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TAE684 (NVP-TAE684) ALK inhibidor

Name: TAE684 (NVP-TAE684)
Brand: Selleck Chemicals
SKU: S1108
Rating: 5 (83 reviews)

Cat. No.S1108

TAE684 (NVP-TAE684) es un potente y selectivo inhibidor de ALK que bloqueó el crecimiento de líneas celulares derivadas de ALCL y dependientes de ALK con valores de IC50 entre 2 y 10 nM, 100 veces más sensible para ALK que InsR. Este compuesto induce la detención del ciclo celular y la apoptosis.

TAE684 (NVP-TAE684) ALK inhibidor Chemical Structure

Estructura química

Peso molecular: 614.2

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Control de calidad

Lote: Pureza: 99.73%

99.73

Dianas relacionadas	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Otros ALK Inhibidores	GSK1838705A Repotrectinib (TPX-0005) AZD3463 Ensartinib dihydrochloride AP26113-analog (ALK-IN-1) ASP3026 NVL-655 (Neladalkib) Envonalkib Belizatinib (TSR-011) HG-14-10-04

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Descripción de la actividad
SCC-3	Growth Inhibition Assay	IC50=0.0000603 μM
SF539	Growth Inhibition Assay	IC50=0.000564 μM
DEL	Growth Inhibition Assay	IC50=0.000927 μM
NB1	Growth Inhibition Assay	IC50=0.00162 μM
SR	Growth Inhibition Assay	IC50=0.00277 μM
KARPAS-299	Growth Inhibition Assay	IC50=0.02384 μM
MHH-CALL-2	Growth Inhibition Assay	IC50=0.02952 μM
SU-DHL-1	Growth Inhibition Assay	IC50=0.04865 μM
A4-Fuk	Growth Inhibition Assay	IC50=0.05565 μM
EW-1	Growth Inhibition Assay	IC50=0.10256 μM
NOS-1	Growth Inhibition Assay	IC50=0.10294 μM
EW-16	Growth Inhibition Assay	IC50=0.10568 μM
TE-11	Growth Inhibition Assay	IC50=0.16096 μM
SW982	Growth Inhibition Assay	IC50=0.16478 μM
LAN-6	Growth Inhibition Assay	IC50=0.17443 μM
MZ1-PC	Growth Inhibition Assay	IC50=0.17835 μM
KS-1	Growth Inhibition Assay	IC50=0.19343 μM
PSN1	Growth Inhibition Assay	IC50=0.19631 μM
LC-2-ad	Growth Inhibition Assay	IC50=0.19692 μM
COLO-320-HSR	Growth Inhibition Assay	IC50=0.19776 μM
OPM-2	Growth Inhibition Assay	IC50=0.22669 μM
SK-NEP-1	Growth Inhibition Assay	IC50=0.23524 μM
ALL-PO	Growth Inhibition Assay	IC50=0.24524 μM
CMK	Growth Inhibition Assay	IC50=0.2553 μM
NCI-H1648	Growth Inhibition Assay	IC50=0.27855 μM
SIG-M5	Growth Inhibition Assay	IC50=0.29159 μM
TGBC24TKB	Growth Inhibition Assay	IC50=0.30218 μM
DOHH-2	Growth Inhibition Assay	IC50=0.31204 μM
NB69	Growth Inhibition Assay	IC50=0.31787 μM
MFH-ino	Growth Inhibition Assay	IC50=0.32523 μM
KP-N-RT-BM-1	Growth Inhibition Assay	IC50=0.33123 μM
MONO-MAC-6	Growth Inhibition Assay	IC50=0.33291 μM
ATN-1	Growth Inhibition Assay	IC50=0.33303 μM
NTERA-S-cl-D1	Growth Inhibition Assay	IC50=0.33396 μM
L-540	Growth Inhibition Assay	IC50=0.36988 μM
GB-1	Growth Inhibition Assay	IC50=0.38867 μM
MV-4-11	Growth Inhibition Assay	IC50=0.39446 μM
KG-1	Growth Inhibition Assay	IC50=0.39561 μM
OVCAR-4	Growth Inhibition Assay	IC50=0.40569 μM
NEC8	Growth Inhibition Assay	IC50=0.41292 μM
SK-MM-2	Growth Inhibition Assay	IC50=0.41609 μM
TE-8	Growth Inhibition Assay	IC50=0.4288 μM
697	Growth Inhibition Assay	IC50=0.43215 μM
NB14	Growth Inhibition Assay	IC50=0.43826 μM
GDM-1	Growth Inhibition Assay	IC50=0.47116 μM
HUTU-80	Growth Inhibition Assay	IC50=0.47375 μM
HL-60	Growth Inhibition Assay	IC50=0.48142 μM
OCI-AML2	Growth Inhibition Assay	IC50=0.48328 μM
ML-2	Growth Inhibition Assay	IC50=0.49031 μM
ES4	Growth Inhibition Assay	IC50=0.49109 μM
NCI-H747	Growth Inhibition Assay	IC50=0.4989 μM
RL95-2	Growth Inhibition Assay	IC50=0.50112 μM
TE-15	Growth Inhibition Assay	IC50=0.51124 μM
TE-12	Growth Inhibition Assay	IC50=0.53349 μM
LB1047-RCC	Growth Inhibition Assay	IC50=0.54549 μM
LB831-BLC	Growth Inhibition Assay	IC50=0.55023 μM
NCI-H1355	Growth Inhibition Assay	IC50=0.55184 μM
CTV-1	Growth Inhibition Assay	IC50=0.55624 μM
RXF393	Growth Inhibition Assay	IC50=0.55794 μM
SW872	Growth Inhibition Assay	IC50=0.56724 μM
MPP-89	Growth Inhibition Assay	IC50=0.57884 μM
RPMI-8226	Growth Inhibition Assay	IC50=0.63526 μM
LS-1034	Growth Inhibition Assay	IC50=0.6358 μM
SJSA-1	Growth Inhibition Assay	IC50=0.63725 μM
HOP-62	Growth Inhibition Assay	IC50=0.65033 μM
KGN	Growth Inhibition Assay	IC50=0.66168 μM
D-336MG	Growth Inhibition Assay	IC50=0.66169 μM
LS-411N	Growth Inhibition Assay	IC50=0.67462 μM
TE-1	Growth Inhibition Assay	IC50=0.69074 μM
LB996-RCC	Growth Inhibition Assay	IC50=0.69389 μM
TE-10	Growth Inhibition Assay	IC50=0.71496 μM
NCI-SNU-16	Growth Inhibition Assay	IC50=0.72664 μM
ES8	Growth Inhibition Assay	IC50=0.74975 μM
COLO-800	Growth Inhibition Assay	IC50=0.76695 μM
ES6	Growth Inhibition Assay	IC50=0.77559 μM
L-363	Growth Inhibition Assay	IC50=0.82375 μM
NMC-G1	Growth Inhibition Assay	IC50=0.83233 μM
LU-134-A	Growth Inhibition Assay	IC50=0.83912 μM
SF268	Growth Inhibition Assay	IC50=0.84042 μM
KARPAS-45	Growth Inhibition Assay	IC50=0.84263 μM
TGW	Growth Inhibition Assay	IC50=0.85863 μM
CHP-126	Growth Inhibition Assay	IC50=0.85957 μM
MOLT-16	Growth Inhibition Assay	IC50=0.87589 μM
LB771-HNC	Growth Inhibition Assay	IC50=0.89757 μM
NALM-6	Growth Inhibition Assay	IC50=0.90739 μM
GCIY	Growth Inhibition Assay	IC50=0.95526 μM
IST-MES1	Growth Inhibition Assay	IC50=0.98824 μM
LB2241-RCC	Growth Inhibition Assay	IC50=0.9884 μM
BL-70	Growth Inhibition Assay	IC50=0.99535 μM
NB17	Growth Inhibition Assay	IC50=1.00639 μM
LXF-289	Growth Inhibition Assay	IC50=1.03076 μM
TK10	Growth Inhibition Assay	IC50=1.05063 μM
K5	Growth Inhibition Assay	IC50=1.06274 μM
NCI-H716	Growth Inhibition Assay	IC50=1.07259 μM
HCE-T	Growth Inhibition Assay	IC50=1.08819 μM
GI-1	Growth Inhibition Assay	IC50=1.09798 μM
KARPAS-422	Growth Inhibition Assay	IC50=1.10022 μM
TE-9	Growth Inhibition Assay	IC50=1.11328 μM
SF126	Growth Inhibition Assay	IC50=1.11568 μM
BB30-HNC	Growth Inhibition Assay	IC50=1.13112 μM
NCI-H1304	Growth Inhibition Assay	IC50=1.13338 μM
HEL	Growth Inhibition Assay	IC50=1.14895 μM
HAL-01	Growth Inhibition Assay	IC50=1.15283 μM
SK-LMS-1	Growth Inhibition Assay	IC50=1.15974 μM
SW954	Growth Inhibition Assay	IC50=1.19567 μM
D-283MED	Growth Inhibition Assay	IC50=1.22379 μM
NCI-H1882	Growth Inhibition Assay	IC50=1.2389 μM
GI-ME-N	Growth Inhibition Assay	IC50=1.25208 μM
SK-PN-DW	Growth Inhibition Assay	IC50=1.26348 μM
C2BBe1	Growth Inhibition Assay	IC50=1.29117 μM
A704	Growth Inhibition Assay	IC50=1.32689 μM
KALS-1	Growth Inhibition Assay	IC50=1.3408 μM
ETK-1	Growth Inhibition Assay	IC50=1.34489 μM
LB647-SCLC	Growth Inhibition Assay	IC50=1.34986 μM
OCUB-M	Growth Inhibition Assay	IC50=1.36143 μM
NCI-H720	Growth Inhibition Assay	IC50=1.36378 μM
NB13	Growth Inhibition Assay	IC50=1.37293 μM
GR-ST	Growth Inhibition Assay	IC50=1.38757 μM
DU-4475	Growth Inhibition Assay	IC50=1.45853 μM
HCC2157	Growth Inhibition Assay	IC50=1.46659 μM
RKO	Growth Inhibition Assay	IC50=1.49922 μM
LS-123	Growth Inhibition Assay	IC50=1.51594 μM
NCI-H69	Growth Inhibition Assay	IC50=1.55811 μM
SW962	Growth Inhibition Assay	IC50=1.5613 μM
PF-382	Growth Inhibition Assay	IC50=1.5696 μM
A101D	Growth Inhibition Assay	IC50=1.57113 μM
NB10	Growth Inhibition Assay	IC50=1.57392 μM
NB5	Growth Inhibition Assay	IC50=1.58476 μM
HCE-4	Growth Inhibition Assay	IC50=1.6085 μM
HT-144	Growth Inhibition Assay	IC50=1.6319 μM
NCI-H524	Growth Inhibition Assay	IC50=1.64307 μM
NKM-1	Growth Inhibition Assay	IC50=1.6866 μM
KURAMOCHI	Growth Inhibition Assay	IC50=1.69573 μM
NCI-H187	Growth Inhibition Assay	IC50=1.70036 μM
U-266	Growth Inhibition Assay	IC50=1.73842 μM
BL-41	Growth Inhibition Assay	IC50=1.76272 μM
SK-N-DZ	Growth Inhibition Assay	IC50=1.78309 μM
Daudi	Growth Inhibition Assay	IC50=1.78967 μM
CPC-N	Growth Inhibition Assay	IC50=1.85096 μM
EM-2	Growth Inhibition Assay	IC50=1.851 μM
HCC1187	Growth Inhibition Assay	IC50=1.86241 μM
LP-1	Growth Inhibition Assay	IC50=1.87143 μM
CAS-1	Growth Inhibition Assay	IC50=1.98299 μM
NB7	Growth Inhibition Assay	IC50=2.00555 μM
VA-ES-BJ	Growth Inhibition Assay	IC50=2.01513 μM
SNU-C2B	Growth Inhibition Assay	IC50=2.03351 μM
LOXIMVI	Growth Inhibition Assay	IC50=2.06786 μM
NCI-H1581	Growth Inhibition Assay	IC50=2.11559 μM
IST-SL2	Growth Inhibition Assay	IC50=2.12445 μM
NOMO-1	Growth Inhibition Assay	IC50=2.17683 μM
TE-6	Growth Inhibition Assay	IC50=2.1905 μM
NCI-H526	Growth Inhibition Assay	IC50=2.19141 μM
MSTO-211H	Growth Inhibition Assay	IC50=2.20041 μM
LS-513	Growth Inhibition Assay	IC50=2.22269 μM
NCI-SNU-1	Growth Inhibition Assay	IC50=2.33256 μM
BB65-RCC	Growth Inhibition Assay	IC50=2.37493 μM
GT3TKB	Growth Inhibition Assay	IC50=2.39972 μM
OS-RC-2	Growth Inhibition Assay	IC50=2.42341 μM
NCI-H2126	Growth Inhibition Assay	IC50=2.43674 μM
SK-UT-1	Growth Inhibition Assay	IC50=2.47467 μM
DMS-114	Growth Inhibition Assay	IC50=2.61524 μM
ONS-76	Growth Inhibition Assay	IC50=2.63641 μM
8-MG-BA	Growth Inhibition Assay	IC50=2.65414 μM
BOKU	Growth Inhibition Assay	IC50=2.72764 μM
LAMA-84	Growth Inhibition Assay	IC50=2.79912 μM
ES1	Growth Inhibition Assay	IC50=2.81804 μM
NCI-H1395	Growth Inhibition Assay	IC50=2.82012 μM
A388	Growth Inhibition Assay	IC50=2.9617 μM
NCCIT	Growth Inhibition Assay	IC50=3.08862 μM
HD-MY-Z	Growth Inhibition Assay	IC50=3.13203 μM
NCI-H510A	Growth Inhibition Assay	IC50=3.18943 μM
NCI-N87	Growth Inhibition Assay	IC50=3.2002 μM
SCLC-21H	Growth Inhibition Assay	IC50=3.26859 μM
SH-4	Growth Inhibition Assay	IC50=3.28797 μM
QIMR-WIL	Growth Inhibition Assay	IC50=3.32849 μM
KM12	Growth Inhibition Assay	IC50=3.33544 μM
ST486	Growth Inhibition Assay	IC50=3.53883 μM
HC-1	Growth Inhibition Assay	IC50=3.62028 μM
BV-173	Growth Inhibition Assay	IC50=3.64088 μM
EW-24	Growth Inhibition Assay	IC50=3.66434 μM
LU-65	Growth Inhibition Assay	IC50=3.6871 μM
ECC4	Growth Inhibition Assay	IC50=3.7756 μM
ARH-77	Growth Inhibition Assay	IC50=4.11067 μM
BC-3	Growth Inhibition Assay	IC50=4.13068 μM
SNB75	Growth Inhibition Assay	IC50=4.2619 μM
MEG-01	Growth Inhibition Assay	IC50=4.27419 μM
NCI-H1417	Growth Inhibition Assay	IC50=4.28443 μM
MDA-MB-134-VI	Growth Inhibition Assay	IC50=4.30601 μM
Becker	Growth Inhibition Assay	IC50=4.47336 μM
DMS-153	Growth Inhibition Assay	IC50=4.66475 μM
TGBC1TKB	Growth Inhibition Assay	IC50=4.68515 μM
EW-3	Growth Inhibition Assay	IC50=4.76248 μM
KE-37	Growth Inhibition Assay	IC50=4.86196 μM
NCI-H23	Growth Inhibition Assay	IC50=4.87227 μM
MC116	Growth Inhibition Assay	IC50=4.94126 μM
NH-12	Growth Inhibition Assay	IC50=4.96439 μM
CTB-1	Growth Inhibition Assay	IC50=4.97721 μM
KM-H2	Growth Inhibition Assay	IC50=5.05323 μM
MOLT-4	Growth Inhibition Assay	IC50=5.1183 μM
NCI-H2141	Growth Inhibition Assay	IC50=5.14268 μM
EB-3	Growth Inhibition Assay	IC50=5.17504 μM
NCI-H1522	Growth Inhibition Assay	IC50=5.26322 μM
MRK-nu-1	Growth Inhibition Assay	IC50=5.43633 μM
no-11	Growth Inhibition Assay	IC50=5.47087 μM
CESS	Growth Inhibition Assay	IC50=5.58034 μM
KMOE-2	Growth Inhibition Assay	IC50=5.58659 μM
REH	Growth Inhibition Assay	IC50=6.25618 μM
KU812	Growth Inhibition Assay	IC50=6.42791 μM
SK-N-FI	Growth Inhibition Assay	IC50=6.60674 μM
MMAC-SF	Growth Inhibition Assay	IC50=7.06492 μM
RCC10RGB	Growth Inhibition Assay	IC50=7.22977 μM
NCI-H322M	Growth Inhibition Assay	IC50=7.33335 μM
NB6	Growth Inhibition Assay	IC50=7.54899 μM
MN-60	Growth Inhibition Assay	IC50=7.69215 μM
NCI-H1092	Growth Inhibition Assay	IC50=8.01734 μM
EKVX	Growth Inhibition Assay	IC50=8.47066 μM
D-263MG	Growth Inhibition Assay	IC50=8.55396 μM
NCI-H209	Growth Inhibition Assay	IC50=8.64006 μM
IST-SL1	Growth Inhibition Assay	IC50=8.89892 μM
ACN	Growth Inhibition Assay	IC50=9.19157 μM
MHH-PREB-1	Growth Inhibition Assay	IC50=9.21219 μM
EW-11	Growth Inhibition Assay	IC50=9.65396 μM
KASUMI-1	Growth Inhibition Assay	IC50=9.7877 μM
KINGS-1	Growth Inhibition Assay	IC50=10.2347 μM
EVSA-T	Growth Inhibition Assay	IC50=10.3192 μM
DSH1	Growth Inhibition Assay	IC50=10.3972 μM
COLO-824	Growth Inhibition Assay	IC50=10.8669 μM
K052	Growth Inhibition Assay	IC50=10.9322 μM
SK-MEL-2	Growth Inhibition Assay	IC50=10.9939 μM
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Información química, almacenamiento y estabilidad

Peso molecular	614.2	Fórmula	C₃₀H₄₀ClN₇O₃S	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	761439-42-3	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	N/A			Smiles	CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC

Solubilidad

In vitro
Lote:

DMSO : 10 mg/mL (16.28 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:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 40%PEG300 2 5%TWEEN80 3 45%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	1.000mg/ml (1.63mM)	Taking the 1 mL working solution as an example, add 100 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol, pH 4 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	10.000mg/ml (16.28mM)	Taking the 1 mL working solution as an example, add 300 μL of 33.33 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol, pH 4, to the above system, mix evenly to clarify it; then continue Add 645 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

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	ALK (Cell lines) 2-10 nM
In vitro	TAE684 (NVP-TAE684) no presenta una reactividad cruzada significativa contra otras quinasas. Este compuesto inhibe potentemente la proliferación de células Ba/F3 NPM-ALK con una IC50 de 3 nM, sin afectar la supervivencia de las células Ba/F3 incluso a 1 µM. También inhibe la proliferación de líneas celulares ALCL humanas que expresan NPM-ALK, incluyendo Karpas-299 y SU-DHL-1, con una IC50 de 2–5 nM. El modelado molecular revela que L258 puede ser uno de los principales determinantes de la selectividad de la quinasa para este químico. Su tratamiento resulta en una inhibición rápida y sostenida de la fosforilación de NPM-ALK. El compuesto induce apoptosis y detención en fase G1 en células Ba/F3 que expresan NPM-ALK y líneas celulares de pacientes con ALCL. Supera notablemente la resistencia en células H3122 CR, que albergan el oncogén de fusión EML4-ALK, disminuyendo el crecimiento celular, suprimiendo la fosforilación de ALK e induciendo apoptosis. El crecimiento de neuritas inducido por la expresión del mutante mALK R1279Q podría ser completamente inhibido por este compuesto a 30 nM.
Ensayo de quinasa	Ensayos enzimáticos in vitro.
Ensayo de quinasa	Todos los ensayos enzimáticos in vitro se realizan en Upstate Biotechnology, con la excepción de InsR e IGF-1R. Para determinar el IC50 de TAE684 (NVP-TAE684) contra InsR e IGF-1R, se realiza un ensayo de fluorescencia resuelta en el tiempo homogéneo. ATP (10 mM) y 20 mg/ml de PolyEY biotinilado (Glu, Tyr 4:1) se combinan con 50 nL de diluciones seriadas de este compuesto (10-500 nM) y 4 ng de enzima InsR en presencia del tampón de reacción de la quinasa (20 mM Tris-Cl, pH 7,5/10 mM MgCl₂/3 mM MnCl₂/1 mM DTT/10 mM NaVO₄/0,1 mg/ml de BSA). Los ensayos se incuban durante 1 hora a temperatura ambiente. Las reacciones se terminan añadiendo 10 mL de la solución de detección que contiene 50 mM de EDTA, 500 mM de KF, 0,5 mg/ml de BSA, 5 mg/mL de anticuerpo anti-fosfotirosina Mab PT66-K marcado con criptato de Eu3+ y 5 mg/mL de estreptavidina-XLent. La reacción se incuba durante media hora y las señales de fluorescencia se leen en Analyst GT.
In vivo	Después de 4 semanas de tratamiento con TAE684 (NVP-TAE684) a 3 y 10 mg/kg, hay un retraso significativo en el desarrollo del linfoma y una reducción de 100 a 1.000 veces en la señal de luminiscencia, sin signos de toxicidad relacionada con el compuesto o la enfermedad en el modelo de linfoma de Karpas-299. Este tratamiento con el compuesto también induce la regresión de la enfermedad en linfomas Karpas-299 establecidos y regula a la baja la expresión de CD30. También muestra una impresionante actividad antitumoral contra tumores de xenoinjerto H3122 CR. Además, el tratamiento con este químico mejora el fenotipo de ojo rugoso de ambos mutantes de ALK, especialmente el observado con ALKR1275Q.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/17185414/ [2] https://pubmed.ncbi.nlm.nih.gov/21502504/ [3] https://pubmed.ncbi.nlm.nih.gov/21838707/

Aplicaciones

Métodos	Biomarcadores	Imágenes	PMID
Growth inhibition assay	Cell viability		18594010
Western blot	p-ROS1 / ROS1 p-ALK / ALK / p-STAT3 / STAT3 / p-ERK / ERK / p-AKT / AKT / Survivin / BIM / PARP		25351743

Soporte técnico

Instrucciones de manipulación

Tel: +1-832-582-8158 Ext:3

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