solo per uso di ricerca

WH-4-023 Lck/Src Inhibitor

N. Cat.: S7565

WH-4-023 (KIN001-112, KIN112, Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.
WH-4-023 Src inhibitor Chemical Structure

Struttura chimica

Peso molecolare: 568.67

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.93%
99.93

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dell'attività PMID
EM-2 Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=0μM SANGER
LAMA-84 Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=0.0000038μM SANGER
EoL-1-cell Growth inhibition assay Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=0.0000095μM SANGER
MEG-01 Growth inhibition assay Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=0.0000163μM SANGER
CTV-1 Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=0.0000318μM SANGER
BL-70 Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay, IC50=0.0000472μM SANGER
K-562 Growth inhibition assay Inhibition of human K-562 cell growth in a cell viability assay, IC50=0.0001617μM SANGER
BV-173 Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=0.0005143μM SANGER
DOHH-2 Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=0.0005969μM SANGER
A704 Growth inhibition assay Inhibition of human A704 cell growth in a cell viability assay, IC50=0.001268μM SANGER
NCI-SNU-16 Growth inhibition assay Inhibition of human NCI-SNU-16 cell growth in a cell viability assay, IC50=0.01572μM SANGER
LC-2-ad Growth inhibition assay Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=0.02033μM SANGER
LB2518-MEL Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=0.04667μM SANGER
D-336MG Growth inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay, IC50=0.04681μM SANGER
LB996-RCC Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=0.05668μM SANGER
Becker Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay, IC50=0.06381μM SANGER
LB1047-RCC Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=0.07592μM SANGER
KS-1 Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay, IC50=0.07758μM SANGER
MPP-89 Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=0.08229μM SANGER
RXF393 Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.10633μM SANGER
LB831-BLC Growth inhibition assay Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=0.12715μM SANGER
HUTU-80 Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=0.17529μM SANGER
A498 Growth inhibition assay Inhibition of human A498 cell growth in a cell viability assay, IC50=0.18945μM SANGER
MZ1-PC Growth inhibition assay Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=0.22716μM SANGER
TE-8 Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=0.23924μM SANGER
MFH-ino Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=0.23925μM SANGER
TE-15 Growth inhibition assay Inhibition of human TE-15 cell growth in a cell viability assay, IC50=0.24276μM SANGER
NTERA-S-cl-D1 Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=0.28855μM SANGER
COLO-829 Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=0.31212μM SANGER
SW684 Growth inhibition assay Inhibition of human SW684 cell growth in a cell viability assay, IC50=0.32588μM SANGER
OS-RC-2 Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=0.35011μM SANGER
IST-MES1 Growth inhibition assay Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50=0.35723μM SANGER
SNB75 Growth inhibition assay Inhibition of human SNB75 cell growth in a cell viability assay, IC50=0.35774μM SANGER
SW954 Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay, IC50=0.37163μM SANGER
RCC10RGB Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=0.42631μM SANGER
VA-ES-BJ Growth inhibition assay Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=0.46261μM SANGER
NCI-H1648 Growth inhibition assay Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.51582μM SANGER
PF-382 Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay, IC50=0.70763μM SANGER
Daudi Growth inhibition assay Inhibition of human Daudi cell growth in a cell viability assay, IC50=0.71411μM SANGER
SW982 Growth inhibition assay Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.85819μM SANGER
SW872 Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay, IC50=0.86458μM SANGER
TE-12 Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50=0.88831μM SANGER
HOP-62 Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.91599μM SANGER
NOS-1 Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=0.95045μM SANGER
BL-41 Growth inhibition assay Inhibition of human BL-41 cell growth in a cell viability assay, IC50=1.00013μM SANGER
TGBC24TKB Growth inhibition assay Inhibition of human TGBC24TKB cell growth in a cell viability assay, IC50=1.03831μM SANGER
KGN Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay, IC50=1.0521μM SANGER
TK10 Growth inhibition assay Inhibition of human TK10 cell growth in a cell viability assay, IC50=1.08418μM SANGER
GB-1 Growth inhibition assay Inhibition of human GB-1 cell growth in a cell viability assay, IC50=1.16064μM SANGER
GCIY Growth inhibition assay Inhibition of human GCIY cell growth in a cell viability assay, IC50=1.2301μM SANGER
LXF-289 Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.27256μM SANGER
RL95-2 Growth inhibition assay Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=1.32436μM SANGER
SW962 Growth inhibition assay Inhibition of human SW962 cell growth in a cell viability assay, IC50=1.33742μM SANGER
HT-144 Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50=1.44517μM SANGER
IST-SL2 Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=1.47421μM SANGER
NB6 Growth inhibition assay Inhibition of human NB6 cell growth in a cell viability assay, IC50=1.69698μM SANGER
SF126 Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50=1.73178μM SANGER
BOKU Growth inhibition assay Inhibition of human BOKU cell growth in a cell viability assay, IC50=1.80527μM SANGER
BB30-HNC Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=1.85472μM SANGER
KLE Growth inhibition assay Inhibition of human KLE cell growth in a cell viability assay, IC50=1.86232μM SANGER
MLMA Growth inhibition assay Inhibition of human MLMA cell growth in a cell viability assay, IC50=1.9231μM SANGER
KINGS-1 Growth inhibition assay Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50=1.96897μM SANGER
ES6 Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50=2.05401μM SANGER
SH-4 Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay, IC50=2.12055μM SANGER
EB-3 Growth inhibition assay Inhibition of human EB-3 cell growth in a cell viability assay, IC50=2.15824μM SANGER
KURAMOCHI Growth inhibition assay Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=2.24236μM SANGER
D-263MG Growth inhibition assay Inhibition of human D-263MG cell growth in a cell viability assay, IC50=2.28853μM SANGER
SF268 Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50=2.48682μM SANGER
NB17 Growth inhibition assay Inhibition of human NB17 cell growth in a cell viability assay, IC50=2.62875μM SANGER
DMS-114 Growth inhibition assay Inhibition of human DMS-114 cell growth in a cell viability assay, IC50=2.79022μM SANGER
MC116 Growth inhibition assay Inhibition of human MC116 cell growth in a cell viability assay, IC50=2.85704μM SANGER
MZ2-MEL Growth inhibition assay Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=3.08643μM SANGER
GI-ME-N Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=3.25166μM SANGER
697 Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=3.39644μM SANGER
ACN Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay, IC50=4.22607μM SANGER
TE-10 Growth inhibition assay Inhibition of human TE-10 cell growth in a cell viability assay, IC50=4.2795μM SANGER
LS-123 Growth inhibition assay Inhibition of human LS-123 cell growth in a cell viability assay, IC50=4.35584μM SANGER
TE-9 Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay, IC50=4.39183μM SANGER
CAS-1 Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=4.4023μM SANGER
BB65-RCC Growth inhibition assay Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=4.69952μM SANGER
MRK-nu-1 Growth inhibition assay Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=4.71792μM SANGER
NCI-H1355 Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=4.87685μM SANGER
KP-N-YS Growth inhibition assay Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50=4.92086μM SANGER
MZ7-mel Growth inhibition assay Inhibition of human MZ7-mel cell growth in a cell viability assay, IC50=5.09269μM SANGER
NCI-H747 Growth inhibition assay Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=5.74159μM SANGER
C2BBe1 Growth inhibition assay Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50=5.78469μM SANGER
RPMI-6666 Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=5.9621μM SANGER
PSN1 Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=6.16376μM SANGER
TE-1 Growth inhibition assay Inhibition of human TE-1 cell growth in a cell viability assay, IC50=6.71768μM SANGER
ETK-1 Growth inhibition assay Inhibition of human ETK-1 cell growth in a cell viability assay, IC50=7.6356μM SANGER
ST486 Growth inhibition assay Inhibition of human ST486 cell growth in a cell viability assay, IC50=8.27227μM SANGER
KU812 Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=8.38738μM SANGER
EHEB Growth inhibition assay Inhibition of human EHEB cell growth in a cell viability assay, IC50=9.0509μM SANGER
IMR-5 Growth inhibition assay Inhibition of human IMR-5 cell growth in a cell viability assay, IC50=9.28459μM SANGER
BB49-HNC Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=9.96548μM SANGER
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=10.3373μM SANGER
CP66-MEL Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=10.6469μM SANGER
NMC-G1 Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=11.0324μM SANGER
SIMA Growth inhibition assay Inhibition of human SIMA cell growth in a cell viability assay, IC50=11.2916μM SANGER
A101D Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=11.8487μM SANGER
IST-MEL1 Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=12.5986μM SANGER
no-10 Growth inhibition assay Inhibition of human no-10 cell growth in a cell viability assay, IC50=13.1434μM SANGER
KALS-1 Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=13.16μM SANGER
GI-1 Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay, IC50=13.2491μM SANGER
ONS-76 Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=13.3728μM SANGER
D-247MG Growth inhibition assay Inhibition of human D-247MG cell growth in a cell viability assay, IC50=13.7709μM SANGER
NCI-H446 Growth inhibition assay Inhibition of human NCI-H446 cell growth in a cell viability assay, IC50=14.1409μM SANGER
NALM-6 Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=14.2358μM SANGER
SK-N-DZ Growth inhibition assay Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=14.442μM SANGER
QIMR-WIL Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=14.5247μM SANGER
MHH-NB-11 Growth inhibition assay Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50=14.6569μM SANGER
A388 Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=14.6758μM SANGER
EVSA-T Growth inhibition assay Inhibition of human EVSA-T cell growth in a cell viability assay, IC50=15.2484μM SANGER
JVM-2 Growth inhibition assay Inhibition of human JVM-2 cell growth in a cell viability assay, IC50=16.4704μM SANGER
EW-16 Growth inhibition assay Inhibition of human EW-16 cell growth in a cell viability assay, IC50=17.7718μM SANGER
CP67-MEL Growth inhibition assay Inhibition of human CP67-MEL cell growth in a cell viability assay, IC50=18.5863μM SANGER
NB13 Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay, IC50=19.0437μM SANGER
NCCIT Growth inhibition assay Inhibition of human NCCIT cell growth in a cell viability assay, IC50=20.0093μM SANGER
SNU-C2B Growth inhibition assay Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=20.5124μM SANGER
SK-NEP-1 Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=22.2335μM SANGER
TE-6 Growth inhibition assay Inhibition of human TE-6 cell growth in a cell viability assay, IC50=22.3864μM SANGER
HCE-4 Growth inhibition assay Inhibition of human HCE-4 cell growth in a cell viability assay, IC50=22.927μM SANGER
TGBC1TKB Growth inhibition assay Inhibition of human TGBC1TKB cell growth in a cell viability assay, IC50=23.3177μM SANGER
L-540 Growth inhibition assay Inhibition of human L-540 cell growth in a cell viability assay, IC50=23.3231μM SANGER
8-MG-BA Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=23.9588μM SANGER
OPM-2 Growth inhibition assay Inhibition of human OPM-2 cell growth in a cell viability assay, IC50=25.106μM SANGER
MHH-PREB-1 Growth inhibition assay Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=26.2134μM SANGER
ALL-PO Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=26.6132μM SANGER
LB771-HNC Growth inhibition assay Inhibition of human LB771-HNC cell growth in a cell viability assay, IC50=27.8393μM SANGER
NEC8 Growth inhibition assay Inhibition of human NEC8 cell growth in a cell viability assay, IC50=29.0389μM SANGER
MSTO-211H Growth inhibition assay Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50=29.059μM SANGER
ATN-1 Growth inhibition assay Inhibition of human ATN-1 cell growth in a cell viability assay, IC50=29.7028μM SANGER
LB373-MEL-D Growth inhibition assay Inhibition of human LB373-MEL-D cell growth in a cell viability assay, IC50=29.7129μM SANGER
NB69 Growth inhibition assay Inhibition of human NB69 cell growth in a cell viability assay, IC50=30.374μM SANGER
LOXIMVI Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=30.8334μM SANGER
HC-1 Growth inhibition assay Inhibition of human HC-1 cell growth in a cell viability assay, IC50=32.8423μM SANGER
SK-UT-1 Growth inhibition assay Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=32.9447μM SANGER
KARPAS-422 Growth inhibition assay Inhibition of human KARPAS-422 cell growth in a cell viability assay, IC50=33.2528μM SANGER
KP-N-RT-BM-1 Growth inhibition assay Inhibition of human KP-N-RT-BM-1 cell growth in a cell viability assay, IC50=33.8198μM SANGER
SIG-M5 Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=34.6805μM SANGER
TE-11 Growth inhibition assay Inhibition of human TE-11 cell growth in a cell viability assay, IC50=38.0936μM SANGER
RKO Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=38.4067μM SANGER
LS-411N Growth inhibition assay Inhibition of human LS-411N cell growth in a cell viability assay, IC50=38.8809μM SANGER
OCUB-M Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=40.2533μM SANGER
OVCAR-4 Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=40.5786μM SANGER
JiyoyeP-2003 Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50=41.2672μM SANGER
no-11 Growth inhibition assay Inhibition of human no-11 cell growth in a cell viability assay, IC50=41.8283μM SANGER
NCI-H1694 Growth inhibition assay Inhibition of human NCI-H1694 cell growth in a cell viability assay, IC50=43.3351μM SANGER
IST-SL1 Growth inhibition assay Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=46.6838μM SANGER
T cells Function assay Inhibition of anti-CD3/CD28-induced IL2 secretion in human T cells, IC50=1.9μM 16884310
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
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
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 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
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 568.67 Formula

C32H36N6O4

Conservazione (Dalla data di ricezione)
N. CAS 837422-57-8 Scarica SDF Conservazione delle soluzioni stock

Sinonimi KIN001-112, KIN112, Dual LCK/SRC inhibitor Smiles CC1=C(C(=CC=C1)C)OC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC(=NC=C3)NC4=CC=C(C=C4)N5CCN(CC5)C

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 12 mg/mL (21.1 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 6 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa Concentrazione Volume Peso molecolare
Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo
Lotto:

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC50/Ki
Lck
(Cell-free assay)
2 nM
Src
(Cell-free assay)
6 nM
In vitro

WH-4-023 shows little activity on p38 and KDR.

Saggio chinasico
Saggio chinasi Lck
Il saggio chinasi Lck HTRF prevede la fosforilazione ATP-dipendente di un peptide substrato biotinilato di gastrina in presenza o assenza di un composto inibitore. La concentrazione finale di gastrina è 1,2 μM. La concentrazione finale di ATP è 0,5 μM (Km app = 0,6 ± 0,1 μM), e la concentrazione finale di Lck (una fusione del dominio GST-chinasi (AA 225−509)) è 250 pM. Le condizioni del tampone sono le seguenti: 50 mM HEPES pH = 7,5, 50 mM NaCl, 20 mM MgCl2, 5 mM MnCl, 2 mM DTT, 0,05% BSA. Il saggio viene spento e bloccato con 160 μL di reagente di rilevamento. I reagenti di rilevamento sono i seguenti: Tampone composto da 50 mM Tris, pH = 7,5, 100 mM NaCl, 3 mM EDTA, 0,05% BSA, 0,1% Tween20. Prima della lettura, la streptavidina alloficocianina (SA-APC) viene aggiunta ad una concentrazione finale nel saggio di 0,0004 mg/mL, insieme all'anticorpo anti-fosfotirosina europilato (Eu-anti-PY) ad una concentrazione finale di 0,025 nM. La piastra del saggio viene letta in un lettore di piastre a fluorescenza Discovery con eccitazione a 320 nm ed emissione a 615 e 655 nm. I saggi per altre chinasi vengono eseguiti in modo simile a quanto descritto sopra, variando le concentrazioni di enzima, substrato peptidico e ATP aggiunti alla reazione, a seconda dell'attività specifica della chinasi e dei Km misurati per i substrati.
Riferimenti