MK-1775 0.32μM R02 exp75 [The Human Chemical-Genetic Interaction Map Project]

Inhibits Wee1, alleviates CDK inhibition

Class / Subclass 1: Cell Cycle / Kinase Inhibitor
Class / Subclass 2: Signal Transduction / Kinase Inhibitor
Class / Subclass 3: DNA Damage, Repair and Replication / Checkpoint Signaling Inhibitor

Compound References

PubChem Name: Adavosertib
Synonyms: AZD1775; MK-1775
CAS #: 955365-80-7
PubChem CID: 24856436
IUPAC: 1-[6-(2-hydroxypropan-2-yl)pyridin-2-yl]-6-[4-(4-methylpiperazin-1-yl)anilino]-2-prop-2-enylpyrazolo[3,4-d]pyrimidin-3-one
INCHI Name: InChI=1S/C27H32N8O2/c1-5-13-34-25(36)21-18-28-26(29-19-9-11-20(12-10-19)33-16-14-32(4)15-17-33)31-24(21)35(34)23-8-6-7-22(30-23)27(2,3)37/h5-12,18,37H,1,13-17H2,2-4H3,(H,28,29,31)
INCHI Key: BKWJAKQVGHWELA-UHFFFAOYSA-N
Molecular Weight: 500.6
Canonical SMILES: CC(C)(C1=NC(=CC=C1)N2C3=NC(=NC=C3C(=O)N2CC=C)NC4=CC=C(C=C4)N5CCN(CC5)C)O
Isomeric SMILES: N/A
Molecular Formula: C27H32N8O2

Compound Supplier

Supplier Name: Repare Therapeutics
Catalog #: Unknown
Lot #: N/A

Compound Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C27H32N8O2 501.2721; found 501.27254

Dose Response Curve

Platform ID: MK-1775
Min: -5.3402; Max: 90.1692

IC	Concentration (µM)
IC10	N/A
IC20	0.2773
IC30	0.3795
IC40	0.4907
IC50	0.6212
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 02
Dose: 320nM
Days of incubation: 8
Doublings: 5.9
Numbers of reads: 14663165

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
38/29	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
PRPS1	-3.80	<0.01
MKLN1	-3.54	<0.01
RNASEH2A	-3.52	<0.01
PKMYT1	-3.42	<0.01
UBE2H	-3.37	<0.01
ZNF445	-3.34	<0.01
WEE1	-3.31	0.05
MSI2	-3.08	<0.01
SMEK1	-3.01	<0.01
SPEN	-2.88	<0.01
WDR26	-2.84	0.01
PRAMEF25	-2.78	0.29
PRAMEF26	-2.77	0.29
FZR1	-2.74	<0.01
KPNA6	-2.72	0.01
LCMT1	-2.71	<0.01
ARL14EP	-2.70	<0.01
RNASEH2B	-2.68	<0.01
RIF1	-2.66	<0.01
TMEM208	-2.65	0.01
CNOT3	-2.64	0.03
YWHAE	-2.62	0.01
KPNA4	-2.61	0.01
ZNF598	-2.59	0.01
ZMYND19	-2.58	0.01
NFRKB	-2.57	0.01
IVNS1ABP	-2.55	0.01
CD52	-2.51	0.01
PPHLN1	-2.50	0.01
TRIP12	-2.49	0.01
MRPL49	2.38	0.06
FBXL12	2.41	0.03
ANP32E	2.41	0.15
FBXO42	2.42	0.03
EPC1	2.43	0.05
NGRN	2.47	0.02
LLGL1	2.51	0.02
HMGXB3	2.63	0.08
ZDHHC17	2.65	<0.01
NBEAL1	2.65	0.04
FARSA	2.68	0.12
CCNL1	2.72	<0.01
DDI2	2.78	<0.01
LRR1	2.80	0.09
PTPN2	2.81	<0.01
CHD2	2.82	<0.01
CEBPG	2.85	<0.01
EIF4G1	2.89	<0.01
PRMT3	2.96	<0.01
DCUN1D1	3.08	0.00
RFC1	3.49	0.10
FAM122A	3.60	0.00
EIF4B	3.77	0.00
CCNA2	4.00	0.00
SKP2	4.63	0.00
EIF4A1	4.65	0.00
SLFN11	5.16	0.00
CDK2	5.42	0.00
GCN1L1	6.17	0.00
EIF2AK4	6.27	0.00

Screen	Correlation	Plot
Pterostilbene 16μM R02 exp78	0.09	View
Resveratrol 16μM R03 exp147	0.079	View
Olaparib 4μM R08 exp512	0.055	View
Trimetrexate 0.03μM R08 exp535	0.052	View
3-Bromopyruvate 7μM R04 exp175	0.068	View
Diepoxybutane 3μM R07 exp354	0.056	View
Erlotinib 10μM R05 exp216	0.056	View
Hydroxyurea 100μM R07 exp329	0.053	View
FK-506 30μM R07 exp359	0.052	View

GO Term	Fold Change	Genes
cyclin A2-CDK2 complex	552.80	CDK2,CCNA2
eukaryotic translation initiation factor 4F complex	150.76	EIF4A1,EIF4B,EIF4G1
RNA cap binding complex	92.13	EIF4A1,EIF4B,EIF4G1
translation factor activity, RNA binding	27.64	GCN1,EIF4A1,EIF4B,EIF4G1
transferase complex	5.99	CDK2,SKP2,CCNA2,DCUN1D1,CCNL1,EPC1,FBXO42,FBXL12,PFKP

Last modified: 2026/01/15 21:36
by 127.0.0.1