Lapatinib

For research use only.

Catalog No.S2111 Synonyms: GW-572016, GSK572016

359 publications

Lapatinib Chemical Structure

CAS No. 231277-92-2

Lapatinib (GSK572016), 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. Lapatinib induces ferroptosis and autophagic cell death.

Size Price Stock Quantity  
10mM (1mL in DMSO) EUR 140 In stock
EUR 108 In stock
EUR 265 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Lapatinib has been cited by 359 publications

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description Lapatinib (GSK572016), 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. Lapatinib induces ferroptosis and autophagic cell death.
Targets
ErbB2 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
ErbB4 [1]
(Cell-free assay)
9.2 nM 10.8 nM 367 nM
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 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LlfWlEPTB;MD6wNlU1PCEQvF2= NFm1T2JUSU6JRWK=
HCC2218 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwMEWzNlYh|ryP MV;TRW5ITVJ?
OCUB-M MlO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoK5TWM2OD1yLkC1O|Qh|ryP M13PZXNCVkeHUh?=
ECC12 NV2yblduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjvTWM2OD1yLkC5NlMyKM7:TR?= NFn6dG5USU6JRWK=
DSH1 MkW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4n6N2lEPTB;MD6wPVM6PiEQvF2= Mn:yV2FPT0WU
BT-474 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfmOoNWUUN3ME2wMlIyOzF3IN88US=> NVXQTHRVW0GQR1XS
BB30-HNC M2LFXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\oV3BKSzVyPUCuNlQ3PTRizszN Mn31V2FPT0WU
EKVX M2fRXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mle0TWM2OD1yLkS0PFc1KM7:TR?= M3TqUHNCVkeHUh?=
TE-12 NVrxfZBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDCTWM2OD1yLkS5NFU4KM7:TR?= MXTTRW5ITVJ?
A388 M1vOb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC0VGVKSzVyPUCuO|IzPThizszN NFPhWmlUSU6JRWK=
TE-9 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFWxO2lKSzVyPUCuO|Q1PTNizszN NGqwOIFUSU6JRWK=
LB2241-RCC NULKSVJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTFwMUW0NFMh|ryP NXHNcYpnW0GQR1XS
LB996-RCC Mln2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrXZndKSzVyPUGuN|YzOjhizszN MUXTRW5ITVJ?
LC-1F MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFwM{iyOFQh|ryP M3PaS3NCVkeHUh?=
TE-6 M1P2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TXfGlEPTB;MT61OVIxOSEQvF2= NF3ySGNUSU6JRWK=
A253 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jKWWlEPTB;MT65O|M{PSEQvF2= M2foXXNCVkeHUh?=
OS-RC-2 M1LCbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHkc4N{UUN3ME2xMlk6OTl7IN88US=> M{DmXHNCVkeHUh?=
TE-1 NIOxW3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TYRWlEPTB;Mj6wOFg{KM7:TR?= MnyyV2FPT0WU
RL95-2 NUjGOWVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvxNHZHUUN3ME2zMlE2PjdizszN NF3HXHVUSU6JRWK=
LS-513 M4XaSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn64TWM2OD1|LkSwNFQyKM7:TR?= NXfQW25HW0GQR1XS
DJM-1 MnXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7PV25KSzVyPUOuOFY6PzVizszN MlPuV2FPT0WU
NMC-G1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33E[GlEPTB;Mz61OFUxOSEQvF2= M2nNbnNCVkeHUh?=
TE-10 M3vSOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TmdWlEPTB;Mz61OVM2PiEQvF2= NWnkVHNoW0GQR1XS
TE-5 NH3MRlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfRWJVKSzVyPUSuNFM4OyEQvF2= MlzoV2FPT0WU
TK10 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTRwMU[1NlIh|ryP M2nnXXNCVkeHUh?=
UACC-812 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLFTWM2OD12LkW2NVU{KM7:TR?= NEPpZnhUSU6JRWK=
SW962 M1XsfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjpdVF1UUN3ME21MlAzOTV7IN88US=> NUTWVm5XW0GQR1XS
SW954 NIjPVW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;Sclg3UUN3ME21MlM6OjR3IN88US=> NF7qPJdUSU6JRWK=
COLO-668 NV\FS49LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz5TWM2OD13LkeyOlY4KM7:TR?= NXP2S3dmW0GQR1XS
LB1047-RCC NILBUINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fENWlEPTB;NT64NFA1PiEQvF2= NIPyRohUSU6JRWK=
NB5 NXTTN3pNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj0U3BKSzVyPU[uNlExODFizszN NWrLRXVuW0GQR1XS
NTERA-S-cl-D1 M4rCSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPjbpRIUUN3ME22MlI3PTZzIN88US=> NW[2UXU{W0GQR1XS
IST-MEL1 NUT6bmc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTZwNEO2PVQh|ryP MVfTRW5ITVJ?
GI-1 NYq5XpZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jEbWlEPTB;Nj61NVY5OiEQvF2= NGXPd3NUSU6JRWK=
TGBC1TKB M2X4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzyTWM2OD15LkC3NVg{KM7:TR?= NWXKNVZyW0GQR1XS
GT3TKB MnK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXmSFh5UUN3ME23MlIzPzR2IN88US=> NFnCPI9USU6JRWK=
EVSA-T NW\FTHlKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkW5TWM2OD15LkSyPFEyKM7:TR?= NE\Jb3lUSU6JRWK=
D-502MG Ml3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTETWM2OD15LkS4PFk1KM7:TR?= MnS2V2FPT0WU
TE-8 NFi2[4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHNTZdDUUN3ME23Mlc3OTV7IN88US=> MWDTRW5ITVJ?
OVCAR-4 MmCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVW1dJlGUUN3ME25MlEyPjd3IN88US=> NHXseFlUSU6JRWK=
D-336MG NIXuOYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vNOGlEPTB;OT60O|M6PSEQvF2= NXOw[GhqW0GQR1XS
GCIY NHfnUZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLD[mNKSzVyPUmuOVc1OiEQvF2= Moi5V2FPT0WU
KS-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjrTWM2OD17Lk[2Nlg4KM7:TR?= MkniV2FPT0WU
HCC2998 MnHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPJV2hCUUN3ME25Mlk3OzB5IN88US=> NE\NU3hUSU6JRWK=
D-247MG Mne0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTlwOUiyPVEh|ryP NVHSfJlQW0GQR1XS
TE-15 MkDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFyLkK0OUDPxE1? NHX5S3lUSU6JRWK=
IST-MES1 M3TFd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXQeJpjUUN3ME2xNE4zPTZ3IN88US=> MmmxV2FPT0WU
ETK-1 NG\IS2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjGU3VKSzVyPUGwMlYzOyEQvF2= M37IeXNCVkeHUh?=
RCC10RGB M{Pj[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LTU2lEPTB;MUCuPVYyKM7:TR?= MkfiV2FPT0WU
KNS-42 M3LaW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrIUol5UUN3ME2xNU44OjV3IN88US=> MVLTRW5ITVJ?
LB771-HNC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLuTWM2OD1zMj6xO|EzKM7:TR?= NFnuflhUSU6JRWK=
SR NF3tN5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGG3bpJKSzVyPUGyMlIxPjRizszN NVuyPYloW0GQR1XS
NCI-H1355 NVrXcGNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHsTWM2OD1zMj64PVg2KM7:TR?= NI\NVINUSU6JRWK=
ES6 MmrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jCRWlEPTB;MUOuNFc5KM7:TR?= NFPWe|RUSU6JRWK=
SK-NEP-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIK4SnJKSzVyPUGzMlI2PzdizszN Mln6V2FPT0WU
D-392MG Mn\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\ZeoJ5UUN3ME2xN{43PDJ6IN88US=> MVHTRW5ITVJ?
NB7 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTHcGh3UUN3ME2xOE4zOzd2IN88US=> NH3ST|lUSU6JRWK=
SK-LMS-1 M2jPSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7MTHJKSzVyPUG0MlUyPDVizszN M1ThZ3NCVkeHUh?=
SK-UT-1 MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nqemlEPTB;MUSuO|g5QSEQvF2= M3jmfnNCVkeHUh?=
CA46 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTF3LkC1PFYh|ryP M1H6OnNCVkeHUh?=
IST-SL2 M2m3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;qV5F3UUN3ME2xOU4yQTBzIN88US=> MUPTRW5ITVJ?
BC-1 MnLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjEb21KSzVyPUG1MlM{OTRizszN NGPXUphUSU6JRWK=
LS-123 M17Efmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTF3LkixO|Mh|ryP NWfkPHM3W0GQR1XS
Ramos-2G6-4C10 M{fI[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjuSodKSzVyPUG2MlA6OjRizszN M4CwVHNCVkeHUh?=
MZ1-PC NIHY[W1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTFTWM2OD1zNj63N|E{KM7:TR?= NH2z[3NUSU6JRWK=
LB647-SCLC NWnEXFFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrwb2lxUUN3ME2xOk46Ozd{IN88US=> NFPteVJUSU6JRWK=
NCI-H1694 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTF5LkG1Nlkh|ryP NVvZc3l{W0GQR1XS
NCI-H322M MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX1TWM2OD1zNz60N|Y3KM7:TR?= MlrSV2FPT0WU
ES7 M2K2[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DHO2lEPTB;MUiuN|kyPCEQvF2= MlLkV2FPT0WU
LC-2-ad MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fQUGlEPTB;MUiuOFM5PiEQvF2= M1;IfnNCVkeHUh?=
SF268 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\xW21KSzVyPUG4Mlc1ODlizszN M2S2cXNCVkeHUh?=
RPMI-8402 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXjdGx{UUN3ME2xPU4xPzR{IN88US=> NWHzO3R4W0GQR1XS
HCE-T NUDNZ5hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;ue25YUUN3ME2yNE4zOzR2IN88US=> M3WwWnNCVkeHUh?=
A101D NInMfY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJyLki1PFch|ryP MV\TRW5ITVJ?
MRK-nu-1 MlLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJyLkmxN{DPxE1? M3jxfHNCVkeHUh?=
LXF-289 NHrycW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJzLkCzPEDPxE1? Mn[yV2FPT0WU
NALM-6 M1fDdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfFTIU1UUN3ME2yNU4yQTZ5IN88US=> MkjoV2FPT0WU
DOHH-2 NFHmS5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\KUmlEPTB;MkGuOFgyOyEQvF2= NHjsN|ZUSU6JRWK=
EW-16 M4PsbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LySGlEPTB;MkKuNVQxOiEQvF2= NVnRbYcyW0GQR1XS
A4-Fuk NFf1RWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfuRXVKSzVyPUKyMlIyPDlizszN NH7TbnZUSU6JRWK=
HD-MY-Z MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXwVmxKUUN3ME2yNk4{QTZ3IN88US=> MVvTRW5ITVJ?
SKM-1 NHnXRVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTJ{LkezOVEh|ryP MWXTRW5ITVJ?
DMS-153 NYqwU2FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzpVFBKSzVyPUKzMlQzODRizszN NHXlZXdUSU6JRWK=
LB373-MEL-D MmHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4X2cmlEPTB;MkOuOVQ2OiEQvF2= Mo[zV2FPT0WU
LP-1 M3q1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfCTWM2OD1{Mz64NFk4KM7:TR?= MoLpV2FPT0WU
GI-ME-N Ml7GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknaTWM2OD1{ND6yPVIh|ryP MX3TRW5ITVJ?
MPP-89 Mk\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHadIQ3UUN3ME2yOU4zODN4IN88US=> NVfCXWRjW0GQR1XS
U-698-M M4TpfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jKcGlEPTB;MkWuNlUxOyEQvF2= NXrr[WFiW0GQR1XS
HC-1 M1rNNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLPTWM2OD1{NT62OFE5KM7:TR?= MonVV2FPT0WU
HCC2157 M2LhXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXsclZVUUN3ME2yOU43PzNizszN MlrLV2FPT0WU
MOLT-4 MmrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\NemlEPTB;Mk[uNlc{KM7:TR?= NHnUVZZUSU6JRWK=
LS-411N M13GXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe4XFdKSzVyPUK2MlM{PjlizszN NWnZVY42W0GQR1XS
Becker MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjDTVlwUUN3ME2yOk42OThzIN88US=> MULTRW5ITVJ?
NCI-H23 NWTONW1RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fKT2lEPTB;Mk[uO|U4PSEQvF2= M3P0NHNCVkeHUh?=
IST-SL1 M3rEbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLab5d[UUN3ME2yO{4{QDZ5IN88US=> M{nScXNCVkeHUh?=
MZ2-MEL M{HLT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nxd2lEPTB;MkeuOFU3PiEQvF2= MVjTRW5ITVJ?
RKO NHLM[VJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPwO4ZKSzVyPUK4MlE1PDZizszN M2i1UnNCVkeHUh?=
TE-441-T NVfMVWJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTJ6Lke4PUDPxE1? Mn\SV2FPT0WU
EW-24 M3nsRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlL2TWM2OD1{OT6xNlU6KM7:TR?= NXrTVnRiW0GQR1XS
no-10 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVn0NVNsUUN3ME2yPU4yPjNzIN88US=> MWXTRW5ITVJ?
D-542MG MnjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfDcpRKSzVyPUK5MlkzOjFizszN NIDiZmJUSU6JRWK=
ST486 NGfJTZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTNyLk[0OVEh|ryP NIDD[|ZUSU6JRWK=
KURAMOCHI MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXMNVhKSzVyPUOwMlgxPTdizszN MlLyV2FPT0WU
ES8 Mlj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTNzLkW5O|Ih|ryP Mk[zV2FPT0WU
BL-41 NX\Lb2JlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Hl[GlEPTB;M{KuNVA2PCEQvF2= Mmr6V2FPT0WU
NB6 M4XjWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPjbFBKSzVyPUOyMlM5PTVizszN MV;TRW5ITVJ?
NCI-H1304 M4jVemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjiRYJKSzVyPUOyMlQ6PjdizszN MlTvV2FPT0WU
MS-1 M1GybGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXS[pFKSzVyPUOyMlc4PTFizszN Mkj0V2FPT0WU
MFH-ino MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DkdmlEPTB;M{SuN|IzPCEQvF2= M{fIfHNCVkeHUh?=
NOS-1 MoX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIm2bGVKSzVyPUO0MlY4PDhizszN NWTPcplQW0GQR1XS
HUTU-80 M3y5Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PqTGlEPTB;M{WuN|Y3PyEQvF2= MWDTRW5ITVJ?
EB2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF6yTFVKSzVyPUO2MlYyQDlizszN NVLOcWozW0GQR1XS
L-540 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYP6bW5kUUN3ME2zO{4zOzB6IN88US=> NEnudXdUSU6JRWK=
NCI-H747 MkCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTN6Lki4OFYh|ryP NEjBfJNUSU6JRWK=
NCI-H446 NXfZTW1ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofzTWM2OD1|OT65OlUyKM7:TR?= NITScnZUSU6JRWK=
MOLT-16 MkTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTR{LkSxOUDPxE1? NF\SXmhUSU6JRWK=
BC-3 Mk\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2L6TWlEPTB;NEWuOFg6PiEQvF2= NUHGWoFKW0GQR1XS
SJSA-1 NFvl[HpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf2VZFmUUN3ME20OU42PDd2IN88US=> NUTUTYRQW0GQR1XS
BB65-RCC MkfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHxU5gxUUN3ME20OU43PjZizszN MlizV2FPT0WU
SNB75 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;OVY1KSzVyPUS2MlAyQCEQvF2= M1vL[nNCVkeHUh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 ; 

PubMed: 29799521     


Downregulation of HSF1, mutp53, and Mdm2 in lapatinib-sensitive parental BT474, but not in lapatinib-resistant BT474R cells, treated with indicated lapatinib concentrations for 24 h.

pEGFR / EGFR / pAkt / Akt / pmTOR / mTOR / PARP / c-PARP ; 

PubMed: 28938602     


SKBR3 and 78617 cells were treated with lapatinib as in panel A, then the expression of phospho-ErbB2 (Tyr1221/1222), ErbB2, phospho-EGFR (Tyr1068), EGFR, phospho-Akt (Ser473), Akt, phospho-Erk1/2 (Thr202/Tyr204), Erk2, phospho-mTOR (Ser2448), and mTOR were analyzed using Western blotting. 

p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1; 

PubMed: 22853430     


A panel of HER2-amplified breast cancer cells were treated with 200nM lapatinib for up to 72 hours to detect the initial downregulation and subsequent upregulation of HER2-HER3 and downstream signaling. Immunoblots were performed using the indicated antibodies.

29799521 28938602 22853430
Immunofluorescence
LC3 ; 

PubMed: 26637440     


SKBR3 GFP-LC3 cells were cultured for 6 days and UACC893 GFP-LC3 cells were cultured for 7 days with 5 μM EZN3046 or EZN4150 .

Vimentin / E-cadherin; 

PubMed: 28243326     


Cells treated with lapatinib (5µM) increased the expression of E-cadherin and inhibited the expression of Vimentin by immunofluorescence. (Magnification: 1000×).

26637440 28243326
Growth inhibition assay
Cell viability (OE19); 

PubMed: 25350844     


Dose-response curves from escalated dose of lapatinib in the presence of 1 µM concentration of saracatinib. The calculated values of IC50 for lapatinib were following; 207.3 nM and 145 nM, respectively, after lapatinib alone and in the presence of saracatinib for parental OE19; >1,000 nM after lapatinib alone for LR2A and LR2B; 91.66 nM and 224.0 nM in the presence of saracatinib in LR2A and LR2B, respectively. Values were presented as relative cellular viability relative to vehicle-treated controls with the mean ± S.E. of quadruplicate from a representative experiment. The p values calculated by two-way ANOVA were <0.0001 comparing lapatinib alone with lapatinib plus saracatinib both in the LR2A and LR2B.

Cell viability (A431 cells); 

PubMed: 28243326     


The MTT assay was performed on the viability of A431 cells by lapatinib at different concentrations (0.1-50μM) and IC50 value was analyzed as indicated on the plot (t-test).

25350844 28243326
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]

Protocol

Kinase Assay:[1]
- Collapse

In vitro kinase assays:

The IC50 values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi of [γ33P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of Lapatinib beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves.
Cell Research:[1]
- Collapse
  • Cell lines: HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, and HB4a c5.2 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~100 μM
  • Incubation Time: 72 hours
  • Method: Cells are exposed to various concentrations of Lapatinib for 72 hours. Relative cell number is estimated using methylene blue staining. The absorbance at 620 nm is read in a Spectra microplate reader. Cell death and cell cycle analysis are assessed by propidium iodide staining and antibody detection of incorporated BrdUrd and staining with propidium iodide.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: CD-1 nude female mice implanted s.c. with HN5 cells, and C.B-17 SCID female mice implanted s.c. with BT474 cells
  • Dosages: ~100 mg/kg
  • Administration: Orally twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (172.09 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 581.06
Formula

C29H26ClFN4O4S

CAS No. 231277-92-2
Storage powder
in solvent
Synonyms GW-572016, GSK572016
Smiles CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03075995 Unknown status Other: hight-fat breakfast Breast Cancer Sun Yat-sen University April 12 2017 Not Applicable
NCT02338245 Completed Drug: ASLAN001|Drug: Lapatinib|Drug: Capecitabine Metastatic Breast Cancer Aslan Pharmaceuticals December 29 2014 Phase 2
NCT02294786 Terminated Drug: Lapatinib|Drug: Capecitabine|Drug: Octreotide Cancer Novartis Pharmaceuticals|Novartis December 17 2014 Phase 2
NCT02213042 Completed Drug: Lapatinib|Biological: Trastuzumab Neoplasms Breast Novartis Pharmaceuticals|Novartis October 24 2014 Phase 2
NCT01782651 Completed Drug: Lapatinib plus capecitabine Neoplasms Breast GlaxoSmithKline August 2014 --
NCT02158507 Active not recruiting Drug: Combination of Veliparib + Lapatinib Metastatic Triple Negative Breast Cancer University of Alabama at Birmingham|Scariot Foundation|GlaxoSmithKline|AbbVie July 2014 Not Applicable

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    If I want to use this compound(S2111, Lapatinib) in tumor-bearing mice via injection, how could I prepare the solution?

  • Answer:

    For I.P. administration, the compound solution should be clear solution. S2111 Lapatinib can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.

EGFR Signaling Pathway Map

EGFR Inhibitors with Unique Features

Related EGFR Products

Tags: buy Lapatinib | Lapatinib supplier | purchase Lapatinib | Lapatinib cost | Lapatinib manufacturer | order Lapatinib | Lapatinib distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID