Lapatinib

Catalog No.S2111 Synonyms: GW-572016, GSK572016

Lapatinib Chemical Structure

Molecular Weight(MW): 581.06

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.

Size Price Stock Quantity  
In DMSO USD 143 In stock
USD 110 In stock
USD 270 In stock
Bulk Discount

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

Cited by 42 Publications

7 Customer Reviews

  • Sensitivity to the ErbB1/ErbB2 inhibitor lapatinib is highest for cancer cells from late-stage tumors in culture (mean ± SEM, p = 0.04 or 0.02 as indicated, Student’s t test; values represent the averages of four experiments, each done in triplicate with primary cells from independent mice).

    Cancer Cell 2012 21(4), 488-503. Lapatinib purchased from Selleck.

    Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using specific antibodies.

    Cancer Lett 2013 340(1), 43-50. Lapatinib purchased from Selleck.

  • Inhibition of HER2 using siRNAs show a similar response measured by induced apoptosis, decreased proliferation and decreased phospho-p70-S6K staining as Lapatinib mono-treatment and combinatorial treatment with Lapatinib and trastuzumab. Trastuzumab mono-treatment is less efficient than siHER2.

    Mol Oncol 2013 7(3), 392-401. Lapatinib purchased from Selleck.

    Lapatinib effectively inhibits EGFR activation, leading to a reduc- tion in STAT1 expression. MDA-MB-468 cells with endogenous expression of EGFR and STAT3 were treated with 25 μM lapatinib for 24 h, harvested and subjected to western blotting for EGFR, p-EGFR, and STAT1 expression.

    Mol Carcinog 2013 52(12), 959-69. Lapatinib purchased from Selleck.

  •  

    Endogenous associations between STAT1, EGFR, and p-STAT3 expression in breast cancer cells. (B) Lapatinib effectively inhibits EGFR activation, leading to a reduction in STAT1 expression. MDA-MB-468 cells with endogenous expression of EGFR and STAT3 were treated with 25 uM lapatinib for 24 h, harvested and subjected to western blotting for EGFR, p-EGFR, and STAT1 expression.

    Mol Carcinog 2012 52, 959-69. Lapatinib purchased from Selleck.

    Combination treatment with lapatinib and CZ0775 significantly induces pro-apoptotic BIM proteins in H195 cells. HCC827 (a) and H1975 (b) cells were treated with either 1 μM lapatinib alone or the combination of 1 μM lapatinib plus 1 μM AZD6244 or CZ0775 for 24 h. Cell lysates were analyzed by Western blotting using the indicated antibodies. The levels of β -actin served as a loading control

    Acta Pharmacol Sin 2013 10.1038/aps.2013.124. Lapatinib purchased from Selleck.

  •  

    EGF and TGF-α-induced CD44 expression is reduced by EGFR inhibitors in SKBR3 breast cancer cells. After serum-starvation for 24 h, the cells were pretreated with EGFR inhibitors, AG1478 or lapatinib for 30 min prior to EGF or TGF-α treatment and then, treated with EGF (A) or TGF-α (B) for 24 h. The level of CD44 mRNA expression was analyzed by real-time PCR. After serum-starvation for 24 h, the cells were pretreated with AG1478 or lapatinib for 30 min prior to EGF or TGF-α treatment and then treated with EGF for 24 h (C). The levels of CD44, EGFR, ERK, and β-actin protein expression were analyzed by Western blotting.

    Anticancer Res 2011 31, 3767-3774. Lapatinib purchased from Selleck.

Purity & Quality Control

Choose Selective EGFR Inhibitors

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)
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 NHf5NVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHoTWM2OD1yLkCyOVQ1KM7:TR?= MXXTRW5ITVJ?
HCC2218 M2iyZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwMEWzNlYh|ryP MVvTRW5ITVJ?
OCUB-M M{e0Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFr1bIRKSzVyPUCuNFU4PCEQvF2= NF;a[3NUSU6JRWK=
ECC12 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzRTZhKSzVyPUCuNFkzOzFizszN MYXTRW5ITVJ?
DSH1 NV;aUpZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkH3TWM2OD1yLkC5N|k3KM7:TR?= MkLhV2FPT0WU
BT-474 MlTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwMkGzNVUh|ryP M2HGd3NCVkeHUh?=
BB30-HNC M33URWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorZTWM2OD1yLkK0OlU1KM7:TR?= M3P1c3NCVkeHUh?=
EKVX MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTBwNES4O|Qh|ryP M1mx[3NCVkeHUh?=
TE-12 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrP[4NKSzVyPUCuOFkxPTdizszN NUn2[og{W0GQR1XS
A388 MlXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLBTWM2OD1yLkeyNlU5KM7:TR?= M4fKXnNCVkeHUh?=
TE-9 M1TjV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4KyV2lEPTB;MD63OFQ2OyEQvF2= MUfTRW5ITVJ?
LB2241-RCC NX7qPJVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFwMUW0NFMh|ryP M{K3PHNCVkeHUh?=
LB996-RCC Mlv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjXU|FKSzVyPUGuN|YzOjhizszN MVLTRW5ITVJ?
LC-1F NIK0ZmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTFwM{iyOFQh|ryP NV;3XG5oW0GQR1XS
TE-6 MnvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPRSGFKSzVyPUGuOVUzODFizszN M3\BOXNCVkeHUh?=
A253 NYq1RmpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XOPWlEPTB;MT65O|M{PSEQvF2= NHj4O5ZUSU6JRWK=
OS-RC-2 M3:3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnzeHdDUUN3ME2xMlk6OTl7IN88US=> M3XDfXNCVkeHUh?=
TE-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnmOW1KSzVyPUKuNFQ5OyEQvF2= MVjTRW5ITVJ?
RL95-2 MlPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;kTWM2OD1|LkG1Olch|ryP NW\FV217W0GQR1XS
LS-513 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTNwNECwOFEh|ryP NIHjV4tUSU6JRWK=
DJM-1 NV\hSXpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLzTWM2OD1|LkS2PVc2KM7:TR?= M{TBeHNCVkeHUh?=
NMC-G1 MnvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTNwNUS1NFEh|ryP MofTV2FPT0WU
TE-10 NU\JfndST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLOdZdKSzVyPUOuOVU{PTZizszN MkG4V2FPT0WU
TE-5 NFHHNFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTRwMEO3N{DPxE1? Mmr6V2FPT0WU
TK10 NHjydGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTRwMU[1NlIh|ryP NEjCPVlUSU6JRWK=
UACC-812 MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVu0SZJ[UUN3ME20MlU3OTV|IN88US=> MWfTRW5ITVJ?
SW962 M1fF[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfkTWM2OD13LkCyNVU6KM7:TR?= NVzoOGJvW0GQR1XS
SW954 NG\aS4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTVwM{myOFUh|ryP NVzyRW1nW0GQR1XS
COLO-668 NX3TNZl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jRRmlEPTB;NT63NlY3PyEQvF2= MontV2FPT0WU
LB1047-RCC NXraSVd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HCeGlEPTB;NT64NFA1PiEQvF2= MlTlV2FPT0WU
NB5 MmLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfkV4VKSzVyPU[uNlExODFizszN NV3XRXZEW0GQR1XS
NTERA-S-cl-D1 M1PCOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUO2S|BKUUN3ME22MlI3PTZzIN88US=> NHXONlNUSU6JRWK=
IST-MEL1 NXm5S2ZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;CWnJKSzVyPU[uOFM3QTRizszN MVHTRW5ITVJ?
GI-1 M2HOSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTZwNUG2PFIh|ryP MXrTRW5ITVJ?
TGBC1TKB M2\QVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTdwMEexPFMh|ryP M2DTSnNCVkeHUh?=
GT3TKB MljvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{e5XGlEPTB;Nz6yNlc1PCEQvF2= MWjTRW5ITVJ?
EVSA-T MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTdwNEK4NVEh|ryP M1izT3NCVkeHUh?=
D-502MG MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULl[Yk{UUN3ME23MlQ5QDl2IN88US=> NY[w[FR2W0GQR1XS
TE-8 M{DUSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH6wS4tKSzVyPUeuO|YyPTlizszN M1HU[3NCVkeHUh?=
OVCAR-4 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvTTWM2OD17LkGxOlc2KM7:TR?= MnPGV2FPT0WU
D-336MG M4rndWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWW4VnBPUUN3ME25MlQ4Ozl3IN88US=> Mn7zV2FPT0WU
GCIY NIHSVGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTlwNUe0NkDPxE1? NVS4T3RXW0GQR1XS
KS-1 NGfnc5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTET4xKSzVyPUmuOlYzQDdizszN M32xe3NCVkeHUh?=
HCC2998 NEXXdoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLiRnlHUUN3ME25Mlk3OzB5IN88US=> NWfT[WlDW0GQR1XS
D-247MG M2rLOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTlwOUiyPVEh|ryP NI\Xc5JUSU6JRWK=
TE-15 M1zpXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jyemlEPTB;MUCuNlQ2KM7:TR?= MlLPV2FPT0WU
IST-MES1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zYNWlEPTB;MUCuNlU3PSEQvF2= M4frR3NCVkeHUh?=
ETK-1 NVWzO|hjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTFyLk[yN{DPxE1? NIO2XYtUSU6JRWK=
RCC10RGB M4L6bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoeyTWM2OD1zMD65OlEh|ryP NUTOfGRLW0GQR1XS
KNS-42 M3jreGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXMN4p5UUN3ME2xNU44OjV3IN88US=> MmTjV2FPT0WU
LB771-HNC NVXBOWIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfvTWM2OD1zMj6xO|EzKM7:TR?= NET3V5pUSU6JRWK=
SR M3;ZWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jRPGlEPTB;MUKuNlA3PCEQvF2= MnK5V2FPT0WU
NCI-H1355 MmD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TpZmlEPTB;MUKuPFk5PSEQvF2= MnPQV2FPT0WU
ES6 M37YPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTF|LkC3PEDPxE1? NUC4bpBxW0GQR1XS
SK-NEP-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPxR|hKSzVyPUGzMlI2PzdizszN NVLsZWp[W0GQR1XS
D-392MG MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDQTWM2OD1zMz62OFI5KM7:TR?= MXHTRW5ITVJ?
NB7 NFPjVJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LMdmlEPTB;MUSuNlM4PCEQvF2= NVrjZY06W0GQR1XS
SK-LMS-1 NInCZ4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLLV2t5UUN3ME2xOE42OTR3IN88US=> NIH4RWNUSU6JRWK=
SK-UT-1 MkDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTF2Lke4PFkh|ryP NILKO4hUSU6JRWK=
CA46 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTyTWM2OD1zNT6wOVg3KM7:TR?= NFr3R5RUSU6JRWK=
IST-SL2 Mor2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\sTWM2OD1zNT6xPVAyKM7:TR?= M4LjXXNCVkeHUh?=
BC-1 MkHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nxfGlEPTB;MUWuN|MyPCEQvF2= NGm2fFhUSU6JRWK=
LS-123 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4THUGlEPTB;MUWuPFE4OyEQvF2= MUHTRW5ITVJ?
Ramos-2G6-4C10 NEnnS|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;DOndJUUN3ME2xOk4xQTJ2IN88US=> Mlu3V2FPT0WU
MZ1-PC NEDSbmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTF4LkezNVMh|ryP MnziV2FPT0WU
LB647-SCLC M2L1Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfLV5ZlUUN3ME2xOk46Ozd{IN88US=> NXPOcGM4W0GQR1XS
NCI-H1694 M3\ERmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLrSYNKSzVyPUG3MlE2OjlizszN MkXWV2FPT0WU
NCI-H322M NEDENZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLMTplrUUN3ME2xO{41OzZ4IN88US=> MnHGV2FPT0WU
ES7 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjpNY1KSzVyPUG4MlM6OTRizszN M1nJ[XNCVkeHUh?=
LC-2-ad MlzBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XOOGlEPTB;MUiuOFM5PiEQvF2= M2XhXXNCVkeHUh?=
SF268 M2\sZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\kTWM2OD1zOD63OFA6KM7:TR?= NITzWpNUSU6JRWK=
RPMI-8402 MmGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPMXlNKSzVyPUG5MlA4PDJizszN NVq2SIs4W0GQR1XS
HCE-T M2C2fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HmRWlEPTB;MkCuNlM1PCEQvF2= NFn5R|NUSU6JRWK=
A101D Ml63S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTJyLki1PFch|ryP NHziOphUSU6JRWK=
MRK-nu-1 NX70dJB3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO0UYNLUUN3ME2yNE46OTNizszN MUDTRW5ITVJ?
LXF-289 M173[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJzLkCzPEDPxE1? MUHTRW5ITVJ?
NALM-6 MlXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTJzLkG5Olch|ryP NHzzNZdUSU6JRWK=
DOHH-2 MnnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jZOmlEPTB;MkGuOFgyOyEQvF2= M2PDVXNCVkeHUh?=
EW-16 NVXx[2FVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;JcmlEPTB;MkKuNVQxOiEQvF2= MnTxV2FPT0WU
A4-Fuk M170NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVH4R3VDUUN3ME2yNk4zOTR7IN88US=> NXXhTJFYW0GQR1XS
HD-MY-Z MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvp[25YUUN3ME2yNk4{QTZ3IN88US=> NEL5UFBUSU6JRWK=
SKM-1 NHf0SXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrFOpp2UUN3ME2yNk44OzVzIN88US=> NX3SRYd2W0GQR1XS
DMS-153 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTJ|LkSyNFQh|ryP NYfKZmFmW0GQR1XS
LB373-MEL-D MnTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPtWm9KSzVyPUKzMlU1PTJizszN NI\3dFFUSU6JRWK=
LP-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;pTWM2OD1{Mz64NFk4KM7:TR?= MVLTRW5ITVJ?
GI-ME-N M33OOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7ZTWM2OD1{ND6yPVIh|ryP NYOwfJJWW0GQR1XS
MPP-89 M2\P[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTJ3LkKwN|Yh|ryP MVjTRW5ITVJ?
U-698-M NEP2TI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXoTWM2OD1{NT6yOVA{KM7:TR?= M1jIPXNCVkeHUh?=
HC-1 NYG2TmttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWSxSJE6UUN3ME2yOU43PDF6IN88US=> MofsV2FPT0WU
HCC2157 NV\UZVN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTJ3Lk[3N{DPxE1? MWTTRW5ITVJ?
MOLT-4 M1jSbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S0W2lEPTB;Mk[uNlc{KM7:TR?= MkPtV2FPT0WU
LS-411N NXPJO2tZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zGdGlEPTB;Mk[uN|M3QSEQvF2= MVfTRW5ITVJ?
Becker NGq2coVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7wfVZ5UUN3ME2yOk42OThzIN88US=> MYrTRW5ITVJ?
NCI-H23 M2m5O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmO0TWM2OD1{Nj63OVc2KM7:TR?= NIDmXHVUSU6JRWK=
IST-SL1 NFjSV|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzsZWFPUUN3ME2yO{4{QDZ5IN88US=> NYP5fmNKW0GQR1XS
MZ2-MEL NULyR4dZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7TNXlQUUN3ME2yO{41PTZ4IN88US=> NGf5XW9USU6JRWK=
RKO M4XWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlO1TWM2OD1{OD6xOFQ3KM7:TR?= M{TMSXNCVkeHUh?=
TE-441-T NF3pPVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1flZWlEPTB;MkiuO|g6KM7:TR?= NUP6SldPW0GQR1XS
EW-24 M4PFSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTJ7LkGyOVkh|ryP NVXOWo4{W0GQR1XS
no-10 NIrreWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TQTWlEPTB;MkmuNVY{OSEQvF2= NGjRRXhUSU6JRWK=
D-542MG NH64eJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLJTWM2OD1{OT65NlIyKM7:TR?= MmjEV2FPT0WU
ST486 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nWPGlEPTB;M{CuOlQ2OSEQvF2= M1HsS3NCVkeHUh?=
KURAMOCHI MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTNyLkiwOVch|ryP NUD1UGFvW0GQR1XS
ES8 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTxTWM2OD1|MT61PVczKM7:TR?= NVjF[GNXW0GQR1XS
BL-41 Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvsVVRQUUN3ME2zNk4yODV2IN88US=> NGnqe|BUSU6JRWK=
NB6 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUL0TXBPUUN3ME2zNk4{QDV3IN88US=> M4jrS3NCVkeHUh?=
NCI-H1304 MnrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTN{LkS5Olch|ryP NFXNfZBUSU6JRWK=
MS-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HHU2lEPTB;M{KuO|c2OSEQvF2= NVLreWdiW0GQR1XS
MFH-ino MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[4TWM2OD1|ND6zNlI1KM7:TR?= MUDTRW5ITVJ?
NOS-1 NYPLS3lnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnFXFBzUUN3ME2zOE43PzR6IN88US=> MlXXV2FPT0WU
HUTU-80 NXTRbXFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\2THFsUUN3ME2zOU4{PjZ5IN88US=> NH[5WWRUSU6JRWK=
EB2 MkSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;LV2l1UUN3ME2zOk43OTh7IN88US=> M13peHNCVkeHUh?=
L-540 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTN5LkKzNFgh|ryP M3TFUHNCVkeHUh?=
NCI-H747 NXrST4Z6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTN6Lki4OFYh|ryP NWni[FQ3W0GQR1XS
NCI-H446 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;YPYFKSzVyPUO5Mlk3PTFizszN NFTxeJNUSU6JRWK=
MOLT-16 MlHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGT6eFdKSzVyPUSyMlQyPSEQvF2= MknLV2FPT0WU
BC-3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;oU|hMUUN3ME20OU41QDl4IN88US=> NGq2b3RUSU6JRWK=
SJSA-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzoTWM2OD12NT61OFc1KM7:TR?= NHfrZVNUSU6JRWK=
BB65-RCC NGDwPVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTR3Lk[2OkDPxE1? M1nKfHNCVkeHUh?=
SNB75 M{jhbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnpTWM2OD12Nj6wNVgh|ryP NXLWZ4ZQW0GQR1XS

... 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]

Protocol

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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
  • Formulation: Formulated in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10)
  • 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

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 (g) = Concentration (mol/L) × Volume (L) × 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03523585 Recruiting Breast Cancer Daiichi Sankyo Inc.|Daiichi Sankyo Co. Ltd. August 1 2018 Phase 3
NCT03500380 Recruiting Breast Neoplasms|Breast Diseases|Capecitabine|HER2-positive Breast Cancer|HER2 Positive Breast Carcinoma RemeGen April 2018 Phase 2
NCT03080805 Recruiting HER2 Positive Metastatic Breast Cancer Jiangsu HengRui Medicine Co. Ltd. May 3 2017 Phase 3
NCT03084939 Recruiting Breast Cancer Hoffmann-La Roche April 24 2017 Phase 3
NCT03085368 Recruiting HER2-positive Breast Cancer Peking Union Medical College Hospital|EddingPharm Oncology Co. LTD. March 1 2017 Phase 2|Phase 3
NCT03052634 Recruiting Advanced Breast Cancer RemeGen November 2016 Phase 1|Phase 2

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 Products4

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