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Lapatinib

(CAS No:231277-92-2)
Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
CAS No:231277-92-2
Molecular Weight(MW):581.06
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 231277-92-2
Molecular formula(MF) C29H26ClFN4O4S
Molecular Weight(MW): 581.06
Alias lapatinib; n-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine; 4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-; Lapatinib(TINIBS); N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine
Solubility
In vitro DMSO 100 mg/mL (172.09 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL
Biological Activity
Description Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
Targets
ErbB2 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
ErbB4 [1]
(Cell-free assay)
c-Src [1]
(Cell-free assay)
C-Raf-1 [1]
(Cell-free assay)
9.2 nM 10.8 nM 367 nM 3.5 μM >10 μM
In vitro

Lapatinib weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib displays higher inhibitory activity against EGFR- or ErbB2-overexpressing cells with IC50 of 0.09-0.21 μM, compared with cells expressing low levels of EGFR or ErbB2 with IC50 of 3-12 μM, and exhibits ~100-fold selectivity over the normal fibroblast cells. Lapatinib potently inhibits the outgrowth of EGFR-overexpressing HN5 and A-431 cells, as well as ErbB2-overexpressing BT474 and N87 cells, and significantly induces G1 arrest of HN5 cells and apoptosis of BT474 cells, which are associated with inhibition of AKT phosphorylation. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1648 Growth Inhibition Assay IC50=0.02544 μM SANGER
HCC2218 Growth Inhibition Assay IC50=0.05326 μM SANGER
OCUB-M Growth Inhibition Assay IC50=0.0574 μM SANGER
ECC12 Growth Inhibition Assay IC50=0.09231 μM SANGER
DSH1 Growth Inhibition Assay IC50=0.09396 μM SANGER
BT-474 Growth Inhibition Assay IC50=0.21315 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.24654 μM SANGER
EKVX Growth Inhibition Assay IC50=0.44874 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.49057 μM SANGER
A388 Growth Inhibition Assay IC50=0.72258 μM SANGER
TE-9 Growth Inhibition Assay IC50=0.74453 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=1.15403 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=1.36228 μM SANGER
LC-1F Growth Inhibition Assay IC50=1.38244 μM SANGER
TE-6 Growth Inhibition Assay IC50=1.55201 μM SANGER
A253 Growth Inhibition Assay IC50=1.97335 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=1.99199 μM SANGER
TE-1 Growth Inhibition Assay IC50=2.0483 μM SANGER
RL95-2 Growth Inhibition Assay IC50=3.1567 μM SANGER
LS-513 Growth Inhibition Assay IC50=3.40041 μM SANGER
DJM-1 Growth Inhibition Assay IC50=3.46975 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=3.54501 μM SANGER
TE-10 Growth Inhibition Assay IC50=3.55356 μM SANGER
TE-5 Growth Inhibition Assay IC50=4.0373 μM SANGER
TK10 Growth Inhibition Assay IC50=4.16522 μM SANGER
UACC-812 Growth Inhibition Assay IC50=4.56153 μM SANGER
SW962 Growth Inhibition Assay IC50=5.02159 μM SANGER
SW954 Growth Inhibition Assay IC50=5.39245 μM SANGER
COLO-668 Growth Inhibition Assay IC50=5.72667 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=5.80046 μM SANGER
NB5 Growth Inhibition Assay IC50=6.21001 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=6.26561 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=6.43694 μM SANGER
GI-1 Growth Inhibition Assay IC50=6.51682 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=7.07183 μM SANGER
GT3TKB Growth Inhibition Assay IC50=7.22744 μM SANGER
EVSA-T Growth Inhibition Assay IC50=7.42811 μM SANGER
D-502MG Growth Inhibition Assay IC50=7.48894 μM SANGER
TE-8 Growth Inhibition Assay IC50=7.76159 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=9.11675 μM SANGER
D-336MG Growth Inhibition Assay IC50=9.47395 μM SANGER
GCIY Growth Inhibition Assay IC50=9.5742 μM SANGER
KS-1 Growth Inhibition Assay IC50=9.66287 μM SANGER
HCC2998 Growth Inhibition Assay IC50=9.96307 μM SANGER
D-247MG Growth Inhibition Assay IC50=9.98291 μM SANGER
TE-15 Growth Inhibition Assay IC50=10.245 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=10.2565 μM SANGER
ETK-1 Growth Inhibition Assay IC50=10.623 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=10.961 μM SANGER
KNS-42 Growth Inhibition Assay IC50=11.7255 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=12.1712 μM SANGER
SR Growth Inhibition Assay IC50=12.2064 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=12.8985 μM SANGER
ES6 Growth Inhibition Assay IC50=13.078 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=13.2577 μM SANGER
D-392MG Growth Inhibition Assay IC50=13.6428 μM SANGER
NB7 Growth Inhibition Assay IC50=14.2374 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=14.5145 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=14.7889 μM SANGER
CA46 Growth Inhibition Assay IC50=15.0586 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=15.1901 μM SANGER
BC-1 Growth Inhibition Assay IC50=15.3314 μM SANGER
LS-123 Growth Inhibition Assay IC50=15.8173 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=16.0924 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=16.7313 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=16.9372 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=17.1529 μM SANGER
NCI-H322M Growth Inhibition Assay IC50=17.4366 μM SANGER
ES7 Growth Inhibition Assay IC50=18.3914 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=18.4386 μM SANGER
SF268 Growth Inhibition Assay IC50=18.7409 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=19.0742 μM SANGER
HCE-T Growth Inhibition Assay IC50=20.2344 μM SANGER
A101D Growth Inhibition Assay IC50=20.8587 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=20.913 μM SANGER
LXF-289 Growth Inhibition Assay IC50=21.038 μM SANGER
NALM-6 Growth Inhibition Assay IC50=21.1967 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=21.4813 μM SANGER
EW-16 Growth Inhibition Assay IC50=22.1402 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=22.2149 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=22.3965 μM SANGER
SKM-1 Growth Inhibition Assay IC50=22.7351 μM SANGER
DMS-153 Growth Inhibition Assay IC50=23.4204 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=23.5452 μM SANGER
LP-1 Growth Inhibition Assay IC50=23.8097 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=24.292 μM SANGER
MPP-89 Growth Inhibition Assay IC50=25.2036 μM SANGER
U-698-M Growth Inhibition Assay IC50=25.2503 μM SANGER
HC-1 Growth Inhibition Assay IC50=25.6418 μM SANGER
HCC2157 Growth Inhibition Assay IC50=25.673 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=26.273 μM SANGER
LS-411N Growth Inhibition Assay IC50=26.3369 μM SANGER
Becker Growth Inhibition Assay IC50=26.5181 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=26.7575 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=27.3867 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=27.4566 μM SANGER
RKO Growth Inhibition Assay IC50=28.1446 μM SANGER
TE-441-T Growth Inhibition Assay IC50=28.789 μM SANGER
EW-24 Growth Inhibition Assay IC50=29.1259 μM SANGER
no-10 Growth Inhibition Assay IC50=29.1631 μM SANGER
D-542MG Growth Inhibition Assay IC50=29.9221 μM SANGER
ST486 Growth Inhibition Assay IC50=30.6451 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=30.8057 μM SANGER
ES8 Growth Inhibition Assay IC50=31.5972 μM SANGER
BL-41 Growth Inhibition Assay IC50=32.1054 μM SANGER
NB6 Growth Inhibition Assay IC50=32.3855 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=32.4967 μM SANGER
MS-1 Growth Inhibition Assay IC50=32.7751 μM SANGER
MFH-ino Growth Inhibition Assay IC50=34.3224 μM SANGER
NOS-1 Growth Inhibition Assay IC50=34.6748 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=35.3667 μM SANGER
EB2 Growth Inhibition Assay IC50=36.6189 μM SANGER
L-540 Growth Inhibition Assay IC50=37.2308 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=38.8846 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=39.9651 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=42.415 μM SANGER
BC-3 Growth Inhibition Assay IC50=45.4896 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=45.5474 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=45.666 μM SANGER
SNB75 Growth Inhibition Assay IC50=46.018 μM SANGER

... Click to View More Cell Line Experimental Data

In vivo Oral administration of Lapatinib (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner. [1]