====== Lapatinib 5μM R01 exp47 ====== ==== Mechanism of Action ==== Inhibits EGFR and ErbB2 receptor tyrosine kinases * **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%Lapatinib Ditosylate%% * **Synonyms:** GW-572016 ditosylate * **CAS #:** 388082-77-7 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/9941095|9941095]] * **IUPAC:** %%N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine;4-methylbenzenesulfonic acid%% * **INCHI Name:** InChI=1S/C29H26ClFN4O4S.2C7H8O3S/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;2*1-6-2-4-7(5-3-6)11(8,9)10/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35);2*2-5H,1H3,(H,8,9,10) * **INCHI Key:** UWYXLGUQQFPJRI-UHFFFAOYSA-N * **Molecular Weight:** 925.5 * **Canonical 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 * **Isomeric SMILES:** N/A * **Molecular Formula:** C43H42ClFN4O10S3 {{:chemogenomics:structures:chem-0027.svg?nolink}} * **Supplier Name:** Selleck Chemicals * **Catalog #:** S1028 * **Lot #:** N/A * **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C29H26ClFN4O4S 581.14201; found 581.14334 * **Platform ID:** LAPATINIB-DITOSYLATE * **Min:** -5.2045; **Max:** 27.8224 {{:chemogenomics:dose_response:dr_89.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |6.4969 | | IC30 |N/A | | IC40 |N/A | | IC50 |N/A | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ ==== Screen Summary ==== * **Round**: 01 * **Dose**: 5µM * **Days of incubation**: 8 * **Doublings**: 5.2 * **Numbers of reads**: 14927766 ==== Screen Results ==== ^Sensitive/Resistant hits (FDR<0.05)^CRANKS^Score Plot^Top 30 Genes^Screen Similarity^Top 30 Sensitive GO terms^Top 30 Resistant GO terms^ |9/0|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Lapatinib_5uM_Round-1_exp47.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp47.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:F:FLVCR1|FLVCR1]]|-4.44|<0.01| |[[:human_genes:S:SLC5A3|SLC5A3]]|-4.19|<0.01| |[[:human_genes:S:SPTLC2|SPTLC2]]|-4.08|<0.01| |[[:human_genes:S:SUGT1|SUGT1]]|-3.95|0.02| |[[:human_genes:C:CEPT1|CEPT1]]|-3.65|<0.01| |[[:human_genes:S:SPTLC1|SPTLC1]]|-3.13|0.01| |[[:human_genes:F:FARSB|FARSB]]|-3.11|0.09| |[[:human_genes:G:GPR107|GPR107]]|-3.04|0.02| |[[:human_genes:H:HEPN1|HEPN1]]|-2.98|0.01| |[[:human_genes:P:PCYT1A|PCYT1A]]|-2.88|0.08| |[[:human_genes:V:VPS25|VPS25]]|-2.65|0.33| |[[:human_genes:C:CHKA|CHKA]]|-2.64|0.02| |[[:human_genes:E:EDAR|EDAR]]|-2.52|0.08| |[[:human_genes:P:PRRC1|PRRC1]]|-2.49|0.36| |[[:human_genes:C:CHGB|CHGB]]|-2.47|0.36| |[[:human_genes:S:SLC7A5|SLC7A5]]|-2.45|0.19| |[[:human_genes:L:LINC00452|LINC00452]]|-2.41|0.21| |[[:human_genes:T:TBC1D31|TBC1D31]]|-2.39|0.21| |[[:human_genes:D:DAD1|DAD1]]|-2.36|0.15| |[[:human_genes:H:HAPLN4|HAPLN4]]|-2.35|0.42| |[[:human_genes:C:C10orf76|C10orf76]]|-2.34|0.34| |[[:human_genes:A:ALG1L2|ALG1L2]]|-2.34|0.34| |[[:human_genes:R:RGS7|RGS7]]|-2.33|0.44| |[[:human_genes:W:WDR82|WDR82]]|-2.31|0.36| |[[:human_genes:U:UBA3|UBA3]]|-2.30|0.58| |[[:human_genes:E:ERCC2|ERCC2]]|-2.29|0.36| |[[:human_genes:S:SGMS1|SGMS1]]|-2.28|0.19| |[[:human_genes:L:LIN9|LIN9]]|-2.27|0.49| |[[:human_genes:P:PI4KB|PI4KB]]|-2.26|0.33| |[[:human_genes:C:CCT6A|CCT6A]]|-2.25|0.37| |[[:human_genes:G:GNAS|GNAS]]|2.19|0.34| |[[:human_genes:M:METTL1|METTL1]]|2.21|0.45| |[[:human_genes:S:SLC47A1|SLC47A1]]|2.22|0.52| |[[:human_genes:C:C1orf95|C1orf95]]|2.23|0.34| |[[:human_genes:P:PSMB3|PSMB3]]|2.23|0.52| |[[:human_genes:N:NUP155|NUP155]]|2.25|0.52| |[[:human_genes:U:U2AF2|U2AF2]]|2.28|0.47| |[[:human_genes:A:AAAS|AAAS]]|2.30|0.45| |[[:human_genes:T:TAF15|TAF15]]|2.31|0.45| |[[:human_genes:C:CEP89|CEP89]]|2.32|0.43| |[[:human_genes:T:TTK|TTK]]|2.33|0.52| |[[:human_genes:Z:ZNF114|ZNF114]]|2.35|0.45| |[[:human_genes:E:EIF3A|EIF3A]]|2.37|0.52| |[[:human_genes:R:RALGDS|RALGDS]]|2.39|0.50| |[[:human_genes:T:TRIM52|TRIM52]]|2.39|0.55| |[[:human_genes:A:ARID4B|ARID4B]]|2.41|0.34| |[[:human_genes:R:RAD51|RAD51]]|2.49|0.58| |[[:human_genes:P:POLA2|POLA2]]|2.51|0.45| |[[:human_genes:U:USP37|USP37]]|2.58|0.34| |[[:human_genes:C:CDC73|CDC73]]|2.65|0.50| |[[:human_genes:H:HK2|HK2]]|2.66|0.34| |[[:human_genes:R:RBM26|RBM26]]|2.73|0.34| |[[:human_genes:P:PSMA5|PSMA5]]|2.76|0.34| |[[:human_genes:U:UBA52|UBA52]]|2.78|0.45| |[[:human_genes:Y:YME1L1|YME1L1]]|2.78|0.35| |[[:human_genes:I:IER3IP1|IER3IP1]]|2.82|0.45| |[[:human_genes:A:ATF7IP|ATF7IP]]|2.85|0.34| |[[:human_genes:T:TRIM44|TRIM44]]|3.06|0.34| |[[:human_genes:S:SNRNP200|SNRNP200]]|3.12|0.34| |[[:human_genes:T:THAP1|THAP1]]|3.45|0.26| ^Screen^Correlation^Plot^ |[[:results:exp149|SB203580 25μM R03 exp149]]|0.083|| |[[:results:exp90|WYE-354 6μM R02 exp90]]|0.071|| |[[:results:exp164|Q15 1 to 2μM on day4 R04 exp164]]|0.069|| |[[:results:exp538|ZLN024 50μM R08 exp538]]|0.063|| |[[:results:exp422|Wiskostatin 3μM R07 exp422]]|0.06|| |[[:results:exp61|YM155 0.0002μM R01 exp61]]|0.057|| |[[:results:exp49|NFN1 0.1μM R01 exp49]]|0.054|| |[[:results:exp83|Trametinib 10μM R02 exp83]]|0.051|| |[[:results:exp461|BS-181 20μM R08 exp461]]|0.076|| |[[:results:exp169|BH1 1μM R04 exp169]]|0.057|| |[[:results:exp41|BI-2536 0.001μM R01 exp41]]|0.056|| |[[:results:exp326|CCT251545 20μM R07 exp326]]|0.054|| |[[:results:exp233|EPZ-5676 30μM R05 exp233]]|0.054|| |[[:results:exp341|BRD2 inhibitor II 20μM R07 exp341]]|0.053|| |[[:results:exp445|∆-9-Tetrahydrocannabinol 30μM R08 exp445]]|0.052|| |[[:results:exp348|Cyclosporin-A 3μM R07 exp348]]|0.051|| |[[:results:exp457|Bisphenol F 50μM R08 exp457]]|0.051|| {{:chemogenomics:comparison_plots:exp149_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp47_vs_exp90.png?nolink |}} {{:chemogenomics:comparison_plots:exp164_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp47_vs_exp538.png?nolink |}} {{:chemogenomics:comparison_plots:exp422_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp47_vs_exp61.png?nolink |}} {{:chemogenomics:comparison_plots:exp47_vs_exp49.png?nolink |}} {{:chemogenomics:comparison_plots:exp47_vs_exp83.png?nolink |}} {{:chemogenomics:comparison_plots:exp461_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp169_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp41_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp326_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp233_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp341_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp445_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp348_vs_exp47.png?nolink |}} {{:chemogenomics:comparison_plots:exp457_vs_exp47.png?nolink |}} ^GO Term^Fold Change^Genes^ |sphinganine metabolic process|636.73|SPTLC2,SPTLC1| |C-palmitoyltransferase activity|318.37|SPTLC2,SPTLC1| |positive regulation of lipophagy|318.37|SPTLC2,SPTLC1| |regulation of lipophagy|318.37|SPTLC2,SPTLC1| |CDP-choline pathway|318.37|CEPT1,PCYT1A,CHKA| |serine C-palmitoyltransferase activity|318.37|SPTLC2,SPTLC1| |sphingomyelin biosynthetic process|191.02|SPTLC2,SPTLC1,SGMS1| |sphingomyelin metabolic process|106.12|SPTLC2,SPTLC1,SGMS1| |phosphatidylcholine biosynthetic process|79.59|CEPT1,PCYT1A,CHKA| |phospholipid biosynthetic process|19.13|SPTLC2,CEPT1,SPTLC1,PCYT1A,CHKA,SGMS1,PI4KB| |phospholipid metabolic process|12.88|SPTLC2,CEPT1,SPTLC1,PCYT1A,CHKA,SGMS1,PI4KB| |organophosphate biosynthetic process|8.60|SPTLC2,CEPT1,SPTLC1,PCYT1A,CHKA,SGMS1,PI4KB| No GO term hits below threshold. (FDR <0.05)