Lapatinib - Small Molecule (ID:10051-999)

HMS LINCS ID: 10051-999
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: 2016-05-06

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
20155
Lapatinib KINOMEscan-2
 KINOMEscan
20266
Multiplexed imaging of protein levels and protein phosphorylation states in the MCF 10A breast cell line treated with nine kinase inhibitors
 Microscopy/Imaging
20267
Highly-multiplexed imaging by Cyclic Immunofluorescence (CycIF) of protein levels and protein phosphorylation states in the MCF 10A breast cell line treated with EGF or four kinase inhibitors
 Microscopy/Imaging
20268
Growth rate-corrected (GR) dose-response metrics across a panel of 71 breast cancer cell lines treated with a library of small molecule and antibody perturbagens. Dataset 1 of 4: Relative cell counts and normalized growth rate inhibition values across technical replicates.
 Analysis
20269
Growth rate-corrected (GR) dose-response metrics across a panel of 71 breast cancer cell lines treated with a library of small molecule and antibody perturbagens. Dataset 2 of 4: Calculated dose-response metrics.
Analysis
20270
Growth rate-corrected (GR) dose-response metric signatures across a panel of 71 breast cancer cell lines treated with a library of small molecule and antibody perturbagens. Dataset 3 of 4: Median, upper quartile, and lower quartile GR metrics per perturbagen.
Analysis

Batch Information:

HMS LINCS Batch ID Provider Provider Batch ID
10051-999-3
10051-999-6
10051-999-7 LC Laboratories