Erlotinib 10μM R05 exp216

Inhibits EGFR, also cyclin G-associated kinase (GAK)

Class / Subclass 1: Signal Transduction / Kinase Inhibitor

Compound References

PubChem Name: Erlotinib
Synonyms: CP-358774; NSC 718781; OSI-774
CAS #: 183321-74-6
PubChem CID: 176870
IUPAC: N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
INCHI Name: InChI=1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25)
INCHI Key: AAKJLRGGTJKAMG-UHFFFAOYSA-N
Molecular Weight: 393.4
Canonical SMILES: COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC
Isomeric SMILES: N/A
Molecular Formula: C22H23N3O4

Compound Supplier

Supplier Name: Cayman Chemical
Catalog #: 10483
Lot #: N/A

Compound Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C22H23N3O4 394.17613; found 394.17708

Dose Response Curve

Platform ID: Erlotinib
Min: -14.1940; Max: 21.2326

IC	Concentration (µM)
IC10	N/A
IC20	N/A
IC30	N/A
IC40	N/A
IC50	N/A
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 05
Dose: 10µM
Days of incubation: 8
Doublings: 4.1
Numbers of reads: 19100357

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
18/31	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
RSRC2	-3.58	0.02
ITPA	-3.04	<0.01
RHOA	-3.01	<0.01
CMIP	-2.88	0.02
PRR12	-2.82	0.02
ATP6V0A2	-2.81	0.04
PTEN	-2.75	0.02
EIF2A	-2.70	0.02
TCF4	-2.69	0.02
BACH2	-2.64	0.04
TRIB3	-2.64	0.04
UBE2N	-2.62	0.04
PPHLN1	-2.60	0.04
DDX6	-2.58	0.06
DOT1L	-2.58	0.04
DRG2	-2.49	0.04
UMPS	-2.48	0.50
CCDC173	-2.44	0.06
CTU1	-2.40	0.04
CNOT8	-2.38	0.05
CNOT2	-2.37	0.05
TRMT1	-2.32	0.06
RER1	-2.27	0.06
INTS12	-2.27	0.06
PRKAR1A	-2.26	0.07
CCDC101	-2.25	0.11
MAPK14	-2.23	0.08
CCM2	-2.22	0.08
FAM208A	-2.21	0.08
MOCS3	-2.20	0.12
FBXW11	2.39	0.15
PFKP	2.42	0.05
RPS12	2.43	0.08
NCLN	2.45	0.04
EIF2B1	2.49	0.02
HSPE1	2.64	0.38
PLN	2.64	0.24
PTPMT1	2.68	0.03
ANP32A	2.70	0.01
NFATC3	2.70	0.01
MBTPS2	2.74	<0.01
EIF3A	2.80	<0.01
TSC1	2.87	<0.01
RPS10	2.93	<0.01
NPRL3	3.01	<0.01
EIF4B	3.05	<0.01
NPRL2	3.13	<0.01
DDX3X	3.21	<0.01
ARID4B	3.21	<0.01
CEBPG	3.50	<0.01
DEPDC5	3.56	<0.01
NANS	3.64	<0.01
EIF3G	3.76	<0.01
EIF4A1	3.93	<0.01
CMAS	4.25	<0.01
TSC2	4.47	<0.01
SERBP1	4.99	<0.01
ATF4	5.36	<0.01
GCN1L1	7.43	<0.01
EIF2AK4	8.48	<0.01

Screen	Correlation	Plot
Temozolomide 200μM R04 exp189	0.098	View
Radicicol 0.16μM R05 exp242	0.079	View
Hippuristanol 0.12μM R08 exp488	0.074	View
LB-100 2μM R05 exp210	0.071	View
Hippuristanol 0.12μM R08 exp489 no dilution day6	0.067	View
Milciclib 2μM R08 exp502	0.063	View
Ethanol 0.01 R05 exp234	0.062	View
GSK626616 14μM R08 exp485	0.062	View
Staurosporine 0.02μM R08 exp524	0.061	View
MK2206 4μM R08 exp504	0.057	View
MK-1775 0.32μM R02 exp75	0.056	View
Rapamycin 10μM R00 exp30	0.055	View
Torin1 0.08μM R02 exp82	0.054	View
Talazoparib 0.006μM R06 exp299	0.053	View
Trimetrexate 0.03μM R08 exp535	0.053	View
Lead acetate 2000μM R08 exp497	0.051	View
LB-100 4.1μM R02 exp72	0.051	View
5-Azacytidine 2μM R07 exp330	0.075	View
EPZ-5676 30μM R05 exp233	0.066	View
Dexamethasone 0.006 to 0.015μM on day4 R07 exp352	0.06	View
Dimethyloxaloylglycine 100μM R05 exp229	0.053	View

GO Term	Fold Change	Genes
cellular response to amino acid starvation	70.51	EIF2AK4,GCN1,ATF4,DEPDC5,NPRL2,NPRL3
negative regulation of TORC1 signaling	67.36	TSC2,DEPDC5,NPRL2,NPRL3,TSC1
response to amino acid starvation	66.28	EIF2AK4,GCN1,ATF4,DEPDC5,NPRL2,NPRL3
translation initiation factor activity	58.76	EIF4A1,EIF3G,EIF4B,EIF3A,EIF2B1
translational initiation	52.60	EIF4A1,EIF3G,DDX3X,EIF4B,EIF3A,EIF2B1
negative regulation of TOR signaling	41.84	TSC2,DEPDC5,NPRL2,NPRL3,TSC1
translation factor activity, RNA binding	41.43	GCN1,EIF4A1,EIF3G,EIF4B,EIF3A,EIF2B1
translation regulator activity, nucleic acid binding	31.87	GCN1,EIF4A1,EIF3G,EIF4B,EIF3A,EIF2B1
translation regulator activity	29.29	GCN1,SERBP1,EIF4A1,EIF3G,EIF4B,EIF3A,EIF2B1
cellular response to starvation	26.15	EIF2AK4,GCN1,ATF4,TSC2,DEPDC5,NPRL2,NPRL3,TSC1
response to starvation	21.24	EIF2AK4,GCN1,ATF4,TSC2,DEPDC5,NPRL2,NPRL3,TSC1
cellular response to nutrient levels	19.13	EIF2AK4,GCN1,ATF4,TSC2,DEPDC5,NPRL2,NPRL3,TSC1
cellular response to extracellular stimulus	16.99	EIF2AK4,GCN1,ATF4,TSC2,DEPDC5,NPRL2,NPRL3,TSC1
translation	13.96	GCN1,EIF4A1,EIF3G,DDX3X,EIF4B,RPS10,EIF3A,EIF2B1,RPS12
cellular response to external stimulus	13.60	EIF2AK4,GCN1,ATF4,TSC2,DEPDC5,NPRL2,NPRL3,TSC1
peptide biosynthetic process	13.05	GCN1,EIF4A1,EIF3G,DDX3X,EIF4B,RPS10,EIF3A,EIF2B1,RPS12
peptide metabolic process	10.51	GCN1,EIF4A1,EIF3G,DDX3X,EIF4B,RPS10,EIF3A,EIF2B1,RPS12
amide biosynthetic process	9.90	GCN1,EIF4A1,EIF3G,DDX3X,EIF4B,RPS10,EIF3A,EIF2B1,RPS12
amide metabolic process	8.04	GCN1,ATF4,CMAS,EIF4A1,EIF3G,DDX3X,EIF4B,RPS10,EIF3A,EIF2B1,RPS12

Erlotinib 10μM R05 exp216

Mechanism of Action

Technical Notes

Compound References

Compound Supplier

Compound Characterization

Dose Response Curve

Screen Summary

Screen Results