Lapatinib (GW-572016) Ditosylate

For research use only.

Catalog No.S1028

77 publications

Lapatinib (GW-572016) Ditosylate Chemical Structure

CAS No. 388082-77-7

Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 191 In stock
USD 147 In stock
USD 257 In stock
USD 400 In stock
USD 670 In stock
USD 797 In stock
USD 1190 In stock
Bulk Discount

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

Selleck's Lapatinib (GW-572016) Ditosylate has been cited by 77 publications

Purity & Quality Control

Choose Selective HER2 Inhibitors

Biological Activity

Description Lapatinib (GW-572016) 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)
9.2 nM 10.8 nM 367 nM
In vitro

Lapatinib Ditosylate 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 Ditosylate 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 Ditosylate inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib Ditosylate 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 Ditosylate 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
HN5 cell line Mn24VJJwdGmoZYLheIlwdiCjc4PhfS=> NFTxNWVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjOOUBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN MnHpNVY1QDN5N{K=
BT474 cell line NX2yXGFzWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFvl[YxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOFc1KGOnbHygcIlv\SxiSVO1NF0xNjB{NTFOwG0> MkXZNVY1QDN5N{K=
HN5 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4nVeWlvcGmkaYTpc44hd2ZiSF61JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkGyJO69VQ>? NETPcVYyPjd5N{SxNC=>
BT474 cell MlvTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWPaV3RLUW6qaXLpeIlwdiCxZjDCWFQ4PCClZXzsJIdzd3e2aDDh[pRmeiB5MjDodpMtKEmFNUC9NE4xQCEQvF2= NWjqeJhPOTZ5N{e0NVA>
N87 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEXTe4tKdmirYnn0bY9vKG:oIF64O{Bk\WyuIHfyc5d1cCCjZoTldkA4OiCqcoOsJGlEPTB;MD6wPEDPxE1? M{\DTVE3Pzd5NEGw
HFF cell NELjfGJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkHqTY5pcWKrdHnvckBw\iCKRl[gZ4VtdCCpcn;3eIgtKEmFNUC9PU46KM7:TR?= MVexOlc4PzRzMB?=
SKBR3 cells MXTDfZRwfG:6aXPpeJkh[XO|YYm= NUHlOJE5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjBzNzFOwG0> NVvyXnVWOTlyMki0NlU>
A431 cells NITtUZVEgXSxdH;4bYNqfHliYYPzZZk> M1XITmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1OzFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlExPCEQvF2= MonYNVk5QDh5NkG=
SKBR3 cells M2rrcmN6fG:2b4jpZ4l1gSCjc4PhfS=> MonUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlAzQSEQvF2= M{jidFE6QDh6N{[x
HepG2 cells NXPVZ5h6WHKxbHnm[ZJifGmxbjDhd5NigQ>? MlXjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9Ok4zPyEQvF2= NVLpSngxOjBzNEO3O|g>
Hep3B2 cells MXfQdo9tcW[ncnH0bY9vKGG|c3H5 M4XUb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwN2IzKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF02NjR7IN88US=> NV;hfGxWOjBzNEO3O|g>
SKHEP1 cells NFLoRlBRem:uaX\ldoF1cW:wIHHzd4F6 MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONSFXQNUBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9OU4{KM7:TR?= NHO1TZczODF2M{e3PC=>
MCF7 cells MlO2VJJwdGmoZYLheIlwdiCjc4PhfS=> NFfmOVRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVYvPiEQvF2= MYGyNFE1Ozd5OB?=
MDA-MB-231 cells NF[5bZlRem:uaX\ldoF1cW:wIHHzd4F6 MnrERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGGodHXyJIhzeyCkeTDBWHAh[2:wdHXueEBie3OjeTygTWM2OD13LkSg{txO MWmyNFE1Ozd5OB?=
SK-BR-3 cells NGDHcJVRem:uaX\ldoF1cW:wIHHzd4F6 MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLVLSMVMh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVAvODRizszN NHrBZYUzODF2M{e3PC=>
A431 cells M2LTcmZ2dmO2aX;uJIF{e2G7 MnH0TY5pcWKrdHnvckBw\iCHR1\SJIlvfHKjY3XscJVt[XJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEF2M{GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5yNUKg{txO M3XuSFIxOzR4NkW1
N87 cells M3LHd2Z2dmO2aX;uJIF{e2G7 MmCwTY5pcWKrdHnvckBw\iCHcnLCNkBqdnS{YXPlcIx2dGG{IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCQOEegZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5zIN88US=> NVr1OpMzOjB|NE[2OVU>
MIAPaCa cells M{fvfWZ2dmO2aX;uJIF{e2G7 MmDkTY5pcWKrdHnvckBw\iCHR1\SJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNTWFR[UOjIHPlcIx{KGK7IFXMTXNCNCCLQ{WwQVAvPDN|IN88US=> M4rmNVIxQDF5NUKz
MIAPaCa cells MV7GeY5kfGmxbjDhd5NigQ>? M{j6bGlvcGmkaYTpc44hd2ZiRWLCZlIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5zNDFOwG0> M3S0[FIxQDF5NUKz
CAL27 cells NVvYT2RRS3m2b4TvfIlkcXS7IHHzd4F6 MWHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDRWwzPyClZXzsd{BwfmW{ZYjwdoV{e2mwZzDFS2ZTKGK7IILld4F7fXKrbjDkfYUhemWmdXP0bY9vKGG|c3H5MEBKSzVyPUCuNFA4KM7:TT6= NFjjOWEzOTB6ME[yPS=>
SKOV3 cells MoPjR5l1d3SxeHnjbZR6KGG|c3H5 MkixR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMhd3[ncnX4dJJme3OrbnegTGVTOiCkeTDy[ZNignW{aX6g[JlmKHKnZIXjeIlwdiCjc4PhfUwhUUN3ME2wMlAxOyEQvF2u MnnENlExQDB4Mkm=
CAL27 cells NHn2eZZHfW6ldHnvckBie3OjeR?= NG\S[nUyPiCq MXTJcohq[mm2aX;uJI9nKEWJRj3pcoR2[2WmIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGNCVDJ5IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGVITlJiYX\0[ZIhOTZiaILzJIJ6KFenc4Tldo4h[myxdDygTWM2OD1yLkCzNkDPxE1? NUOwUW5{OjFyOEC2Nlk>
SK-BR-3 cells MlH5VJJwdGmoZYLheIlwdiCjc4PhfS=> Mn7URY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDFdoJDOiCxdnXy[ZhxemW|c3nu[{BpfW2jbjDTT{1DWi1|IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkCzNkDPxE1? NV3LOHRXOjF3N{C4OFM>
BXF T24 cells Mnn3R5l1d3SxeHnjbZR6KGG|c3H5 Mon3OEBl[Xm| M3j1bWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJZTiCWMkSgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVkvPjVizszN NYLEUINVOjJzNkm2NFE>
CXF 269L cells MnvDR5l1d3SxeHnjbZR6KGG|c3H5 M3O3TlQh\GG7cx?= M{HqdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNZTiB{NknMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF05NjN4IN88US=> NVrXXHA3OjJzNkm2NFE>
DIFI cells MmPER5l1d3SxeHnjbZR6KGG|c3H5 NUj6fmwyPCCmYYnz MkfHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSGlHUSClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;MD6yN|Uh|ryP Mnn0NlIyPjl4MEG=
HT-29 cells M4rJT2N6fG:2b4jpZ4l1gSCjc4PhfS=> NGj0NpA1KGSjeYO= NVPhV|FWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRvMkmgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVQvPjJizszN NU\VNWlKOjJzNkm2NFE>
RKO cells NW\DeGlmS3m2b4TvfIlkcXS7IHHzd4F6 M{nxfVQh\GG7cx?= M4\WdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJMVyClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;NT6zOUDPxE1? NXG1N2Y3OjJzNkm2NFE>
GXF251L cells MXzDfZRwfG:6aXPpeJkh[XO|YYm= MmTGOEBl[Xm| M1fWOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdZTjJ3MVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVEvPDhizszN Mn;1NlIyPjl4MEG=
LIXF 575L cells NXTyNIFpS3m2b4TvfIlkcXS7IHHzd4F6 NGLGPGE1KGSjeYO= NIXNWVZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNUViIIEW3OWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTdwMUig{txO NWK2ZpUzOjJzNkm2NFE>
LXFA 289L cells MYjDfZRwfG:6aXPpeJkh[XO|YYm= NEnHNW41KGSjeYO= NEfQXY5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIEK4PWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTVwN{mg{txO MUOyNlE3QTZyMR?=
LXFA 526L NVnyVGtpS3m2b4TvfIlkcXS7IHHzd4F6 MUi0JIRigXN? NI\PcVdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIEWyOmwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTRwMkGg{txO MV6yNlE3QTZyMR?=
LXFA 629L cells NED1emdEgXSxdH;4bYNqfHliYYPzZZk> MkfkOEBl[Xm| NGLWZWhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIE[yPWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTJwOEeg{txO MV6yNlE3QTZyMR?=
LXFL 1121L cells M{HMPGN6fG:2b4jpZ4l1gSCjc4PhfS=> M{Ll[lQh\GG7cx?= MoixR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHhHVCBzMUKxUEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Py55MzFOwG0> MWCyNlE3QTZyMR?=
LXFL 529L cells NYKyTndMS3m2b4TvfIlkcXS7IHHzd4F6 NH3rPIs1KGSjeYO= MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMXGZNKDV{OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvPTFizszN NXvXPGJKOjJzNkm2NFE>
MCF7 cells NXO3cW5qS3m2b4TvfIlkcXS7IHHzd4F6 M2jYPFQh\GG7cx?= MnTUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;ND64N{DPxE1? NWq3TnAzOjJzNkm2NFE>
MDA231 cells Mkm2R5l1d3SxeHnjbZR6KGG|c3H5 MYO0JIRigXN? M4PISmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSTJ|MTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9O{44KM7:TR?= NWjiWFJEOjJzNkm2NFE>
OVXF 899L NWPM[WNlS3m2b4TvfIlkcXS7IHHzd4F6 M4LmW|Qh\GG7cx?= MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDPWnhHKDh7OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvOzVizszN MmmzNlIyPjl4MEG=
PAXF 546L cells M3vCb2N6fG:2b4jpZ4l1gSCjc4PhfS=> Mn7SOEBl[Xm| NF;QWYNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSViIIEW0Omwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTZwMUKg{txO NWr0RlB7OjJzNkm2NFE>
PANC1 cells MlfmR5l1d3SxeHnjbZR6KGG|c3H5 NVzqVoliPCCmYYnz NGjNPXlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSU6FMTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9PE4yOiEQvF2= M4PiflIzOTZ7NkCx
22Rv1 cell NWm4foFZS3m2b4TvfIlkcXS7IHHzd4F6 MYe0JIRigXN? NGf5[mJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckAzOlK4MTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9Ok4xPiEQvF2= M3fh[VIzOTZ7NkCx
DU145 cells MYrDfZRwfG:6aXPpeJkh[XO|YYm= MVe0JIRigXN? NU\hbWF1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVIvQTlizszN NHTL[5YzOjF4OU[wNS=>
LNCAP cells MnjpR5l1d3SxeHnjbZR6KGG|c3H5 NIXTbIo1KGSjeYO= MnewR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG5ESVBiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUOuOlgh|ryP MmXkNlIyPjl4MEG=
PC3M cells NIG4R4lEgXSxdH;4bYNqfHliYYPzZZk> MXm0JIRigXN? M1TsXmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEO01iY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuOVUh|ryP NEO4PVQzOjF4OU[wNS=>
NIH/3T3 cells MWfQdo9tcW[ncnH0bY9vKGG|c3H5 MmT6O|IhcA>? NUnaZYI1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDOTWgwO1R|IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OE4{KM7:TR?= MWOyNlU6PTF5Nx?=
NCI-H1648 cell MnrBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMU[0PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODJ3NESg{txO M1PVbXNCVkeHUh?=
NMC-G1 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGK0cW9KdmirYnn0bY9vKG:oIHj1cYFvKE6PQz3HNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPTR3MEGg{txO MUPTRW5ITVJ?
NTERA-S-cl-D1 cell MoPVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYnJcohq[mm2aX;uJI9nKGi3bXHuJG5VTVKDLWOtZ4wuTDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkK2OVYyKM7:TR?= NXHUNplNW0GQR1XS
OCUB-M cell M{PDfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFU4PCEQvF2= NGntTnFUSU6JRWK=
OS-RC-2 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnzwTY5pcWKrdHnvckBw\iCqdX3hckBQWy2UQz2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46QTF7OTFOwG0> NGPKZVFUSU6JRWK=
OVCAR-4 cell NXrBbY9qT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUn5b4J{UW6qaXLpeIlwdiCxZjDoeY1idiCRVlPBVk01KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS5zMU[3OUDPxE1? MVTTRW5ITVJ?
RL95-2 cell NIjsSlBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NE\vboVKdmirYnn0bY9vKG:oIHj1cYFvKFKOOUWtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOTV4NzFOwG0> MXPTRW5ITVJ?
SW954 cell NGGwellIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkL2TY5pcWKrdHnvckBw\iCqdX3hckBUXzl3NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuN|kzPDVizszN NXLFS5p[W0GQR1XS
SW962 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUPJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTZ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zPVI1PSEQvF2= NYLTR|QzW0GQR1XS
TE-1 cell NX\MVlFDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3;RRWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuNFIyPTlizszN NEjJdYJUSU6JRWK=
A253 cell NHmxbZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmGxTY5pcWKrdHnvckBw\iCqdX3hckBCOjV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= NEC0O3BUSU6JRWK=
A388 cell NED1bIhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGE{QDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkC0PFMh|ryP M3P0fHNCVkeHUh?=
BB30-HNC cell NWPLdGlyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWHNc5NEUW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOUezN|Uh|ryP MVjTRW5ITVJ?
TE-12 cell MkPZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVXX[VFiUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ{NUig{txO M2rWenNCVkeHUh?=
TE-5 cell MmrVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnTnTY5pcWKrdHnvckBw\iCqdX3hckBVTS13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yOFY2PCEQvF2= NXv5Ro5lW0GQR1XS
TE-6 cell M2XpW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWjJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5NFU4KM7:TR?= NGG2d5FUSU6JRWK=
TE-8 cell NH3yWHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXvJcohq[mm2aX;uJI9nKGi3bXHuJHRGNThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkCzO|Mh|ryP Ml;qV2FPT0WU
TE-9 cell NITNWG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkTmTY5pcWKrdHnvckBw\iCqdX3hckBVTS17IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT61OVIxOSEQvF2= M{fNVXNCVkeHUh?=
TK10 cell M33OTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1i5OWlvcGmkaYTpc44hd2ZiaIXtZY4hXEtzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVY2OjJizszN M4XwdHNCVkeHUh?=
DSH1 cell MlnDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{PoPGlvcGmkaYTpc44hd2ZiaIXtZY4hTFOKMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFk{QTZizszN M1XERXNCVkeHUh?=
ECC12 cell NYHIPHhjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnjtTY5pcWKrdHnvckBw\iCqdX3hckBGS0NzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFkzOzFizszN MXHTRW5ITVJ?
EKVX cell M1;l[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFS1TmdKdmirYnn0bY9vKG:oIHj1cYFvKEWNVmigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1QDd2IN88US=> M4PLTHNCVkeHUh?=
HCC2218 cell NV34[2FtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mo\BTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{MkG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTN{NjFOwG0> MY\TRW5ITVJ?
LB2241-RCC cell NYS4UGV{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFv4[Y9KdmirYnn0bY9vKG:oIHj1cYFvKEyEMkK0NU1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkG1OFA{KM7:TR?= M4TrZXNCVkeHUh?=
LB996-RCC cell MkjhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmDGTY5pcWKrdHnvckBw\iCqdX3hckBNSjl7Nj3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjN4MkK4JO69VQ>? MoCyV2FPT0WU
LC-1F cell NF24THFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFflfodKdmirYnn0bY9vKG:oIHj1cYFvKEyFLUHGJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{QDJ2NDFOwG0> MVXTRW5ITVJ?
LS-513 cell M3j1U2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXHldJpiUW6qaXLpeIlwdiCxZjDoeY1idiCOUz21NVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjRyMESxJO69VQ>? NFfFPGlUSU6JRWK=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ErbB2 / t-ErbB2 / p-Akt / t-Akt / p-Erk / t-Erk; 

PubMed: 25238247     


Dose response of lapatinib and PD168393 on phosphorylation of ErbB2, AKT and ERK in Calu3 and SkBr3 cells in response to EGF treatment. p-ErbB2: phosphorylated ErbB2; t-ErbB2: total-ErbB2; p-AKT: phosphorylated AKT; t-AKT: total AKT; p-ERK: phosphorylated ERK; t-ERK: total ERK.

pEGFR / EGFR / p-mTOR / 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. All values are presented as the mean ± standard error (S.E.) (**p < 0.01).

25238247 28938602
Growth inhibition assay
Cell viability ; 

PubMed: 24947784     


Huh7 (A), HepG2 (B), or HA22T (C) HCC cells were left untreated or treated with 0.1% DMSO (vehicle, D) or with DMSO containing various concentrations of lapatinib (1.25, 2.5, 5, or 10 μM) for 3 days. Relative amounts of viable cells were detected by MTS assay. O.D. values from DMSO-treated control cells were designated 100%.

24947784
In vivo Oral administration of Lapatinib Ditosylate (~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
  • 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 (108.05 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+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 925.46
Formula

C29H26ClFN4O4S.2C7H8O3S

CAS No. 388082-77-7
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O.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 need to use S1028 for treating tumor-bearing mice with injection, how could I prepare the solution?

  • Answer:

    S1028 Lapatinib Ditosylate can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as clear solution.

HER2 Signaling Pathway Map

HER2 Inhibitors with Unique Features

Related HER2 Products

Tags: buy GW-572016|GW-572016 ic50|GW-572016 price|GW-572016 cost|GW-572016 solubility dmso|GW-572016 purchase|GW-572016 manufacturer|GW-572016 research buy|GW-572016 order|GW-572016 mouse|GW-572016 chemical structure|GW-572016 mw|GW-572016 molecular weight|GW-572016 datasheet|GW-572016 supplier|GW-572016 in vitro|GW-572016 cell line|GW-572016 concentration|GW-572016 nmr|GW-572016 in vivo|GW-572016 clinical trial|GW-572016 inhibitor|GW-572016 Protein Tyrosine Kinase inhibitor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID