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Silmitasertib (CX-4945) sodium salt Casein Kinase 2 Inhibitor

Name: Silmitasertib (CX-4945) sodium salt
Brand: Selleck Chemicals
SKU: S0707
Rating: 5 (62 reviews)

N° Cat.S0707

Le Silmitasertib (CX-4945) sodium salt est un inhibiteur puissant, biodisponible par voie orale et sélectif de la caséine kinase 2 (CK2) avec une IC50 de 1 nM contre CK2α et CK2α'.

Silmitasertib (CX-4945) sodium salt Casein Kinase inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 371.75

Aller à

Contrôle qualité

Lot : Pureté : 99.95%

99.95

Cibles apparentées	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Autre Casein Kinase Inhibiteurs	Silmitasertib (CX-4945) D 4476 TBB IC261 PF-670462 Ellagic Acid hydrate TTP 22 Longdaysin PF 4800567 (E/Z)-GO289

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Description de lactivité	PMID
Jurkat	Function assay			Inhibition of CK2 in human Jurkat cells assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay, IC50=0.1μM	21174434
MIAPaCa2	Antiproliferative assay		4 days	Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay, IC50=1.1μM	21174434
PC3	Antiproliferative assay		4 days	Antiproliferative activity against human PC3 cells after 4 days by alamar blue assay, IC50=2.1μM	21174434
HCT116	Antiproliferative assay		4 days	Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay, IC50=2.2μM	21174434
H1299	Antiproliferative assay		4 days	Antiproliferative activity against human H1299 cells after 4 days by alamar blue assay, IC50=2.4μM	21174434
Jurkat	Antiproliferative assay		4 days	Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay, IC50=2.5μM	21174434
A549	Antiproliferative assay		4 days	Antiproliferative activity against human A549 cells after 4 days by alamar blue assay, IC50=3μM	21174434
A375	Antiproliferative assay		4 days	Antiproliferative activity against human A375 cells after 4 days by alamar blue assay, IC50=3.9μM	21174434
BxPC3	Antiproliferative assay		4 days	Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay, IC50=4.4μM	21174434
LNCAP	Antiproliferative assay		4 days	Antiproliferative activity against human LNCAP cells after 4 days by alamar blue assay, IC50=4.7μM	21174434
K562	Antiproliferative assay		4 days	Antiproliferative activity against human K562 cells after 4 days by alamar blue assay, IC50=5.3μM	21174434
MDA-MB-231	Antiproliferative assay		4 days	Antiproliferative activity against human MDA-MB-231 cells after 4 days by alamar blue assay, IC50=6.4μM	21174434
MCF7	Antiproliferative assay		4 days	Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay, IC50=8.9μM	21174434
Hs 578T	Antiproliferative assay		4 days	Antiproliferative activity against human Hs 578T cells after 4 days by alamar blue assay, IC50=13.1μM	21174434
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50=5.2μM	22339433
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, IC50=6.5μM	22339433
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, IC50=8.2μM	22339433
LNCAP	Cytotoxicity assay		4 days	Cytotoxicity against human LNCAP cells assessed as cell viability after 4 days by CCK8 method, IC50=4.59μM	22832316
LNCAP	Apoptosis assay	>10 uM	1 to 2 days	Induction of apoptosis in human LNCAP cells assessed as increase in caspase3 activation at >10 uM after 1 to 2 days	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2alpha in human LNCAP cells assessed as reduction of survivin expression at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	1 to 10 uM	12 hrs	Inhibition of CK2 in human LNCAP cells assessed as androgen receptor nuclear translocation at 1 to 10 uM after 12 hrs by Alexa Fluor 488 staining based fluorescence assay	22832316
LNCAP	Function assay	1 to 10 uM	1 day	Inhibition of CK2 in human LNCAP cells assessed as DHT-mediated androgen receptor activation at 1 to 10 uM after 1 day by luciferase assay	22832316
LNCAP	Function assay	10 uM	8 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor dependent PSA mRNA level at 10 uM after 8 hrs by real time PCR analysis	22832316
LNCAP	Function assay	10 uM	8 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor dependent TMPRSS2 mRNA level at 10 uM after 8 hrs by real time PCR analysis	22832316
LNCAP	Function assay	1 to 10 uM	8 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of DHT-induced androgen receptor dependent TMPRSS2 mRNA expression at 1 to 10 uM after 8 hrs by real time PCR analysis	22832316
LNCAP	Function assay	3 uM	8 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor dependent DHT-induced PSA mRNA expression at 3 uM after 8 hrs by real time PCR analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor nuclear translocation at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Apoptosis assay	30 uM	72 hrs	Induction of apoptosis in human LNCAP cells at 30 uM after 72 hrs by AnnexinV staining based fluorescent microscopy	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Downregulation of CK2alpha expression in human LNCAP cells assessed as reduction of cytosolic protein level at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Downregulation of CK2alpha expression in human LNCAP cells assessed as reduction of nuclear protein level at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2alpha in human LNCAP cells assessed as reduction of p21 phosphorylation at threonine145 at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2alpha in human LNCAP cells assessed as reduction of Akt phosphorylation at Ser473 at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2alpha in human LNCAP cells assessed as reduction of XIAP expression at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2alpha in human LNCAP cells assessed as induction of CHOP expression at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor nuclear translocation at 10 uM after 12 to 24 hrs by HCS analysis	22832316
MV4-11	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human MV4-11 cells after 1 to 3 days by MTS assay, CC50=3μM	23711832
U937	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human U937 cells after 1 to 3 days by MTS assay, CC50=4.2μM	23711832
Jurkat	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human Jurkat cells after 1 to 3 days by MTS assay, CC50=4.5μM	23711832
K562	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human K562 cells after 1 to 3 days by MTS assay, CC50=7μM	23711832
A549	Function assay	10 uM		Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM by Western blot method	24012124
A549	Function assay	30 uM	48 hrs	Inhibition of CK2-mediated MMP2 activation in human A549 cells at 30 uM after 48 hrs by gelatin-zymography	24012124
A549	Function assay	10 uM	4 to 24 hrs	Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 4 to 24 hrs by Western blot method	24012124
A549	Function assay	10 uM	15 to 30 mins	Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM after 15 to 30 mins by Western blot method	24012124
A549	Function assay	10 uM	24 hrs	Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 24 hrs by Western blot method	24012124
A549	Function assay	1 to 10 uM	24 hrs	Inhibition of CK2-mediated MT1-MMP expression in human A549 cells at 1 to 10 uM after 24 hrs by Western blot method	24012124
Sf9	Function assay			Inhibition of CDK2/cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate in presence of [gamma33P]ATP, IC50=1.8μM	24681986
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTS assay, CC50=9.9μM	26850376
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
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS 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
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 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
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
Sf21 insect	Function assay		20 mins	Inhibition of recombinant human full length N-terminal His6-tagged CK2alpha expressed in Sf21 insect cells using CK2tide as substrate treated for 20 mins measured after 90 mins in presence of MgCl2 by caliper mobility shift assay, IC50<0.003μM	29559278
786-0	Function assay		24 hrs	Inhibition of CK2 in human 786-0 cells assessed as decrease in Akt1 phosphorylation at Ser129 after 24 hrs by Western blot analysis, IC50=1μM	30689946
786-0	Function assay		24 hrs	Inhibition of CK2 in human 786-0 cells assessed as decrease in alpha-catenin phosphorylation at Ser641 after 24 hrs by Western blot analysis, EC50=1μM	30689946
786-0	Function assay		24 hrs	Inhibition of CK2 in human 786-0 cells assessed as reduction in STAT3 phosphorylation at Y705 after 24 hrs by Western blot analysis, EC50=5.3μM	30689946
HeLa	Function assay	8 uM	12 hrs	Inhibition EGFP-CK2alpha (unknown origin) expressed in human HeLa cells induction of EGFP-CK2alpha translocation from nucleoli to nuclear matrix and cytoplasm at 8 uM after 12 hrs by Hoechst-33342-staining based microscopy	30689946
Vero E6	Function assay		48 hrs	IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells), IC50=3.89045μM	32353859
pulmonary smooth muscle cells	Function assay			Inhibition of de-differentiation of human pulmonary smooth muscle cells assessed as reduction in contractile to synthetic forms change, EC=0.001μM	ChEMBL
Jurkat T	Function assay			Modulation of Endogenous Assay: The human leukemia Jurkat T-cell line was maintained in RPMI 1640 (Cambrex) supplemented with 10% fetal calf serum and 50 ng/ml Geutamycin. Before treatment cells were washed, resuspended at a density of about 106 cells/mil, IC50=0.1μM	ChEMBL
pulmonary smooth muscle cells	Function assay	1 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as down-regulation of COL1 protein expression at 1 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	10 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as down-regulation of COL1 protein expression at 10 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	1 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as down-regulation of CCN2 protein expression at 1 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	10 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as down-regulation of CCN2 protein expression at 10 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	1 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as up-regulation of ACTA2 protein expression at 1 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	10 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as up-regulation of ACTA2 protein expression at 10 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	1 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as up-regulation of MYH11 protein expression at 1 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	10 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as up-regulation of MYH11 protein expression at 10 nM by Western blot analysis	ChEMBL
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Informations chimiques, stockage et stabilité

Poids moléculaire	371.75	Formule	C₁₉H₁₁ClN₃NaO₂	Stockage (À partir de la date de réception)	3 years -20°C powder
N° CAS	1309357-15-0	--		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	N/A			Smiles	C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)[O-])C4=C2C=CN=C4.[Na+]

Solubilité

In vitro
Lot:

DMSO : 24 mg/mL (64.55 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	1.200mg/ml (3.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 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 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	0.150mg/ml (0.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	10.000mg/ml (26.90mM)	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 clarify; 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.
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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC₅₀/Ki	CK2α (Cell-free assay) 1 nM CK2α' (Cell-free assay) 1 nM
Références	[1] https://pubmed.ncbi.nlm.nih.gov/21159648/

Informations sur lessai clinique

(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Sponsor/Collaborateurs	Date de début	Phases
NCT05817708	Completed	COVID-19	Senhwa Biosciences Inc.	November 7 2022	Phase 1
NCT04668209	Terminated	Coronavirus	University of Arizona\|Senhwa Biosciences Inc.	January 21 2021	Phase 2
NCT04663737	Completed	Covid19	Chris Recknor MD\|Senhwa Biosciences Inc.	December 3 2020	Phase 2
NCT03904862	Suspended	Medulloblastoma Childhood	Pediatric Brain Tumor Consortium\|National Cancer Institute (NCI)\|American Lebanese Syrian Associated Charities (ALSAC)	July 25 2019	Phase 1\|Phase 2
NCT02128282	Completed	Cholangiocarcinoma	Senhwa Biosciences Inc.	June 2014	Phase 1\|Phase 2

Support technique

Instructions de manipulation

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

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