Lapatinib - Small Molecule (ID:10051-104)

HMS LINCS ID: 10051-104
Name: Lapatinib
Alternative Names: GW-572016; Tykerb
LINCS ID: LSM-1051
PubChem CID: 208908
ChEBI ID:
ChEMBL ID: 554
Molecular Mass: 580.13
InChi: InChI=1S/C29H26ClFN4O4S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35)
InChi Key: BCFGMOOMADDAQU-UHFFFAOYSA-N
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
Relevant Citations:
Comments:
Date Publicly Available:
Most Recent Update: 2016-04-04

Target Affinity:

(see Study 20000)
Target Affinity Spectrum Value HUGO Gene Name
1
(Kd <100 nM)
EGFR, ERBB2, ERBB4, Tuba1a
2
(equivalent to 100 nM ≤ Kd < 1µM)
PI4KB, PIK3C2B, RAF1
3
(equivalent to 1µM ≤ Kd < 10 µM)
CDC7, CDK1, CHEK2, CHUK, CSNK1A1, DYRK1A, DYRK3, DYRK4, EEF2K, ERBB3, GRK5, HIPK2, HIPK4, IKBKB, IRAK1, MAP2K5, MAP2K7, MAP4K2, MAPK13, MATK, MINK1, MST1R, NEK4, PASK, PIK3C2G, PRKCG, PRKCI, PRKCZ, RIPK2, ROCK1, ROCK2, RPS6KB1, SLK, STK10, TAOK1, TBK1, TSSK2
10
(confirmed non-binding)
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Datasets:

HMS Dataset ID Dataset Title HMS Dataset Type
20000
Target Affinity Spectrum (TAS) vectors for compounds in the HMS LINCS small molecule library.
Analysis
20107
Lapatinib KINOMEscan
KINOMEscan
20237
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 1 of 15: Cell count and relative growth within biological replicate 1.
Microscopy/Imaging
20238
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 2 of 15: Cell count and relative growth within biological replicate 2.
Microscopy/Imaging
20239
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 3 of 15: Cell count and relative growth within biological replicate 3.
Microscopy/Imaging
20240
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 4 of 15: Mean cell count and mean growth rate across biological replicate 1.
Microscopy/Imaging
20241
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 5 of 15: Mean cell count and mean growth rate across biological replicate 2.
Microscopy/Imaging
20242
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 6 of 15: Mean cell count and mean growth rate across biological replicate 3.
Microscopy/Imaging
20243
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 7 of 15: Mean cell count and mean growth rate across all replicates.
Microscopy/Imaging
20245
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 8 of 15: Cell count and normalized growth rate inhibition values within biological replicate 1.
Microscopy/Imaging
20246
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 9 of 15: Cell count and normalized growth rate inhibition values within biological replicate 2.
Microscopy/Imaging
20247
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 10 of 15: Cell count and normalized growth rate inhibition values within biological replicate 3.
Microscopy/Imaging
20248
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 11 of 15: Mean cell count and mean normalized growth rate inhibition values across biological replicate 1.
Microscopy/Imaging
20249
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 12 of 15: Mean cell count and mean normalized growth rate inhibition values across biological replicate 2.
Microscopy/Imaging
20250
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 13 of 15: Mean cell count and mean normalized growth rate inhibition values across biological replicate 3.
Microscopy/Imaging
20251
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 14 of 15: Mean cell count and mean normalized growth rate inhibition values across all replicates.
Microscopy/Imaging
20252
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 15 of 15: Calculated dose-response metrics.
Analysis
20256
Breast Cancer Cell Density: Imaging assay of the density- and context-dependence of small molecule perturbagen response in breast cancer cell lines. Dataset 1 of 3: Cell count and normalized growth rate inhibition values.
Microscopy/Imaging
20257
Breast Cancer Cell Density: Imaging assay of the density- and context-dependence of small molecule perturbagen response in breast cancer cell lines. Dataset 2 of 3: Mean cell count and mean normalized growth rate inhibition values across all replicates.
Microscopy/Imaging
20258
Breast Cancer Cell Density: Imaging assay of the density- and context-dependence of small molecule perturbagen response in breast cancer cell lines. Dataset 3 of 3: Calculated dose-response metrics.
Analysis
20259
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (drug combination treatments). Dataset 1 of 2: Cell count and normalized growth rate inhibition values.
Microscopy/Imaging
20260
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (drug combination treatments). Dataset 2 of 2: Mean cell count and mean normalized growth rate inhibition values across technical replicates.
Microscopy/Imaging
20324
Tyrosine Kinase Inhibitor-induced cardiotoxicity in hiPSC derived cardiomyocytes - pilot dataset
RNA-Seq
20325
Tyrosine Kinase Inhibitor-induced cardiotoxicity in hiPSC derived cardiomyocytes - pilot dataset (qPCR validation)
qPCR
20349
Tyrosine Kinase Inhibitor-induced cardiotoxicity in hiPSC derived cardiomyocytes - Proteomics
Proteomics

KINOMEscan Image

Batch Information:

HMS LINCS Batch ID Provider Provider Batch ID
10051-104-1 Haoyuan chemexpress HY-999-20101220
10051-104-2 GSK/Commercial LC Laboratories BLP-106