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CC-5013 (Lenalidomide) Immunomodulator

Name: CC-5013 (Lenalidomide)
Brand: Selleck Chemicals
SKU: S1029
Rating: 5 (177 reviews)

Cat.Nr.S1029

Lenalidomide is een TNF-α secretie-remmer met een IC50 van 13 nM in PBMC's. Lenalidomide (CC-5013) is een ligand van ubiquitine E3 ligase cereblon (CRBN), en veroorzaakt selectieve ubiquitinatie en degradatie van twee lymfoïde transcriptiefactoren, IKZF1 en IKZF3, door de CRBN-CRL4 ubiquitine ligase. Lenalidomide bevordert cleaved caspase-3 expressie en remt VEGF expressie en induceert apoptose.

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

Chemische structuur

Moleculair gewicht: 259.26

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Kwaliteitscontrole

Batch: Zuiverheid: 99.97%

99.97

Gerelateerde doelwitten	Proteasome E1 Activating E3 Ligase DUB p97 SUMO E2 conjugating
Overige E3 ligase Ligand Inhibitoren	CC-99282

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	259.26	Formule	C₁₃H₁₃N₃O₃	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	191732-72-6	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	CC-5013			Smiles	C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3N

Oplosbaarheid

In vitro
Batch:

DMSO : 51 mg/mL (196.71 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	CRBN VEGF TNF-α (PBMCs) 13 nM
In vitro	Lenalidomide induceert sterk IL-2 en sIL-2R productie. Deze door de verbinding geïnduceerde tyrosinefosforylatie van CD28 op T-cellen wordt gevolgd door een stroomafwaartse activering van NF-κB. Deze verbinding en pomalidomide remmen autoubiquitinatie van CRBN in HEK293 T-cellen die thalidomide-bindend competent wild-type CRBN tot expressie brengen, maar niet thalidomide-bindend defectief CRBN(YW/AA). Overexpressie van CRBN wild-type eiwit, maar niet CRBN(YW/AA) mutant eiwit, in KMS12 myeloomcellen, versterkt pomalidomide-gemedieerde reducties in c-myc en IRF4 expressie en verhoogt p21(WAF-1) expressie. Langdurige selectie voor resistentie tegen deze verbinding in H929 myeloomcellijnen gaat gepaard met een reductie in CRBN, terwijl in DF15R myeloomcellen die resistent zijn tegen zowel pomalidomide als deze chemische stof, CRBN-eiwit ondetecteerbaar is. Deze chemische stof voorkomt de inductie van defecten door de expressie van tumorcelremmende moleculen te downreguleren. Het voorkomt de inductie van tumor-geïnduceerde T-cel lytische synapsdysfunctie. Deze verbindingbehandeling blokkeert door CLL-cellen geïnduceerde T-cel actine synapsdysfunctie, bootst antilichaamblokkade na en downreguleert de expressie van CLL-remmende liganden en hun receptoren op T-cellen. Deze behandeling voorkomt tumor-geïnduceerde immuunsuppressie in FL, DLBCL, HL, MM, SCC en OC en downreguleert immunosuppressieve ligandexpressie op alle onderzochte tumorcellen. De CTL-doodfunctie neemt significant toe na antilichaamblokkade van CLL-remmende liganden of deze chemische behandeling vergeleken met controlebehandelingen. Behandeling van autologe CLL-T-cel co-culturen met dit middel keert de verminderde CD8⁺ T-cel lytische synapsvorming en granzyme B-trafficking om.
Kinase Assay	Analyse voor remming van TNF-synthese door humane PBMC's
Kinase Assay	Humane PBMC's van normale donoren worden verkregen door Ficoll-Hypaque dichtheidsgradientcentrifugatie. Cellen (10⁶ cellen/mL) worden gekweekt in RPMI aangevuld met 10 AB+ serum, 2 mM L-glutamine, 100 U/mL penicilline en 100 μg/mL streptomycine. Lenalidomide wordt opgelost in DMSO bij 20 mg/mL; verdere verdunning gebeurt met kweekmedium. De uiteindelijke DMSO-concentratie in alle analyses, inclusief de controles, is 0,25%. Deze verbinding wordt 1 uur voorafgaand aan de toevoeging van LPS aan cellen toegevoegd. PBMC's (10⁶ cellen/mL) worden gestimuleerd met 1 μg/mL LPS van Salmonella minnesota R595. Cellen, in drievoud, worden gedurende 18-20 uur bij 37 °C in 5% CO₂ met LPS geïncubeerd. Supernatanten worden vervolgens geoogst en geanalyseerd op cytokineniveaus. In sommige experimenten worden supernatanten tot gebruik bij -70 °C ingevroren. De cellevensvatbaarheid wordt bepaald door de Trypanblauwe exclusiekleurstofmethode. De concentratie van TNFα in de kweeksupernatanten wordt bepaald door ELISA. Deze chemische stof wordt in minimaal drie afzonderlijke experimenten getest. Het percentage remming wordt bepaald als 100 × [1 - (cytokine(experimenteel)/cytokine(controle))].
In vivo	De inductie van angiogenese door bFGF wordt significant geremd door orale behandeling met Lenalidomide op een dosisafhankelijke manier. Deze verbinding vermindert significant het percentage gevasculariseerd gebied van 5,16% (controlegroep) tot 2,58% (50 mg/kg). Het vermindert significant de berekende totale MVL van 21,07 (controle) tot 8,11 (50 mg/kg). Deze chemische stof remt significant de migratie van HUVEC's door de fibronectine-gecoate membranen naar 0,1 ng/mL bFGF bij 100 μM, 1 ng/mL VEGF bij concentraties van 10 μM en 100 μM.
Referenties	[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

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	phospho-IKKβ / IKKβ MDM2 / p-MDM2 / p-p53 / p53		22698399
Growth inhibition assay	Cell viability		22698399

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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	--

Technische ondersteuning

Gebruiksaanwijzing

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

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Veelgestelde vragen

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

Antwoord:
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.

Vraag 2:
what is the procedure to resuspend it？

Antwoord:
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.

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