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WH-4-023 Lck/Src Inhibitor

Name: WH-4-023
Brand: Selleck Chemicals
SKU: S7565
Availability: InStock
Rating: 5 (32 reviews)

Cat.No.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.

Chemical Structure

Molecular Weight: 568.67

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Quality Control

Batch: Purity: 99.93%

99.93

Related Targets	EGFR VEGFR JAK PDGFR FGFR HIF FLT FLT3 HER2 Bcr-Abl
Other Src Inhibitors	Saracatinib (AZD0530) PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 RK 24466 Tolimidone (MLR-1023) 1-Naphthyl PP1(1-NA-PP1) UM-164 Myristic Acid

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 12 mg/mL (21.1 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
Clear solution	5%DMSO 1 30%PEG300 2 5%Tween80 3 60%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (1.76mM)	Taking the 1 mL working solution as an example, add 50 μL 20 mg/ml clarified DMSO stock solution to 300 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 600 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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Dosage: mg/kg

Average weight of animals: g

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight	568.67	Formula	C₃₂H₃₆N₆O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	837422-57-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	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

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.
Kinase Assay	Lck Kinase Assay
Kinase Assay	The Lck HTRF kinase assay involves ATP-dependent phosphorylation of a biotinylated substrate peptide of gastrin in the presence or absence of inhibitor compound. The final concentration of gastrin is 1.2 μM. The final concentration of ATP is 0.5 μM (Km app = 0.6 ± 0.1 μM), and the final concentration of Lck (a GST-kinase domain fusion (AA 225−509)) is 250 pM. Buffer conditions are as follows: 50 mM HEPES pH = 7.5, 50 mM NaCl, 20 mM MgCl₂, 5 mM MnCl, 2 mM DTT, 0.05% BSA. The assay is quenched and stopped with 160 μL of detection reagent. Detection reagents are as follows: Buffer made of 50 mM Tris, pH = 7.5, 100 mM NaCl, 3 mM EDTA, 0.05% BSA, 0.1% Tween20. Prior to reading, Streptavidin allophycocyanin (SA-APC) is added at a final concentration in the assay of 0.0004 mg/mL, along with europilated anti-phosphotyrosine Ab (Eu-anti-PY) at a final conc of 0.025 nM. The assay plate is read in a Discovery fluorescence plate reader with excitation at 320 nm and emission at 615 and 655 nm. Assays for other kinases are done in a similar way as described above, varying the concentrations of enzyme, peptide substrate, and ATP added to the reaction, depending on the specific activity of the kinase and measured Kms for the substrates.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16884310/ [2] https://pubmed.ncbi.nlm.nih.gov/34848870/ [3] https://pubmed.ncbi.nlm.nih.gov/28618271/

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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):