CFI-400945 25μM R08 exp469 [The Human Chemical-Genetic Interaction Map Project]

Inhibits PLK4, blocks centriole duplication, induces mitotic defects and cell death

Class / Subclass 1: Signal Transduction / Kinase Inhibitor
Class / Subclass 2: Cell Cycle / Mitotic Inhibitor

Compound References

PubChem Name: CFI-400945 free base
Synonyms: N/A
CAS #: 1338806-73-7
PubChem CID: 58486178
IUPAC: (2'S,3R)-2'-[3-[(E)-2-[4-[[(2S,6R)-2,6-dimethylmorpholin-4-yl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]-5-methoxyspiro[1H-indole-3,1'-cyclopropane]-2-one
INCHI Name: InChI=1S/C33H34N4O3/c1-20-17-37(18-21(2)40-20)19-23-6-4-22(5-7-23)8-12-29-26-11-9-24(14-31(26)36-35-29)28-16-33(28)27-15-25(39-3)10-13-30(27)34-32(33)38/h4-15,20-21,28H,16-19H2,1-3H3,(H,34,38)(H,35,36)/b12-8+/t20-,21+,28-,33-/m0/s1
INCHI Key: DADASRPKWOGKCU-FVTQAUBDSA-N
Molecular Weight: 534.6
Canonical SMILES: CC1CN(CC(O1)C)CC2=CC=C(C=C2)C=CC3=NNC4=C3C=CC(=C4)C5CC56C7=C(C=CC(=C7)OC)NC6=O
Isomeric SMILES: C[C@@H]1CN(C[C@@H](O1)C)CC2=CC=C(C=C2)/C=C/C3=NNC4=C3C=CC(=C4)[C@@H]5C[C@]56C7=C(C=CC(=C7)OC)NC6=O
Molecular Formula: C33H34N4O3

Compound Supplier

Supplier Name: Med Chem Express
Catalog #: HY-12300
Lot #: 23771

Compound Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C33H34N4O3 535.27037; found 535.27075

Dose Response Curve

Platform ID: CFI400945
Min: -8.6037; Max: 76.6696

IC	Concentration (µM)
IC10	19.9700
IC20	24.7200
IC30	28.4900
IC40	32.0000
IC50	35.6100
IC60	39.6200
IC70	44.5100
IC80	51.3000
IC90	63.5100

Screen Summary

Round: 08
Dose: 25µM
Days of incubation: 8
Doublings: -0.4
Numbers of reads: 14411620

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
29/0	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
SCYL1	-3.97	<0.01
GPR107	-3.67	<0.01
GOLGA8H	-3.43	0.04
SLC5A3	-3.39	<0.01
OSBPL9	-3.35	<0.01
TMEM167B	-3.19	<0.01
OSBPL11	-3.07	<0.01
COG7	-3.02	<0.01
PCYT1A	-3.00	<0.01
YIPF5	-2.99	<0.01
SGMS1	-2.98	<0.01
CYB561D2	-2.94	<0.01
ATP6V0A2	-2.84	<0.01
COPZ1	-2.79	<0.01
UNC50	-2.79	<0.01
GAGE2A	-2.79	0.23
FLVCR1	-2.78	<0.01
SART1	-2.77	0.13
ARL1	-2.75	<0.01
YIPF4	-2.74	<0.01
ARID4B	-2.71	0.01
VKORC1L1	-2.63	<0.01
ZBTB7A	-2.62	0.01
COG5	-2.59	0.02
TM9SF2	-2.54	0.01
COPB2	-2.50	0.24
GOLGA6L1	-2.49	0.46
DDX3X	-2.48	0.02
PI4KB	-2.47	0.04
ZNF91	-2.47	0.02
URM1	1.98	0.32
WDR77	1.98	0.38
P2RY4	1.99	0.32
C11orf87	2.00	0.32
DSCR4	2.00	0.32
RRAGA	2.00	0.33
TBC1D16	2.06	0.33
SHISA4	2.07	0.32
CERCAM	2.08	0.26
ODC1	2.10	0.26
MEAF6	2.16	0.33
CDH22	2.17	0.29
GEMIN8	2.17	0.33
DDX55	2.20	0.26
ALG13	2.22	0.26
PHIP	2.23	0.15
LIN52	2.31	0.10
MRPS5	2.33	0.17
ENO1	2.34	0.33
PARK2	2.35	0.09
TAMM41	2.36	0.09
UQCR10	2.40	0.09
ATP5B	2.40	0.09
PAXBP1	2.49	0.09
RPE	2.57	0.09
SARS	2.81	0.39
SUPV3L1	2.84	0.09
SARS2	2.97	0.09
TRIAP1	3.07	0.09
GMPPB	3.59	0.09

Screen	Correlation	Plot
Clomiphene 4.4μM R02 exp68	0.072	View
WYE-354 6μM R02 exp90	0.07	View
Q15 1 to 2μM on day4 R04 exp164	0.062	View
Chlorpromazine 10μM R07 exp344	0.062	View
Ibrutinib 10μM R08 exp442	0.06	View
Q15 2.7μM R02 exp79	0.059	View
Monensin 0.3μM R08 exp507	0.057	View
Oligomycin-A 20μM R00 exp26	0.052	View
Thioridazine 5μM R08 exp530	0.051	View
Vemurafenib 6.6μM R08 exp434	0.051	View
BH1 1μM R04 exp169	0.08	View
BS-181 20μM R08 exp461	0.06	View
42°C R08 exp539	0.056	View

GO Term	Fold Change	Genes
COPI-coated vesicle membrane	131.50	SCYL1,COPZ1,COPB2
COPI-coated vesicle	87.67	SCYL1,COPZ1,COPB2
intra-Golgi vesicle-mediated transport	79.18	COG7,COPZ1,COG5,COPB2
retrograde vesicle-mediated transport, Golgi to endoplasmic reticulum	51.14	SCYL1,COG7,COPZ1,COPB2
Golgi organization	27.68	GOLGA8H,COG7,YIPF5,ARL1,YIPF4,COG5
Golgi vesicle transport	15.62	SCYL1,COG7,YIPF5,COPZ1,YIPF4,COG5,COPB2
Golgi apparatus subcompartment	11.80	GOLGA8H,COG7,YIPF5,SGMS1,ARL1,YIPF4,COG5
Golgi membrane	9.35	TMEM167B,COG7,SGMS1,ATP6V0A2,COPZ1,UNC50,ARL1,COG5,COPB2,PI4KB

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