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AZD1480 JAK inhibidor

Cat. No.S2162

AZD1480 es un nuevo inhibidor de JAK2 competitivo de ATP con una IC50 de 0,26 nM en un ensayo sin células, selectividad contra JAK3 y Tyk2, y en menor medida contra JAK1. Fase 1.
AZD1480 JAK inhibidor Chemical Structure

Estructura química

Peso molecular: 348.77

Saltar a

Control de calidad

Lote: Pureza: 99.16%
99.16

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad PMID
SW620 Function Assay 5 μM 48 h DMSO blocks JAK2/STAT3 signaling 25954974
LoVo  Function Assay 5 μM 48 h DMSO blocks JAK2/STAT3 signaling 25954974
HN5 Growth Inhibition Assay 72 h EC50=3.81 ± 1.99 μM 25810010
Cal33 Growth Inhibition Assay 72 h EC50=3.37 ± 0.75 μM 25810010
UM-22B Growth Inhibition Assay 72 h EC50=2.66 ± 0.24 μM 25810010
686LN Growth Inhibition Assay 72 h EC50=2.05 ± 1.33 μM 25810010
UM SCC-1 Growth Inhibition Assay 72 h EC50=1.67 ± 0.42 μM 25810010
UM-22A Growth Inhibition Assay 72 h EC50=1.32 ± 0.39 μM 25810010
OSC19 Growth Inhibition Assay 72 h EC50=1.26 ± 0.20 μM 25810010
PCI-52 Growth Inhibition Assay 72 h EC50=1.00 ± 0.09 μM 25810010
PCI-15B Growth Inhibition Assay 72 h EC50=0.99 ± 1.74 μM 25810010
UMSCC-1 Function Assay 0.0005-1.6 μM 24 h abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner 25810010
Cal33 Function Assay 0.0005-3.8 μM 24 h abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner 25810010
HH5 Function Assay 0.0005-3.8 μM 24 h abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner 25810010
UM-22A Function Assay 0.0005-1.6 μM 24 h abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner 25810010
A1847 Function Assay 0.05-10 μM 24 h DMSO  reduces phosphorylated STAT3 levels 25646015
OVCAR-5 Function Assay 0.05-10 μM 24 h DMSO  reduces phosphorylated STAT3 levels 25646015
OVCAR-8 Function Assay 0.05-10 μM 24 h DMSO  reduces phosphorylated STAT3 levels 25646015
MOVCAR-5447 Function Assay 0.05-10 μM 24 h DMSO  reduces phosphorylated STAT3 levels 25646015
MOVCAR-5009 Function Assay 0.05-10 μM 24 h DMSO  reduces phosphorylated STAT3 levels 25646015
A1847 Cell Viability Assay 0.05-10 μM 72 h DMSO reduces cell viability at the concerntration of 5 μM 25646015
OVCAR-5 Cell Viability Assay 0.05-10 μM 72 h DMSO reduces cell viability at the concerntration of 5 μM 25646015
OVCAR-8  Cell Viability Assay 0.05-10 μM 72 h DMSO reduces cell viability at the concerntration of 5 μM 25646015
OVCAR-5  Apoptosis Assay 0.5/1/5 μM 48 h DMSO induces significant apoptosis at high concerntration 25646015
OVCAR-8  Apoptosis Assay 0.5/1/5 μM 48 h DMSO induces significant apoptosis at high concerntration 25646015
AKRSL Cell Viability Assay 72 h IC50＞10 μM 25504635
PALJDL Cell Viability Assay 72 h IC50=2.4 μM 25504635
MO4 Function Assay 0.5/1/5 μM 6 h inhibits P-STAT3 expression  25149535
DU145  Function Assay 0-200 nM 1 h  suppresses IL-6-activated Stat3 and ERK1/2 signaling 24577942
DU145  Function Assay 800 nM 72 h suppresses IL-6-induced migratory 24577942
CWR22Rv1 Function Assay 800 nM 72 h suppresses IL-6-induced migratory 24577942
N592 Growth Inhibition Assay IC50=0.84 μM 24158701
H82 Growth Inhibition Assay IC50=1.37 μM 24158701
GLC4 Growth Inhibition Assay IC50=1.79 μM 24158701
H526 Growth Inhibition Assay IC50=3.08 μM 24158701
H1173 Growth Inhibition Assay IC50=2.39 μM 24158701
DMS114 Growth Inhibition Assay IC50=0.73 μM 24158701
NCI-N592 Function Assay 0.3/1/3 μM 24 h induces G2/M cell cycle arrest 24158701
GLC4 Function Assay 0.3/1/3 μM 24 h induces G2/M cell cycle arrest 24158701
NCI-H82 Function Assay 0.3/1/3 μM 24 h induces G2/M cell cycle arrest 24158701
NCI-N592 Apoptosis Assay 0.3/1/3 μM 48 h increases the level of cleaved-Caspase 3 24158701
GLC4 Apoptosis Assay 0.3/1/3 μM 48 h increases the level of cleaved-Caspase 3 24158701
NCI-H82 Apoptosis Assay 0.3/1/3 μM 48 h increases the level of cleaved-Caspase 3 24158701
CWR22Rv1  Apoptosis Assay IC50=0.482 μM 23942095
CWR22Pc Apoptosis Assay IC50=0.438 μM 23942095
PC-3 Apoptosis Assay IC50=1.755 μM 23942095
DU145 Apoptosis Assay IC50=3.517 μM 23942095
RC165N Apoptosis Assay IC50=2.083 μM 23942095
ARPE19 Growth Inhibition Assay DMSO IC50=24.38 μM 23531921
HEK293 Growth Inhibition Assay DMSO IC50=8.67 μM 23531921
KCNR Growth Inhibition Assay DMSO IC50=0.46 μM 23531921
SY5Y Growth Inhibition Assay DMSO IC50=0.36 μM 23531921
BE2 Growth Inhibition Assay DMSO IC50=0.71 μM 23531921
AS Growth Inhibition Assay DMSO IC50=1.53 μM 23531921
NGP Growth Inhibition Assay DMSO IC50=0.56 μM 23531921
IMR32 Growth Inhibition Assay DMSO IC50=0.66 μM 23531921
LAN5 Growth Inhibition Assay DMSO IC50=1.04 μM 23531921
RH18 Growth Inhibition Assay DMSO IC50=1.42 μM 23531921
RH30 Growth Inhibition Assay DMSO IC50=1.25 μM 23531921
RH17 Growth Inhibition Assay DMSO IC50=2.51 μM 23531921
RH28 Growth Inhibition Assay DMSO IC50=4.28 μM 23531921
RH36 Growth Inhibition Assay DMSO IC50=5.37 μM 23531921
RH41 Growth Inhibition Assay DMSO IC50=0.48 μM 23531921
RD Growth Inhibition Assay DMSO IC50=4.32 μM 23531921
TC32 Growth Inhibition Assay DMSO IC50=3.85 μM 23531921
TC71 Growth Inhibition Assay DMSO IC50=4.33 μM 23531921
KCNR Apoptosis Assay 0.5/1.0/2.5 μM 24 h DMSO induces an increase in caspase 3/7 activity 23531921
SY5Y Apoptosis Assay 0.5/1.0/2.5 μM 24 h DMSO induces an increase in caspase 3/7 activity 23531921
Rh18 Apoptosis Assay 0.5/1.0/2.5 μM 24 h DMSO induces an increase in caspase 3/7 activity 23531921
TC32 Apoptosis Assay 0.5/1.0/2.5 μM 24 h DMSO induces an increase in caspase 3/7 activity 23531921
KCNR Function Assay 0.5/1.0/2.5/5 μM 24 h DMSO inhibits both endogenous constitutive and IL-6-induced STAT3 activation 23531921
SY5Y Function Assay 0.5/1.0/2.5/5 μM 24 h DMSO inhibits both endogenous constitutive and IL-6-induced STAT3 activation 23531921
Rh18 Function Assay 0.5/1.0/2.5/5 μM 24 h DMSO inhibits both endogenous constitutive and IL-6-induced STAT3 activation 23531921
TC32 Function Assay 0.5/1.0/2.5/5 μM 24 h DMSO inhibits both endogenous constitutive and IL-6-induced STAT3 activation 23531921
TPC-1 Growth Inhibition Assay 1 µM 0-4 d DMSO inhibits cell growth after 2 d treatment 23056499
MZ-CRC1  Growth Inhibition Assay 1 µM 0-5 d DMSO inhibits cell growth after 1 d treatment 23056499
TT  Growth Inhibition Assay 1 µM 0-4 d DMSO inhibits cell growth after 1 d treatment 23056499
TPC-1 Function Assay 1 µM 72 h DMSO induces G1 blockage 23056499
MZ-CRC1  Function Assay 1 µM 72 h DMSO induces G1 blockage 23056499
TT  Function Assay 1 µM 72 h DMSO induces G1 blockage 23056499
MZ-CRC1  Apoptosis Assay 1 µM 48 h DMSO induces apoptosis 23056499
TT  Apoptosis Assay 1 µM 48 h DMSO induces apoptosis 23056499
HD-LM2 Growth Inhibition Assay 72 h DMSO IC50=7.844 μM 22829094
L-428 Growth Inhibition Assay 72 h DMSO IC50=7.947 μM 22829094
KM-H2 Growth Inhibition Assay 72 h DMSO IC50=1.308 μM 22829094
L-540 Growth Inhibition Assay 72 h DMSO IC50=8.216 μM 22829094
HD-LM2 Function Assay 0.1/0.5/1/5 μM 72 h DMSO inhibits STAT3, STAT5 and STAT6 phosphorylation 22829094
L-428 Function Assay 0.1/0.5/1/5 μM 72 h DMSO inhibits STAT3, STAT5 and STAT6 phosphorylation 22829094
KM-H2 Function Assay 0.1/0.5/1/5 μM 72 h DMSO inhibits STAT3, STAT5 and STAT6 phosphorylation 22829094
L-540 Function Assay 0.1/0.5/1/5 μM 72 h DMSO inhibits STAT3, STAT5 and STAT6 phosphorylation 22829094
HD-LM2 Apoptosis Assay 1/5 μM 72 h DMSO induces apoptosis 22829094
L-428 Apoptosis Assay 1/5 μM 72 h DMSO induces apoptosis 22829094
KM-H2 Apoptosis Assay 1/5 μM 72 h DMSO induces apoptosis 22829094
L-540 Apoptosis Assay 1/5 μM 72 h DMSO induces apoptosis 22829094
U251-MG Function Assay 1 µM 0-16 h inhibits constitutive STAT-3 and JAK2 activation 22027691
U87-MG Function Assay 1 µM 0-16 h inhibits constitutive STAT-3 and JAK2 activation 22027691
4C8 Function Assay 1 µM 0-16 h inhibits constitutive STAT-3 and JAK2 activation 22027691
U251-MG Growth Inhibition Assay 1/10 µM 24/48/72 h inhibits cell proliferation at a concentration of 10 µM 22027691
U87-MG Growth Inhibition Assay 1/10 µM 24/48/72 h inhibits cell proliferation at a concentration of 10 µM 22027691
4C8 Growth Inhibition Assay 1/10 µM 24/48/72 h inhibits cell proliferation at a concentration of 10 µM 22027691
U266 Apoptosis Assay 0.5-2 μM 48/72 h induces apoptosis dose dependently 21164517
Kms.11 Apoptosis Assay 0.5-2 μM 48/72 h induces apoptosis dose dependently 21164517
8226 Apoptosis Assay 0.5-2 μM 48/72 h induces apoptosis dose dependently 21164517
SET2 Growth inhibition assay 48 hrs Growth inhibition of human SET2 cells expressing Jak2 V617F mutant after 48 hrs by MTS assay, GI50 = 0.016 μM. 21138246
SET2 Function assay 1 hr Inhibition of Stat3 phosphorylation in human SET2 cells after 1 hr by Western blotting, IC50 = 0.023 μM. 21138246
SET2 Function assay 1 hr Inhibition of Stat5 phosphorylation in human SET2 cells after 1 hr by Western blotting, IC50 = 0.025 μM. 21138246
HEL Function assay 1 hr Inhibition of Stat5 phosphorylation in human HEL cells after 1 hr by Western blotting, IC50 = 0.041 μM. 21138246
Ba/F3 Function assay Inhibition of Stat5 phosphorylation in mouse Ba/F3 cells expressing TEL-Jak2, IC50 = 0.046 μM. 21138246
UKE1 Growth inhibition assay 48 hrs Growth inhibition of human UKE1 cells expressing Jak2 V617F mutant after 48 hrs by MTS assay, GI50 = 0.054 μM. 21138246
BA/F3 Growth inhibition assay 48 hrs Growth inhibition of mouse BA/F3 cells expressing Tel-JAK2 kinase after 48 hrs by MTS assay, GI50 = 0.06 μM. 21138246
HEL Function assay 1 hr Inhibition of Stat3 phosphorylation in human HEL cells after 1 hr by Western blotting, IC50 = 0.08 μM. 21138246
HEL Growth inhibition assay 48 hrs Growth inhibition of human HEL cells expressing Jak2 V617F mutant after 48 hrs by MTS assay, GI50 = 0.39 μM. 21138246
BA/F3 Growth inhibition assay 48 hrs Growth inhibition of mouse BA/F3 cells expressing Tel-JAK1 kinase after 48 hrs by MTS assay, GI50 = 0.7 μM. 21138246
BA/F3 Growth inhibition assay 48 hrs Growth inhibition of mouse BA/F3 cells expressing Tel-Tyk2 kinase after 48 hrs by MTS assay, GI50 = 2 μM. 21138246
BA/F3 Growth inhibition assay 48 hrs Growth inhibition of mouse BA/F3 cells expressing Tel-JAK3 kinase after 48 hrs by MTS assay, GI50 = 2.1 μM. 21138246
UKE1 Function assay 1 hr Inhibition of Stat5 phosphorylation in human UKE1 cells after 1 hr by Western blotting 21138246
SW620 Cell cycle assay 3.3 uM 24 hrs Cell cycle arrest in human SW620 cells assessed as accumulation at G2/M phase at 3.3 uM after 24 hrs by flow cytometry 21138246
HEL Function assay 0.3 uM 5 mins Inhibition of Stat5 phosphorylation in human HEL cells at 0.3 uM after 5 mins by Western blotting 21138246
HEL Function assay 0.3 uM 30 to 60 mins Inhibition of Stat5 phosphorylation in human HEL cells at 0.3 uM after 30 to 60 mins by Western blotting 21138246
BA/F3 Antitumor assay 30 mg/kg 12 hrs Antitumor activity against mouse BA/F3 cells expressing Tel-JAK2 xenografted in NCr mouse assessed as reduction of phosphorylated Stat5 level in spleen at 30 mg/kg, po after 12 hrs by Western blotting 21138246
HEL Function assay 0.3 uM 5 mins Inhibition of Stat3 phosphorylation in human HEL cells at 0.3 uM after 5 mins by Western blotting 21138246
HEL Function assay 0.3 uM 30 to 60 mins Inhibition of Stat3 phosphorylation in human HEL cells at 0.3 uM after 30 to 60 mins by Western blotting 21138246
Hs578T Function assay 1 uM 24 hrs Inhibition of STAT3C-mediated transcription in human Hs578T cells at 1 uM after 24 hrs by luciferase reporter gene assay 24978112
NCI-H1975 Function assay 0.003 to 3 uM 2 hrs Inhibition of JAK1 in human NCI-H1975 cells assessed as reduction in STAT3 phosphorylation at 0.003 to 3 uM after 2 hrs by Western blot analysis 26614408
HEL 92.1.7 Function assay 2 hrs Inhibition of JAK2 in human HEL 92.1.7 cells assessed as reduction in STAT5 phosphorylation after 2 hrs by Western blot analysis 26614408
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
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Información química, almacenamiento y estabilidad

Peso molecular 348.77 Fórmula

C14H14ClFN8

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 935666-88-9 Descargar SDF Almacenamiento de soluciones madre

Sinónimos N/A Smiles CC1=CC(=NN1)NC2=NC(=NC=C2Cl)NC(C)C3=NC=C(C=N3)F

Solubilidad

In vitro
Lote:

DMSO : 70 mg/mL (200.7 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Targets/IC50/Ki
JAK2
(Cell-free assay)
0.26 nM
In vitro
5μM AZD1480 induce la detención en G2/M y la muerte celular al inhibir las quinasas Aurora. Este compuesto es un potente inhibidor de JAK2 que puede suprimir el crecimiento, la supervivencia, así como la señalización de FGFR3 y STAT3 y los objetivos posteriores, incluida la ciclina D2 en células de mieloma múltiple humano. A bajas concentraciones micromolares, bloquea la proliferación celular e induce la apoptosis de las líneas celulares de mieloma. Este químico bloquea eficazmente la fosforilación constitutiva e inducida por estímulos de JAK1, JAK2 y STAT-3 tanto en células de glioma humanas como murinas, y conduce a una disminución de la proliferación celular y la inducción de apoptosis. Es un potente inhibidor competitivo de molécula pequeña de la quinasa JAK1/2, y es capaz de inhibir la fosforilación de STAT3 y el crecimiento tumoral de una manera dependiente de STAT3. Este inhibidor inhibe la angiogénesis tumoral y la metástasis en parte al afectar el microambiente tumoral.
Ensayo de quinasa
ensayos de quinasa
Los estudios de inhibición de AZD1480 se realizan utilizando Jak1, Jak2 o Jak3 recombinantes en condiciones de tampón de 50 mM HEPES pH 7,3, 1 mM DTT, 0,01% Tween-20, 50 mM/ml BSA y 10 mM MgCl2. La enzima Jak3 se expresa como fusión de GST N-terminal en células de insecto y se purifica mediante cromatografía de afinidad con glutatión y de exclusión por tamaño. Las enzimas se ensayan en presencia de este compuesto (respuesta a la dosis de 10 puntos, por triplicado, de 8,3 μM a 0,3 nM en pasos de dilución de media logaritmo) utilizando 1,5 μM de sustrato peptídico (Jak1: FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2 y Jak3: FAM-SRCtide) y se criban bajo sus ATP Km respectivos (Jak1: 55 μM, Jak2: 15 μM, Jak3: 3 μM) y una concentración de ATP fisiológica aproximada de 5 mM. Los péptidos fosforilados y no fosforilados se separan y cuantifican mediante un sistema Caliper LC3000 para calcular el porcentaje de inhibición.
In vivo
AZD1480 inhibe la fosforilación de STAT3 en un modelo de xenoinjerto de tumores sólidos humanos y mieloma múltiple. In vivo, este compuesto inhibe el crecimiento de tumores subcutáneos y aumenta la supervivencia de ratones con tumores de glioblastoma intracraneal (GBM) al inhibir la actividad de STAT-3, lo que indica que la inhibición farmacológica de la vía JAK/STAT-3 por este químico debe considerarse para su estudio en el tratamiento de pacientes con tumores de GBM. Bloquea la infiltración pulmonar de células mieloides y la formación de metástasis pulmonares en modelos murinos singénicos experimentales y modelos metastásicos espontáneos. Además, este agente reduce la angiogénesis y la metástasis en un modelo de tumor de xenoinjerto humano. El inhibidor de Jak2 suprime el crecimiento de xenoinjertos de tumores sólidos humanos que albergan actividad persistente de Stat3.
Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/21920898/
  • [5] https://pubmed.ncbi.nlm.nih.gov/19962667/

Aplicaciones

Métodos Biomarcadores Imágenes PMID
Western blot p-STAT3 / STAT3 / p-JAK2 / JAK2 p-STAT1 / STAT1 / p-STAT5 / STAT5 / p-STAT6 / STAT6 p-ERK / ERK / p-p38 / p38 / SOCS3 / p-SHP2 / SHP2
S2162-WB1
22027691
Immunofluorescence pSTAT5
S2162-IF1
30140255
Growth inhibition assay Cell proliferation Cell viability
S2162-viability1
22027691

Información del ensayo clínico

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT Reclutamiento Condiciones Patrocinador/Colaboradores Fecha de inicio Fases
NCT01219543 Terminated
Solid Tumour|Advanced Solid Malignancies|Child-Pugh A to B7 Advanced Hepatocellular Carcinoma|EGFR and/or ROS Mutant NSCLC|Lung Metastasis Carcinoma|Gastric Cancer
AstraZeneca
 November 2010 Phase 1
NCT01112397 Terminated
Solid Malignancies
AstraZeneca
 April 2010 Phase 1

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