Home Angiogenesis Src inhibitor WH-4-023

연구용

WH-4-023 Lck/Src Inhibitor

제품 번호: 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

화학 구조

분자량: 568.67

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품질 관리 (Quality Control)

배치: 순도: 99.93%
99.93

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 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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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 568.67 화학식

C32H36N6O4

 보관 (수령일로부터)
CAS 번호 837422-57-8 SDF 다운로드 원액 보관

동의어 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

용해도 (Solubility)

In vitro
배치:

DMSO : 12 mg/mL (21.1 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 6 mg/mL

Water : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

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

WH-4-023은 p38 및 KDR에 대해 거의 활성을 나타내지 않습니다.

키나아제 분석
Lck 키나아제 분석
Lck HTRF 키나아제 분석은 억제제 화합물의 존재 또는 부재 하에 가스트린의 비오틴화된 기질 펩타이드에 대한 ATP 의존적 인산화를 포함합니다. 가스트린의 최종 농도는 1.2 μM입니다. ATP의 최종 농도는 0.5 μM(Km app = 0.6 ± 0.1 μM)이고, Lck(GST-키나아제 도메인 융합체(AA 225−509))의 최종 농도는 250 pM입니다. 완충액 조건은 다음과 같습니다: 50 mM HEPES pH = 7.5, 50 mM NaCl, 20 mM MgCl2, 5 mM MnCl, 2 mM DTT, 0.05% BSA. 분석은 160 μL의 검출 시약으로 켄칭(quenched) 및 중단됩니다. 검출 시약은 다음과 같습니다: 50 mM Tris, pH = 7.5, 100 mM NaCl, 3 mM EDTA, 0.05% BSA, 0.1% Tween20으로 구성된 완충액. 판독하기 전에 Streptavidin allophycocyanin(SA-APC)을 분석 최종 농도 0.0004 mg/mL로 첨가하고, europilated anti-phosphotyrosine Ab(Eu-anti-PY)를 최종 농도 0.025 nM로 함께 첨가합니다. 분석 플레이트는 320 nm에서의 여기 및 615 nm와 655 nm에서의 방출을 갖는 Discovery 형광 플레이트 판독기에서 판독됩니다. 다른 키나아제에 대한 분석도 위에서 설명한 것과 유사한 방식으로 수행되며, 키나아제의 특정 활성과 기질에 대해 측정된 Km에 따라 반응에 첨가되는 효소, 펩타이드 기질 및 ATP의 농도를 변경합니다.
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