Assay IC50=47.6828 μM SANGER
PSN1 Growth Inhibition Assay IC50=47.7813 μM SANGER
NIH3T3 Function assay Inhibition of human c-Src in NIH3T3 cells, IC50 = 0.0027 μM. 17064066
HEK293 Function assay 1 hr Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0398 μM. 29941193
HEK293 Function assay 1 hr Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.418 μM. 29941193
Rh30 Antiproliferative assay 48 hrs Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay, IC50 = 10.1 μM. 23787099
Huh7 Antiviral assay 2.5 uM 5 days Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control 17360676
Huh7 Antiviral assay 2.5 uM 6 days Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control 17360676
Vero Antiviral assay 2.5 uM 4 days Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control 17360676
Vero Antiviral assay 2.5 uM 6 days Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control 17360676
C6/36 Antiviral assay 2.5 uM 4 days Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control 17360676
C6/36 Antiviral assay 2.5 uM 5 days Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control 17360676
Vero Antiviral assay 3 days Antiviral activity against Dengue virus infected in african green monkey Vero cells administered after viral challenge after 3 days by viral plaque assay 17360676
Vero Antiviral assay 2.5 uM 5 days Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control 17360676
Huh7 Antiviral assay 2.5 uM 4 days Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control 17360676
C6/36 Antiviral assay 2.5 uM 6 days Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control 17360676
HEK293 Function assay 0.1 to 1 uM 16 hrs Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting 26191369
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
HEK293 Function assay 0.1 to 1 uM 16 hrs Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting 26191369
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Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 542.03 Formel

C27H32ClN5O5

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 379231-04-6 SDF herunterladen Lagerung von Stammlösungen

Synonyme N/A Smiles CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 100 mg/mL (184.49 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus (Mechanism of Action)

Merkmale
The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.
Targets/IC50/Ki
c-Src
(Cell-free assay)
2.7 nM
LCK
(Cell-free assay)
<4 nM
c-YES
(Cell-free assay)
4 nM
EGFR (L861Q)
(Cell-free assay)
4 nM
Lyn
(Cell-free assay)
5 nM
EGFR (L858R)
(Cell-free assay)
5 nM
Fyn
(Cell-free assay)
10 nM
FGR
(Cell-free assay)
10 nM
BLK
(Cell-free assay)
11 nM
v-Abl
(Cell-free assay)
30 nM
EGFR
(Cell-free assay)
66 nM
c-Kit
(Cell-free assay)
200 nM
EphA2
(Cell-free assay)
236 nM
In vitro

Saracatinib (AZD0530) also potently inhibits other Src tyrosine kinase family members including c-Yes, Fyn, Lyn, Blk, Fgr, and Lck with IC50 from 4-10 nM. It sensitively inhibits Src Y530F NIH 3T3 with IC50 of 80 nM. This compound significantly impairs the invasion of HT1080 cells through a 3-dimensional collagen matrix and completely inhibits EGF-induced cell scattering in NBT-II bladder cancer cells. It potent inhibits Src activation in DU145 and PC3 cells, which through inhibition of Y419 phosphorylation. It inhibits the growth of prostate cancer including PC3, DU145, CWR22Rv1 and LNCaP, while showing low activity in LAPC-4, PZ-HPV7 and RWPE-1 cells. It induces cell cycle arrest at G1/S but not caspase 3 cleavages. It also significantly inhibits DU145 and PC3 migration in the Boyden chamber. It gives a potent and sustained blockage of AKT and enhances the sensitivity to irradiation in A549 and Calu-6 cells. It inhibits osteoclast in activity, resorption and formation. It also reversibly prevents osteoclast precursor migration.

Kinase-Assay
Kinase-Assay
Die IC50 der Tyrosinkinaseaktivität wird mittels eines enzymgekoppelten Immunosorbent-Assays (ELISA) mit rekombinanten katalytischen Domänen einer Reihe von Rezeptor- und Nicht-Rezeptor-Tyrosinkinasen gemessen (in einigen Fällen wird nur ein Teil der katalytischen Domäne verwendet). Diese Verbindung dosis liegt im Bereich von 0,001-10 mM. Spezifitätsassays gegen eine Reihe von Serin/Threonin-Kinasen werden unter Verwendung eines Filterfangassays mit 32P durchgeführt. Kurz gesagt, Multidrop-384-Platten, die 0,5 μL Saracatinib (AZD0530) oder Kontrollen (nur DMSO oder pH 3,0 Pufferkontrollen) enthalten, werden 5 min lang mit 15 μL Enzym plus Peptid/Proteinsubstrat inkubiert, bevor die Reaktion durch Zugabe von 10 μL 20 mM Mg-ATP eingeleitet wird. Für alle Enzyme wird die Endkonzentration an die Michaelis-Konstante (Km) angenähert. Die Assays werden 30 min bei Raumtemperatur durchgeführt, bevor sie durch Zugabe von 5 μL Orthophosphorsäure beendet werden. Nach dem Mischen werden die Well-Inhalte auf eine P81 UniFilter-Platte gesammelt, wobei Orthophosphorsäure als Waschpuffer verwendet wird. Anschließend wird die IC50 berechnet.
In vivo

Saracatinib (AZD0530) shows great tumor growth inhibition in Src3T3 allografts and a moderate growth delay in Calu-6, MDA-MB-231, AsPc-1 and BT474C xenografts. This compound also shows great antitumor activity in orthotopic DU145 xenograft mice at a dose of 25mg/kg (orally administered, daily).

Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/19372577/
  • [5] https://pubmed.ncbi.nlm.nih.gov/19216789/
  • [6] https://pubmed.ncbi.nlm.nih.gov/18493848/
  • [7] https://pubmed.ncbi.nlm.nih.gov/19451593/

Anwendungen (Applications)

Methoden Biomarker Bilder PMID
Western blot pY576-FAK / pY861-FAK / FAK pY418 Src / Src / pY410 CAS / CAS / Py421 Cortactin / Cortactin p-Akt / p-mTOR / Akt / mTOR / p-S6 / S6 / p-AMPKα / AMPKα
S1006-WB1
20551056
Growth inhibition assay Cell number
S1006-viability1
24349321

Klinische Studieninformationen (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2026-09-02)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
NCT04307953 ACTIVE_NOT_RECRUITING
Fibrodysplasia Ossificans Progressiva
Amsterdam UMC, location VUmc
 2020-08-05 PHASE2
NCT04598919 ACTIVE_NOT_RECRUITING
Idiopathic Pulmonary Fibrosis (IPF)
National Jewish Health
 2020-11-12 PHASE1; PHASE2
NCT03661125 UNKNOWN
Parkinson Disease Psychosis
King's College London
 2019-04-11 EARLY_PHASE1
NCT04598919 Active not recruiting
Idiopathic Pulmonary Fibrosis (IPF)
National Jewish Health|Yale University|Icahn School of Medicine at Mount Sinai|AstraZeneca|National Center for Advancing Translational Sciences (NCATS)|Baylor University|International Center for Health Outcomes and Innovation Research
 2020-11-12 Phase 1|Phase 2
NCT04307953 Recruiting
Fibrodysplasia Ossificans Progressiva
Amsterdam UMC location VUmc|Royal National Orthopaedic Hospital NHS Trust|Klinikum Garmisch-Patenkirchen|University of Oxford|Brigham and Women''s Hospital|AstraZeneca|Innovative Medicines Initiative
 2020-08-05 Phase 2
NCT02737202 TERMINATED
Pulmonary Lymphangioleiomyomatosis
Baylor College of Medicine
 2016-04 PHASE2

Häufig gestellte Fragen (Frequently Asked Questions)

Frage 1:
What is its half-life?

Antwort:
Based on the following paper, its half-life in vivo is around 40 hours and it reaches its peak level around 2–4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long