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Saracatinib (AZD0530) Src inhibiteur

Name: Saracatinib (AZD0530)
Brand: Selleck Chemicals
SKU: S1006
Rating: 5 (308 reviews)

Réf. CatalogueS1006

Le Saracatinib (AZD0530) est un puissant inhibiteur de Src avec une IC50 de 2,7 nM dans les essais sans cellules, et est puissant contre c-Yes, Fyn, Lyn, Blk, Fgr et Lck ; moins actif pour Abl et EGFR (L858R et L861Q). Il induit l'autophagy et est en phase 2/3.

Saracatinib (AZD0530) Src inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 542.03

Aller à

Contrôle Qualité

Lot : Pureté : 99.99%

99.99

Cibles apparentées	EGFR VEGFR JAK PDGFR FGFR HIF FLT FLT3 HER2 Bcr-Abl
Autre Src Inhibiteurs	WH-4-023 PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 Tolimidone (MLR-1023) UM-164 1-Naphthyl PP1(1-NA-PP1) RK 24466 Myristic Acid

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Description de lactivité	PMID
CTV-1	Growth Inhibition Assay			IC50=0.06143 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=0.1599 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=0.23688 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=0.265 μM	SANGER
TE-15	Growth Inhibition Assay			IC50=0.27412 μM	SANGER
NCI-H1648	Growth Inhibition Assay			IC50=0.28116 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=0.3268 μM	SANGER
LB996-RCC	Growth Inhibition Assay			IC50=0.44196 μM	SANGER
K-562	Growth Inhibition Assay			IC50=0.44967 μM	SANGER
D-336MG	Growth Inhibition Assay			IC50=0.50304 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=0.60529 μM	SANGER
EW-24	Growth Inhibition Assay			IC50=0.62693 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=0.65249 μM	SANGER
NCCIT	Growth Inhibition Assay			IC50=0.73218 μM	SANGER
NCI-H1436	Growth Inhibition Assay			IC50=0.79049 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=0.86203 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=0.87275 μM	SANGER
A704	Growth Inhibition Assay			IC50=0.8921 μM	SANGER
TK10	Growth Inhibition Assay			IC50=0.90669 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=1.19779 μM	SANGER
C2BBe1	Growth Inhibition Assay			IC50=1.20507 μM	SANGER
RXF393	Growth Inhibition Assay			IC50=1.2436 μM	SANGER
KGN	Growth Inhibition Assay			IC50=1.27687 μM	SANGER
NB69	Growth Inhibition Assay			IC50=1.37497 μM	SANGER
TE-11	Growth Inhibition Assay			IC50=1.43418 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=1.44105 μM	SANGER
ST486	Growth Inhibition Assay			IC50=1.45852 μM	SANGER
HOP-62	Growth Inhibition Assay			IC50=1.50246 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=1.55083 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=1.55453 μM	SANGER
TE-10	Growth Inhibition Assay			IC50=1.66252 μM	SANGER
RL95-2	Growth Inhibition Assay			IC50=1.66902 μM	SANGER
DOHH-2	Growth Inhibition Assay			IC50=1.71782 μM	SANGER
MFH-ino	Growth Inhibition Assay			IC50=1.7787 μM	SANGER
GB-1	Growth Inhibition Assay			IC50=1.79833 μM	SANGER
SK-N-DZ	Growth Inhibition Assay			IC50=1.84688 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=1.88574 μM	SANGER
SW982	Growth Inhibition Assay			IC50=1.92093 μM	SANGER
KALS-1	Growth Inhibition Assay			IC50=1.98722 μM	SANGER
TGBC24TKB	Growth Inhibition Assay			IC50=2.05958 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=2.16084 μM	SANGER
SW962	Growth Inhibition Assay			IC50=2.17178 μM	SANGER
SW872	Growth Inhibition Assay			IC50=2.18507 μM	SANGER
NCI-H747	Growth Inhibition Assay			IC50=2.25714 μM	SANGER
MZ1-PC	Growth Inhibition Assay			IC50=2.29356 μM	SANGER
MSTO-211H	Growth Inhibition Assay			IC50=2.35723 μM	SANGER
BL-70	Growth Inhibition Assay			IC50=2.47422 μM	SANGER
SW954	Growth Inhibition Assay			IC50=2.57408 μM	SANGER
SNB75	Growth Inhibition Assay			IC50=2.68594 μM	SANGER
IST-SL2	Growth Inhibition Assay			IC50=2.72379 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=2.87005 μM	SANGER
KU812	Growth Inhibition Assay			IC50=3.05299 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=3.12109 μM	SANGER
ETK-1	Growth Inhibition Assay			IC50=3.20767 μM	SANGER
SF126	Growth Inhibition Assay			IC50=3.31174 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=3.557 μM	SANGER
KNS-42	Growth Inhibition Assay			IC50=3.65 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=3.73433 μM	SANGER
PF-382	Growth Inhibition Assay			IC50=3.83698 μM	SANGER
SH-4	Growth Inhibition Assay			IC50=4.25259 μM	SANGER
KM12	Growth Inhibition Assay			IC50=4.32416 μM	SANGER
NB5	Growth Inhibition Assay			IC50=4.41864 μM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=4.65256 μM	SANGER
Becker	Growth Inhibition Assay			IC50=4.66416 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=4.81344 μM	SANGER
KINGS-1	Growth Inhibition Assay			IC50=4.82373 μM	SANGER
LS-123	Growth Inhibition Assay			IC50=5.49684 μM	SANGER
SF268	Growth Inhibition Assay			IC50=5.61262 μM	SANGER
A388	Growth Inhibition Assay			IC50=5.63667 μM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=6.01811 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=6.02075 μM	SANGER
ES4	Growth Inhibition Assay			IC50=6.53074 μM	SANGER
SR	Growth Inhibition Assay			IC50=6.58807 μM	SANGER
BB49-HNC	Growth Inhibition Assay			IC50=6.73206 μM	SANGER
KLE	Growth Inhibition Assay			IC50=6.78377 μM	SANGER
HUTU-80	Growth Inhibition Assay			IC50=6.98466 μM	SANGER
SNU-C2B	Growth Inhibition Assay			IC50=7.82737 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=7.94904 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=8.42808 μM	SANGER
GDM-1	Growth Inhibition Assay			IC50=8.97292 μM	SANGER
LC4-1	Growth Inhibition Assay			IC50=9.00911 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=9.15006 μM	SANGER
EoL-1-cell	Growth Inhibition Assay			IC50=9.30192 μM	SANGER
BOKU	Growth Inhibition Assay			IC50=9.96466 μM	SANGER
EVSA-T	Growth Inhibition Assay			IC50=10.6568 μM	SANGER
D-283MED	Growth Inhibition Assay			IC50=10.9176 μM	SANGER
NB1	Growth Inhibition Assay			IC50=11.0242 μM	SANGER
RPMI-8402	Growth Inhibition Assay			IC50=11.178 μM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=11.1806 μM	SANGER
NB7	Growth Inhibition Assay			IC50=11.3297 μM	SANGER
RPMI-6666	Growth Inhibition Assay			IC50=12.9567 μM	SANGER
697	Growth Inhibition Assay			IC50=13.2701 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=13.5948 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay			IC50=13.9234 μM	SANGER
BE-13	Growth Inhibition Assay			IC50=14.3915 μM	SANGER
SKM-1	Growth Inhibition Assay			IC50=14.4499 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=14.7591 μM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=14.7898 μM	SANGER
ECC4	Growth Inhibition Assay			IC50=17.0277 μM	SANGER
ES3	Growth Inhibition Assay			IC50=17.4655 μM	SANGER
LB647-SCLC	Growth Inhibition Assay			IC50=17.4949 μM	SANGER
NB10	Growth Inhibition Assay			IC50=18.5256 μM	SANGER
L-540	Growth Inhibition Assay			IC50=18.8109 μM	SANGER
NCI-H2126	Growth Inhibition Assay			IC50=19.51 μM	SANGER
HH	Growth Inhibition Assay			IC50=20.0099 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=23.2289 μM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=23.8658 μM	SANGER
KP-N-YS	Growth Inhibition Assay			IC50=23.9255 μM	SANGER
EC-GI-10	Growth Inhibition Assay			IC50=24.5989 μM	SANGER
EKVX	Growth Inhibition Assay			IC50=26.0203 μM	SANGER
TGBC1TKB	Growth Inhibition Assay			IC50=26.434 μM	SANGER
Daudi	Growth Inhibition Assay			IC50=27.0773 μM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=27.081 μM	SANGER
NB6	Growth Inhibition Assay			IC50=27.488 μM	SANGER
ES6	Growth Inhibition Assay			IC50=27.9123 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay			IC50=28.0373 μM	SANGER
K5	Growth Inhibition Assay			IC50=28.1287 μM	SANGER
ES1	Growth Inhibition Assay			IC50=28.7773 μM	SANGER
LC-1F	Growth Inhibition Assay			IC50=29.7346 μM	SANGER
SCLC-21H	Growth Inhibition Assay			IC50=30.7317 μM	SANGER
SK-PN-DW	Growth Inhibition Assay			IC50=32.5598 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=32.9773 μM	SANGER
TE-5	Growth Inhibition Assay			IC50=33.0362 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay			IC50=33.5048 μM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=33.7666 μM	SANGER
LOXIMVI	Growth Inhibition Assay			IC50=33.7928 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=35.144 μM	SANGER
A253	Growth Inhibition Assay			IC50=35.7429 μM	SANGER
HCC1599	Growth Inhibition Assay			IC50=36.7053 μM	SANGER
EB-3	Growth Inhibition Assay			IC50=36.9518 μM	SANGER
GOTO	Growth Inhibition Assay			IC50=37.3224 μM	SANGER
SW684	Growth Inhibition Assay			IC50=41.8495 μM	SANGER
DEL	Growth Inhibition Assay			IC50=42.0522 μM	SANGER
HT-144	Growth Inhibition Assay			IC50=42.1676 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=43.4596 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=44.3925 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=44.5034 μM	SANGER
RCC10RGB	Growth Inhibition Assay			IC50=44.7392 μM	SANGER
CP67-MEL	Growth Inhibition Assay			IC50=45.6241 μM	SANGER
NB17	Growth Inhibition Assay			IC50=45.6643 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=45.9464 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay			IC50=46.0119 μM	SANGER
HCE-4	Growth Inhibition Assay			IC50=46.5968 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=46.7682 μM	SANGER
KARPAS-422	Growth Inhibition Assay			IC50=47.0895 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=47.1622 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=47.6828 μM	SANGER
PSN1	Growth Inhibition Assay			IC50=47.7813 μM	SANGER
NIH3T3	Function assay			Inhibition of human c-Src in NIH3T3 cells, IC50 = 0.0027 μM.	17064066
HEK293	Function assay		1 hr	Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0398 μM.	29941193
HEK293	Function assay		1 hr	Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.418 μM.	29941193
Rh30	Antiproliferative assay		48 hrs	Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay, IC50 = 10.1 μM.	23787099
Huh7	Antiviral assay	2.5 uM	5 days	Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control	17360676
Huh7	Antiviral assay	2.5 uM	6 days	Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control	17360676
Vero	Antiviral assay	2.5 uM	4 days	Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control	17360676
Vero	Antiviral assay	2.5 uM	6 days	Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control	17360676
C6/36	Antiviral assay	2.5 uM	4 days	Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control	17360676
C6/36	Antiviral assay	2.5 uM	5 days	Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control	17360676
Vero	Antiviral assay		3 days	Antiviral activity against Dengue virus infected in african green monkey Vero cells administered after viral challenge after 3 days by viral plaque assay	17360676
Vero	Antiviral assay	2.5 uM	5 days	Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control	17360676
Huh7	Antiviral assay	2.5 uM	4 days	Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control	17360676
C6/36	Antiviral assay	2.5 uM	6 days	Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control	17360676
HEK293	Function assay	0.1 to 1 uM	16 hrs	Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting	26191369
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 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
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
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
HEK293	Function assay	0.1 to 1 uM	16 hrs	Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting	26191369
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Informations chimiques, stockage et stabilité

Poids moléculaire	542.03	Formule	C₂₇H₃₂ClN₅O₅	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	379231-04-6	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	N/A			Smiles	CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl

Solubilité

In vitro
Lot:

DMSO : 100 mg/mL (184.49 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 100 mg/mL

Water : 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 commerciale pour des tests personnalisés.	5.000mg/ml (9.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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 commerciale pour des tests personnalisés.	1.650mg/ml (3.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 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.
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 : Saisir 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 : Saisir la formulation in vivo (Ceci est seulement 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, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

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

Note : 1. Veuillez vous assurer 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 chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Caractéristiques	The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.
Targets/IC₅₀/Ki	c-Src (Cell-free assay) 2.7 nM LCK (Cell-free assay) <4 nM c-YES (Cell-free assay) 4 nM EGFR (L861Q) (Cell-free assay) 4 nM Lyn (Cell-free assay) 5 nM EGFR (L858R) (Cell-free assay) 5 nM Fyn (Cell-free assay) 10 nM FGR (Cell-free assay) 10 nM BLK (Cell-free assay) 11 nM v-Abl (Cell-free assay) 30 nM EGFR (Cell-free assay) 66 nM c-Kit (Cell-free assay) 200 nM EphA2 (Cell-free assay) 236 nM
In vitro	Le Saracatinib (AZD0530) inhibe également puissamment d'autres membres de la famille des tyrosine kinases Src, y compris c-Yes, Fyn, Lyn, Blk, Fgr et Lck avec des IC50 de 4 à 10 nM. Il inhibe de manière sensible Src Y530F NIH 3T3 avec une IC50 de 80 nM. Ce composé altère significativement l'invasion des cellules HT1080 à travers une matrice de collagène tridimensionnelle et inhibe complètement la dispersion cellulaire induite par l'EGF dans les cellules de cancer de la vessie NBT-II. Il inhibe puissamment l'activation de Src dans les cellules DU145 et PC3, par inhibition de la phosphorylation de Y419. Il inhibe la croissance des cancers de la prostate, y compris PC3, DU145, CWR22Rv1 et LNCaP, tout en montrant une faible activité dans les cellules LAPC-4, PZ-HPV7 et RWPE-1. Il induit un arrêt du cycle cellulaire en G1/S mais pas les clivages de la caspase 3. Il inhibe également significativement la migration des DU145 et PC3 dans la chambre de Boyden. Il provoque un blocage puissant et soutenu d'AKT et améliore la sensibilité à l'irradiation dans les cellules A549 et Calu-6. Il inhibe l'ostéoclaste en activité, résorption et formation. Il empêche également de manière réversible la migration des précurseurs d'ostéoclastes.
Essai kinase	Essai Kinase
Essai kinase	L'IC50 de l'activité tyrosine kinase est mesurée par un dosage immunoenzymatique (ELISA) avec des domaines catalytiques recombinants d'un panel de récepteurs et de tyrosine kinases non-récepteurs (dans certains cas, seule une partie du domaine catalytique est utilisée). Ce composé est dosé dans une gamme de 0,001 à 10 mM. Des dosages de spécificité contre un panel de sérine/thréonine kinases sont réalisés à l'aide d'un essai de capture sur filtre avec du ³²P. En bref, des plaques 384 puits multidrop contenant 0,5 μL de Saracatinib (AZD0530) ou des contrôles (DMSO seul ou contrôles tampon pH 3,0) sont incubées avec 15 μL d'enzyme plus substrat peptidique/protéique pendant 5 min avant que la réaction ne soit initiée par l'ajout de 10 μL de 20 mM Mg-ATP. Pour toutes les enzymes, la concentration finale est approximée à la constante de Michaelis (K_m). Les essais sont réalisés pendant 30 min à température ambiante avant l'arrêt par l'ajout de 5 μL d'acide orthophosphorique. Après mélange, le contenu des puits est recueilli sur une plaque P81 Uniﬁlter, en utilisant de l'acide orthophosphorique comme tampon de lavage. L'IC50 est ensuite calculée.
In vivo	Le Saracatinib (AZD0530) montre une grande inhibition de la croissance tumorale dans les allogreffes Src3T3 et un délai de croissance modéré dans les xénogreffes Calu-6, MDA-MB-231, AsPc-1 et BT474C. Ce composé montre également une grande activité antitumorale chez les souris xénogreffées orthotopiques DU145 à une dose de 25 mg/kg (administrée oralement, quotidiennement).
Références	[1] https://pubmed.ncbi.nlm.nih.gov/18679417/ [2] https://pubmed.ncbi.nlm.nih.gov/19393585/ [3] https://pubmed.ncbi.nlm.nih.gov/19240653/ [4] https://pubmed.ncbi.nlm.nih.gov/19372577/ [5] https://pubmed.ncbi.nlm.nih.gov/19216789/ [6] https://pubmed.ncbi.nlm.nih.gov/18493848/ [7] https://pubmed.ncbi.nlm.nih.gov/19451593/

Applications

Méthodes	Biomarqueurs	Images	PMID
Western blot	pY576-FAK / pY861-FAK / FAK pY418 Src / Src / pY410 CAS / CAS / Py421 Cortactin / Cortactin p-Akt / p-mTOR / Akt / mTOR / p-S6 / S6 / p-AMPKα / AMPKα		20551056
Growth inhibition assay	Cell number		24349321

Informations sur lessai clinique

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

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT04598919	Active not recruiting	Idiopathic Pulmonary Fibrosis (IPF)	National Jewish Health\|Yale University\|Icahn School of Medicine at Mount Sinai\|AstraZeneca\|National Center for Advancing Translational Sciences (NCATS)\|Baylor University\|International Center for Health Outcomes and Innovation Research	November 12 2020	Phase 1\|Phase 2
NCT04307953	Recruiting	Fibrodysplasia Ossificans Progressiva	Amsterdam UMC location VUmc\|Royal National Orthopaedic Hospital NHS Trust\|Klinikum Garmisch-Patenkirchen\|University of Oxford\|Brigham and Women''s Hospital\|AstraZeneca\|Innovative Medicines Initiative	August 5 2020	Phase 2
NCT02085603	Completed	Cancer	Sheffield Teaching Hospitals NHS Foundation Trust\|AstraZeneca	March 2014	Phase 2
NCT01864655	Completed	Alzheimer''s Disease	Stephen M. Strittmatter\|National Institute of Neurological Disorders and Stroke (NINDS)\|Yale University	July 2013	Phase 1
NCT01000896	Withdrawn	Cancer\|Non Small Cell Lung Cancer\|Epithelial Ovarian Cancer	AstraZeneca	January 2010	Phase 1

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Foire aux questions

Question 1:
What is its half-life?

Réponse :
Based on the following paper, its half-life in vivo is around 40 hours and it reaches its peak level around 2–4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long

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