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CC-5013 (Lenalidomide) Inmunomodulador

Name: CC-5013 (Lenalidomide)
Brand: Selleck Chemicals
SKU: S1029
Rating: 5 (178 reviews)

Cat. No.S1029

Lenalidomide es un inhibidor de la secreción de TNF-α con IC50 de 13 nM en PBMC. Lenalidomide (CC-5013) es un ligando de la ubiquitin E3 ligase cereblon (CRBN), y causa ubiquitilación y degradación selectiva de dos factores de transcripción linfoideos, IKZF1 e IKZF3, por la ubiquitin ligasa CRBN-CRL4. Lenalidomide promueve la expresión de la cleaved caspase-3 e inhibe la expresión de VEGF e induce la apoptosis.

CC-5013 (Lenalidomide) E3 ligase Ligand Químico Chemical Structure

Estructura química

Peso molecular: 259.26

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.97%

99.97

Dianas relacionadas	Proteasome E1 Activating E3 Ligase DUB SUMO p97 E2 conjugating
Otros E3 ligase Ligand Inhibidores	CC-99282

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
LB771-HNC	Growth Inhibition Assay			IC50=2.15038 μM	SANGER
L-363	Growth Inhibition Assay			IC50=2.92212 μM	SANGER
JAR	Growth Inhibition Assay			IC50=2.97001 μM	SANGER
EoL-1-cell	Growth Inhibition Assay			IC50=4.10515 μM	SANGER
BT-549	Growth Inhibition Assay			IC50=6.21849 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=7.89512 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=8.67585 μM	SANGER
HMV-II	Growth Inhibition Assay			IC50=10.0172 μM	SANGER
HCC1806	Growth Inhibition Assay			IC50=11.4467 μM	SANGER
KASUMI-1	Growth Inhibition Assay			IC50=11.571 μM	SANGER
SK-MEL-28	Growth Inhibition Assay			IC50=11.9764 μM	SANGER
RPMI-8226	Growth Inhibition Assay			IC50=12.6241 μM	SANGER
T47D	Growth Inhibition Assay			IC50=13.2099 μM	SANGER
HOP-62	Growth Inhibition Assay			IC50=13.48 μM	SANGER
A2058	Growth Inhibition Assay			IC50=13.8199 μM	SANGER
SW620	Growth Inhibition Assay			IC50=14.2473 μM	SANGER
LCLC-103H	Growth Inhibition Assay			IC50=14.4892 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=14.5796 μM	SANGER
PANC-08-13	Growth Inhibition Assay			IC50=14.9108 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=15.3979 μM	SANGER
DEL	Growth Inhibition Assay			IC50=15.499 μM	SANGER
K5	Growth Inhibition Assay			IC50=16.1486 μM	SANGER
SK-MEL-24	Growth Inhibition Assay			IC50=16.4652 μM	SANGER
ACN	Growth Inhibition Assay			IC50=16.5297 μM	SANGER
H9	Growth Inhibition Assay			IC50=16.626 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=17.143 μM	SANGER
HSC-4	Growth Inhibition Assay			IC50=17.6601 μM	SANGER
IGROV-1	Growth Inhibition Assay			IC50=17.783 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=17.9968 μM	SANGER
LN-405	Growth Inhibition Assay			IC50=19.9076 μM	SANGER
MSTO-211H	Growth Inhibition Assay			IC50=20.3573 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=20.5759 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=22.1563 μM	SANGER
ES3	Growth Inhibition Assay			IC50=22.6963 μM	SANGER
SBC-1	Growth Inhibition Assay			IC50=23.8696 μM	SANGER
CTV-1	Growth Inhibition Assay			IC50=25.0149 μM	SANGER
HuP-T3	Growth Inhibition Assay			IC50=25.4009 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=25.5407 μM	SANGER
HDLM-2	Growth Inhibition Assay			IC50=28.2026 μM	SANGER
ABC-1	Growth Inhibition Assay			IC50=29.6974 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=29.7317 μM	SANGER
WM-115	Growth Inhibition Assay			IC50=30.3099 μM	SANGER
SW1990	Growth Inhibition Assay			IC50=30.33 μM	SANGER
HCC70	Growth Inhibition Assay			IC50=30.7346 μM	SANGER
KYSE-520	Growth Inhibition Assay			IC50=30.8839 μM	SANGER
JEG-3	Growth Inhibition Assay			IC50=31.1614 μM	SANGER
C8166	Growth Inhibition Assay			IC50=31.2274 μM	SANGER
SK-OV-3	Growth Inhibition Assay			IC50=31.6755 μM	SANGER
NCI-H526	Growth Inhibition Assay			IC50=32.683 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=32.9568 μM	SANGER
ECC10	Growth Inhibition Assay			IC50=34.7443 μM	SANGER
A2780	Growth Inhibition Assay			IC50=35.3601 μM	SANGER
KY821	Growth Inhibition Assay			IC50=35.7681 μM	SANGER
MKN1	Growth Inhibition Assay			IC50=36.2137 μM	SANGER
EKVX	Growth Inhibition Assay			IC50=37.4212 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=38.3885 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=39.7789 μM	SANGER
COR-L105	Growth Inhibition Assay			IC50=40.4746 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay			IC50=41.2069 μM	SANGER
Mewo	Growth Inhibition Assay			IC50=41.9871 μM	SANGER
BCPAP	Growth Inhibition Assay			IC50=43.7917 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=44.2776 μM	SANGER
NCI-H1693	Growth Inhibition Assay			IC50=46.6986 μM	SANGER
H-EMC-SS	Growth Inhibition Assay			IC50=48.3224 μM	SANGER
697	Growth Inhibition Assay			IC50=50.3545 μM	SANGER
KP-N-YS	Growth Inhibition Assay			IC50=52.3142 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=52.7024 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=52.8559 μM	SANGER
NCI-H2342	Growth Inhibition Assay			IC50=53.0508 μM	SANGER
KYSE-270	Growth Inhibition Assay			IC50=53.6364 μM	SANGER
LU-135	Growth Inhibition Assay			IC50=55.1853 μM	SANGER
OE33	Growth Inhibition Assay			IC50=55.818 μM	SANGER
ML-2	Growth Inhibition Assay			IC50=55.9489 μM	SANGER
KMOE-2	Growth Inhibition Assay			IC50=56.2893 μM	SANGER
Daoy	Growth Inhibition Assay			IC50=56.3204 μM	SANGER
KNS-62	Growth Inhibition Assay			IC50=57.0142 μM	SANGER
NBsusSR	Growth Inhibition Assay			IC50=57.5705 μM	SANGER
UACC-257	Growth Inhibition Assay			IC50=58.6264 μM	SANGER
LU-139	Growth Inhibition Assay			IC50=58.826 μM	SANGER
CAL-85-1	Growth Inhibition Assay			IC50=58.8643 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=58.8942 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=59.091 μM	SANGER
A3-KAW	Growth Inhibition Assay			IC50=59.2809 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=59.6287 μM	SANGER
A388	Growth Inhibition Assay			IC50=60.449 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=60.9905 μM	SANGER
GCT	Growth Inhibition Assay			IC50=61.0786 μM	SANGER
K-562	Growth Inhibition Assay			IC50=61.5333 μM	SANGER
NCI-H1666	Growth Inhibition Assay			IC50=61.875 μM	SANGER
NCI-H1993	Growth Inhibition Assay			IC50=63.4043 μM	SANGER
NCI-H358	Growth Inhibition Assay			IC50=65.0121 μM	SANGER
NB6	Growth Inhibition Assay			IC50=65.988 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=67.0798 μM	SANGER
DOK	Growth Inhibition Assay			IC50=67.4948 μM	SANGER
HT-1376	Growth Inhibition Assay			IC50=69.8314 μM	SANGER
NEC8	Growth Inhibition Assay			IC50=70.1243 μM	SANGER
G-402	Growth Inhibition Assay			IC50=70.9395 μM	SANGER
GR-ST	Growth Inhibition Assay			IC50=71.172 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=71.4434 μM	SANGER
CHP-212	Growth Inhibition Assay			IC50=71.965 μM	SANGER
KU812	Growth Inhibition Assay			IC50=72.9702 μM	SANGER
Becker	Growth Inhibition Assay			IC50=73.1489 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay			IC50=74.7486 μM	SANGER
A498	Growth Inhibition Assay			IC50=74.9308 μM	SANGER
NCI-H69	Growth Inhibition Assay			IC50=75.7663 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=78.6147 μM	SANGER
CAL-33	Growth Inhibition Assay			IC50=78.9939 μM	SANGER
COLO-680N	Growth Inhibition Assay			IC50=79.1007 μM	SANGER
D-283MED	Growth Inhibition Assay			IC50=79.812 μM	SANGER
ATN-1	Growth Inhibition Assay			IC50=81.1187 μM	SANGER
NCI-N87	Growth Inhibition Assay			IC50=81.7296 μM	SANGER
MHH-NB-11	Growth Inhibition Assay			IC50=81.8849 μM	SANGER
HEL	Growth Inhibition Assay			IC50=82.4134 μM	SANGER
NB69	Growth Inhibition Assay			IC50=83.0033 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=83.2575 μM	SANGER
COLO-829	Growth Inhibition Assay			IC50=85.4912 μM	SANGER
ONS-76	Growth Inhibition Assay			IC50=85.7908 μM	SANGER
EW-3	Growth Inhibition Assay			IC50=86.2032 μM	SANGER
EW-11	Growth Inhibition Assay			IC50=86.4336 μM	SANGER
SW900	Growth Inhibition Assay			IC50=87.2053 μM	SANGER
MOLT-13	Growth Inhibition Assay			IC50=87.2243 μM	SANGER
HuP-T4	Growth Inhibition Assay			IC50=91.0405 μM	SANGER
HCC1419	Growth Inhibition Assay			IC50=91.6374 μM	SANGER
CAL-72	Growth Inhibition Assay			IC50=92.0219 μM	SANGER
Mo-T	Growth Inhibition Assay			IC50=92.7697 μM	SANGER
OC-314	Growth Inhibition Assay			IC50=92.8821 μM	SANGER
BHT-101	Growth Inhibition Assay			IC50=93.1 μM	SANGER
EW-18	Growth Inhibition Assay			IC50=93.8462 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=94.3055 μM	SANGER
MDA-MB-361	Growth Inhibition Assay			IC50=96.0516 μM	SANGER
DF15	Function assay		4 hrs	Induction of CRL4/CRBN ubiquitin ligase-mediated aiolos degradation in human DF15 cells expressing pLOC-ePL-tagged aiolos after 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay, EC50 = 0.053 μM.	28358507
DF15	Function assay		4 hrs	Induction of cereblon-mediated ikaros degradation in human DF15 cells expressing ePL-tagged ikaros after 4 hrs by luminometric analysis, EC50 = 0.067 μM.	28425720
DF15	Function assay		4 hrs	Induction of cereblon-mediated aiolos degradation in human DF15 cells expressing ePL-tagged aiolos after 4 hrs by luminometric analysis, EC50 = 0.087 μM.	28425720
T-cells	Function assay		2 to 3 days	Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA, EC50 = 0.15 μM.	23168019
NAMALWA	Antiproliferative assay		72 hrs	Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50 = 0.36 μM.	23168019
CD34+ progenitor cells	Function assay		14 days	Decrease in erythroid differentiation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient assessed as CD36 expression after 14 days	17576924
CD34+ progenitor cells	Function assay		14 days	Decrease in myeloid differentiation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient assessed as CD33 expression after 14 days	17576924
CD34+ progenitor cells	Function assay		14 days	Decrease in erythroid differentiation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient assessed as glycophorin A expression after 14 days	17576924
CD34+ progenitor cells	Growth inhibition assay		14 days	Inhibition of cell proliferation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient after 14 days	17576924
CD34+ progenitor cells	Growth inhibition assay		14 days	Growth inhibition of CD34+ progenitor cells from non-del(5q) myelodysplastic syndrome patient after 14 days	17576924
DF15	Function assay	0.1 to 10 uM	5 hrs	Induction of cereblon-mediated aiolos degradation in human DF15 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis	28425720
OPM2	Function assay	0.1 to 10 uM	5 hrs	Induction of cereblon-mediated aiolos degradation in human OPM2 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis	28425720
DF15	Function assay	0.1 to 10 uM	5 hrs	Induction of cereblon-mediated ikaros degradation in human DF15 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis	28425720
OPM2	Function assay	0.1 to 10 uM	5 hrs	Induction of cereblon-mediated ikaros degradation in human OPM2 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis	28425720
EC9706	Antiproliferative assay	150 ug/mL	48 hrs	Antiproliferative activity against human EC9706 cells at 150 ug/mL after 48 hrs by CCK-8 assay	28757066
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	259.26	Fórmula	C₁₃H₁₃N₃O₃	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	191732-72-6	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	CC-5013			Smiles	C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3N

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 51 mg/mL (196.71 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.
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	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	10.000mg/ml (38.57mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 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 make it clear; then continue to add 500 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.

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 (Mechanism of Action)

Targets/IC₅₀/Ki	CRBN VEGF TNF-α (PBMCs) 13 nM
In vitro	La lenalidomida induce fuertemente la producción de IL-2 y sIL-2R. Esta fosforilación de tirosina de CD28 en células T, inducida por el compuesto, es seguida por una activación posterior de NF-κB. Este compuesto y la pomalidomida inhiben la autoubiquitinación de CRBN en células HEK293 T que expresan CRBN de tipo salvaje competente para la unión a la talidomida, pero no CRBN(YW/AA) defectuoso en la unión a la talidomida. La sobreexpresión de la proteína CRBN de tipo salvaje, pero no de la proteína mutante CRBN(YW/AA), en células de mieloma KMS12, amplifica las reducciones mediadas por la pomalidomida en la expresión de c-myc e IRF4 y aumenta la expresión de p21(WAF-1). La selección a largo plazo para la resistencia a este compuesto en líneas celulares de mieloma H929 se acompaña de una reducción en CRBN, mientras que en células de mieloma DF15R resistentes tanto a la pomalidomida como a este químico, la proteína CRBN es indetectable. Este químico previene la inducción de defectos al regular a la baja la expresión de moléculas inhibidoras de células tumorales. Previene la inducción de disfunción sináptica lítica de células T inducida por tumores. El tratamiento con este compuesto bloquea la disfunción sináptica de actina de células T inducida por células de LLC, imita el bloqueo de anticuerpos y regula a la baja la expresión de ligandos inhibidores de LLC y sus receptores en células T. Este tratamiento previene la inmunosupresión inducida por tumores en FL, DLBCL, HL, MM, SCC y OC y regula a la baja la expresión de ligando inmunosupresor en todas las células tumorales examinadas. La función de muerte de CTL aumenta significativamente después del bloqueo de anticuerpos de ligandos inhibidores de LLC o el tratamiento con este químico en comparación con los tratamientos de control. El tratamiento de cocultivos de células T de LLC autólogos con este agente revierte la formación de sinapsis lítica de células T CD8⁺ y el tráfico de granzima B.
Ensayo de quinasa	Ensayo de inhibición de la síntesis de TNF por PBMC humanas
Ensayo de quinasa	Las PBMC humanas de donantes normales se obtienen mediante centrifugación en gradiente de densidad de Ficoll-Hypaque. Las células (10⁶ células/mL) se cultivan en RPMI suplementado con 10 suero AB+, 2 mM de l-glutamina, 100 U/mL de penicilina y 100 μg/mL de estreptomicina. La lenalidomida se disuelve en DMSO a 20 mg/mL; la dilución posterior se realiza con medio de cultivo. La concentración final de DMSO en todos los ensayos, incluidos los controles, es del 0,25 %. Este compuesto se añade a las células 1 hora antes de la adición de LPS. Las PBMC (10⁶ células/mL) se estimulan con 1 μg/mL de LPS de Salmonella minnesota R595. Las células, por triplicado, se incuban con LPS durante 18-20 horas a 37 °C en 5 % de CO₂. Los sobrenadantes se recolectan y se analizan para determinar los niveles de citocinas. En algunos experimentos, los sobrenadantes se mantienen congelados a -70 °C hasta su uso. La viabilidad celular se analiza mediante el método de exclusión del colorante azul de tripano. La concentración de TNFα en los sobrenadantes de cultivo se determina mediante ELISA. Este químico se ensaya en un mínimo de tres experimentos separados. El porcentaje de inhibición se determina como 100 × [1 - (citocina(experimental)/citocina(control))].
In vivo	La inducción de angiogénesis por bFGF es significativamente inhibida por el tratamiento oral de Lenalidomide de manera dosis-dependiente. Este compuesto disminuye significativamente el porcentaje de área vascularizada del 5,16 % (grupo control) al 2,58 % (50 mg/kg). Reduce significativamente el MVL total calculado de 21,07 (control) a 8,11 (50 mg/kg). Este químico inhibe significativamente la migración de HUVEC a través de las membranas recubiertas de fibronectina hacia 0,1 ng/mL de bFGF a 100 μM, 1 ng/mL de VEGF a concentraciones de 10 μM y 100 μM.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/10386948/ [2] https://pubmed.ncbi.nlm.nih.gov/16255679/ [3] https://pubmed.ncbi.nlm.nih.gov/22552008/ [4] https://pubmed.ncbi.nlm.nih.gov/22547582/ [5] https://pubmed.ncbi.nlm.nih.gov/15797261/ [6] https://pubmed.ncbi.nlm.nih.gov/21968939/ [7] https://pubmed.ncbi.nlm.nih.gov/19951978/ [8] http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=74&abstractID=50171 [9] http://cancerres.aacrjournals.org/cgi/content/short/72/8_MeetingAbstracts/1942?rss=1

Aplicaciones (Applications)

Métodos	Biomarcadores	Imágenes	PMID
Western blot	phospho-IKKβ / IKKβ MDM2 / p-MDM2 / p-p53 / p53		22698399
Growth inhibition assay	Cell viability		22698399

Información del ensayo clínico (Clinical Trial Information)

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

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT06177028	Not yet recruiting	Cognitive Impairment Mild\|Cognitive Dysfunction\|Amyloid Plaque\|Neurodegenerative Disease Hereditary\|Inflammation Brain	St. Joseph''s Hospital and Medical Center Phoenix\|Texas Tech University	January 2 2024	Phase 2
NCT06149286	Recruiting	Relapsed/Refractory Follicular Lymphoma\|Marginal Zone Lymphoma (MZL)	Regeneron Pharmaceuticals	December 28 2023	Phase 3
NCT06299553	Recruiting	DLBCL - Diffuse Large B Cell Lymphoma	Incyte Biosciences Italy S.r.l	December 4 2023	--

Preguntas frecuentes (Frequently Asked Questions)

Pregunta 1:
What is the formulation for its injection (i.p.) in mice?

Respuesta:
This paper has the information you need: http://link.springer.com/article/10.1208/s12248-012-9401-2. Add it to the appropriate volume of sterile phosphate-buffered saline (PBS) containing 1% hydrochloric acid (HCl). The pH of this preparation was adjusted to 7.0–7.6 using sodium hydroxide and sterile filtered using a 0.22 μm Steriflip filter.

Pregunta 2:
what is the procedure to resuspend it？

Respuesta:
This compound can be resuspended by DMSO, with a solubility of about 52 mg/mL (200.57 mM). For in vivo study, the working solution can be prepared with the vehicle of: 30% PEG400/0.5% Tween80/5% propylene glycol for oral administration.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):