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CYC116

Name: CYC116
Brand: Selleck Chemicals
SKU: S1171
Rating: 5 (7 reviews)

Catalog No.S1171

For research use only.

CYC116 is a potent inhibitor of Aurora A/B with K_i of 8.0 nM/9.2 nM, is less potent to VEGFR2 (K_i of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.

CAS No. 693228-63-6

Selleck's CYC116 has been cited by 7 Publications

1 Customer Review

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Aurora Kinase Signaling Pathway Map

Biological Activity

Description

Features

An orally bioavailable, small molecule inhibitor of Aurora kinase/VEGFR2.

Targets

Aurora A ^[1] (Cell-free assay)	Aurora B ^[1] (Cell-free assay)	VEGFR2 ^[1] (Cell-free assay)	FLT3 ^[1] (Cell-free assay)	CDK2/CyclinE ^[1] (Cell-free assay)	Click to View More Targets
8 nM(Ki)	9 nM(Ki)	44 nM(Ki)	44 nM(Ki)	0.39 μM(Ki)	Click to View More Targets

In vitro

The most Aurora-selective CYC116 shows inhibitory effect on Aurora A and B kinases 50-fold more potently than any of the CDKs assayed. ^[1] CYC116 is initially screened against a panel of human leukemia and solid tumor cell lines using an MTT antiproliferative assay. The results show that CYC116 has broad-spectrum antitumor activity and shows specific cytotoxicity against the acute myelogenous leukemia cell line MV4-11 with IC50 of 34 nM. ^[1] In addition, anti-proliferative activity of CYC116 is found to be associated with Aurora A and B modulation such as, inhibition of Aurora autophosphorylation, reduction of histone H3 phosphorylation, polyploidy, followed by cell death, resulting from a failure in cytokinesis. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

A2780 cells	M13YdmN6fG:2b4jpZ4l1gSCjc4PhfS=>		NIPI[ok6PiCq	Mni0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVI4QDBiY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JG1VXCCjc4PhfS=>	MkLVNlA1PjJ{NkO=
MIAPaCa2 cells	MojIR5l1d3SxeHnjbZR6KGG\|c3H5		NHu5WlE6PiCq	NFrSdIlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOUUGSYVPhNkBk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7	M{HKUVIxPDZ{Mk[z
HT-29 cells	NX;YeWF5S3m2b4TvfIlkcXS7IHHzd4F6		MojqPVYhcA>?	NGq4PFNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6	M4LJblIxPDZ{Mk[z
MCF7 cells	NEPBVpVEgXSxdH;4bYNqfHliYYPzZZk>		M{OweVk3KGh?	MmH3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG\|c3H5	M4LVOFIxPDZ{Mk[z
HeLa cells	NXHGOFlIS3m2b4TvfIlkcXS7IHHzd4F6		NHvlOJk6PiCq	NWXYdWc{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6	M3T1O\|IxPDZ{Mk[z
COLO205 cells	NX\5T4xvS3m2b4TvfIlkcXS7IHHzd4F6		Mn7MPVYhcA>?	Ml7pR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR29NVzJyNTDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6	NGrQeFUzODR4MkK2Ny=>
HCT116 cells	M13vWGN6fG:2b4jpZ4l1gSCjc4PhfS=>		NYPXUYo2QTZiaB?=	MknMR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk>	NVfyN4hIOjB2NkKyOlM>
K562 cells	M1fvZWN6fG:2b4jpZ4l1gSCjc4PhfS=>		MlXkPVYhcA>?	M3X1O2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JG1VXCCjc4PhfS=>	M4Ppe\|IxPDZ{Mk[z
CCRF-CEM cells	Mo[5R5l1d3SxeHnjbZR6KGG\|c3H5		NEHEVGg6PiCq	MoDUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2NTTi2FRV2gZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>?	M{flSlIxPDZ{Mk[z
MV4-11 cells	MW\DfZRwfG:6aXPpeJkh[XO\|YYm=		NVL1TJE2QTZiaB?=	NGLzUHFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOXjRvMUGgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>?	M2XF[VIxPDZ{Mk[z
HL60 cells	Mo\qR5l1d3SxeHnjbZR6KGG\|c3H5		M2q5Zlk3KGh?	MmnwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG\|c3H5	MlHHNlA1PjJ{NkO=
NCI-H460 cells	Mn7OR5l1d3SxeHnjbZR6KGG\|c3H5		M4GwV\|k3KGh?	MlHqR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUh2NkCgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>?	NFX1TVIzODR4MkK2Ny=>
MESSA cells	NXH6b\|FsS3m2b4TvfIlkcXS7IHHzd4F6		M3fPWlk3KGh?	M3PucGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1GW1ODIHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk>	MnPONlA1PjJ{NkO=
U2OS cells	MY\GeY5kfGmxbjDhd5NigQ>?	Mnz0NE4xPy1zMDD1US=>	MWqyJIg>	MkDVTY5pcWKrdHnvckBw\iCDdYLvdoEhc2mwYYPlJIlvKG6xY3;kZZpwdGVvc4nuZ4hzd26renXkJIh2dWGwIGWyU3Mh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKG:oIHjpd5RwdmViSEOgd4VzcW6nLUGwJJBpd3OyaH;yfYxifGmxbjDheEAxNjB5IITvJFExKHWPIHHmeIVzKDJiaILzJIludXWwb3\seY9z\XOlZX7j[UBucWO{b4Pjc5B6	MYmyNFQ3OjJ4Mx?=
A549 cells	NIDvNWNHfW6ldHnvckBie3OjeR?=	Ml;KNE42NTJizszN	NVvKOGFxPyCq	M3zMOmNmdGxiY4njcIUh[XK{ZYP0JIlvKGG\|eX7jbJJwdm:3czDoeY1idiCDNUS5JINmdGy\|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCxZjDjfYNtcW5iQkGtcoVo[XSrdnWgeIV1emGybH;p[EBk\WyuczDheEBIOSCyaHHz[UBifCByLkWgeI8hOiC3TTDh[pRmeiB5IHjyd{BjgSCIQVPTJIFv[Wy7c3nz	MlnPNlA1PjJ{NkO=
SW620 cells	NWe1XnM2TnWwY4Tpc44h[XO\|YYm=	M{XMUVEh\|ryP	MoP2OFghcA>?	Ml7CSYZn\WO2IH;uJI1qfG:2aXOgbY5l\XhiaX6gbJVu[W5iU2e2NlAh[2WubIOgZZN{\XO\|ZXSgZZMh[XCyZXHyZY5k\SCxZjDwc4x6eGyxaXSgZ4VtdHNiYYSgNUB2VSCjZoTldkA1QCCqcoOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDGRWNUKGGwYXz5d4l{	NEHqPIwzODR4MkK2Ny=>
HeLa cells	MWPGeY5kfGmxbjDhd5NigQ>?	MknONU4zPSEQvF2=	M2DSbVchcA>?	NUXtXINZUW6qaXLpeIlwdiCxZjDBeZJwemFia3nuZZNmKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgZ49ueGyndHWgbY5pcWKrdHnvckBw\iCqaYP0c45mKEh\|IIDoc5NxcG:{eXzheIlwdiCjdDCxMlI2KHWPIHHmeIVzKDdiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?=	NELvUWczODR4MkK2Ny=>
A549 cells	NXLrcGlbTnWwY4Tpc44h[XO\|YYm=		MYi3JIg>	MnzRTY5pcWKrdHnvckBw\iCDdYLvdoEhc2mwYYPlJIlvKGi3bXHuJGE2PDliY3XscJMh[XO\|ZYPz[YQh[XNiY3;uZ4VvfHKjdHnvckBz\XG3aYLl[EBnd3JiaHHs[k1u[XirbXHsJIlvcGmkaYTpc44hd2ZiaHnzeI9v\SCKMzDz[ZJqdmVvMUCgdIhwe3Cqb4L5cIF1cW:wIHHmeIVzKDdiaILzJIludXWwb3\seY9z\XOlZX7j[UBucWO{b4Pjc5B6	NWjpd5BLOjB2NkKyOlM>
BxPC3 cells	NXW3cmlPS3m2b4TvfIlkcXS7IHHzd4F6		MYG5OkBp	M{izWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJ5WEN\|IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk>	MlzMNlA1PjJ{NkO=
HUPT4 cells	MkGxR5l1d3SxeHnjbZR6KGG\|c3H5		MmTlPVYhcA>?	NYjT[5BnS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFWSVESgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>?	NFvaVHAzODR4MkK2Ny=>
Saos2 cells	M3uxWGN6fG:2b4jpZ4l1gSCjc4PhfS=>		MUe5OkBp	MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTZY9{OiClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG\|c3H5	M32wc\|IxPDZ{Mk[z

Click to View More Cell Line Experimental Data

In vivo

Mice bearing subcutaneous NCI-H460 xenografts are given CYC116 orally for 5 days, at dose levels of 75 and 100 mg/kg q.d. It leads to tumor growth delays of 2.3 and 5.8 days, which translated into specific growth delays of 0.32 and 0.81, respectively. ^[1]

Protocol (from reference)

Kinase Assay:^[1]	Kinase Assays: Aurora A kinase assays are performed using a 25 μL reaction volume (25 mM β-glycerophosphate, 20 mM Tris/HCl, pH 7.5, 5 mM EGTA, 1 mM DTT, 1 mM Na₃VO₄, 10 μg of kemptide (peptide substrate)). Recombinant Aurora A kinase is diluted in 20 mM Tris/HCl, pH 8, containing 0.5 mg/mL BSA, 2.5% glycerol, and 0.006% Brij-35. Reactions are started by the addition of 5 μL Mg/ATP mix (15 mM MgCl₂, 100 μM ATP, with 18.5 kBq γ-³²P-ATP per well) and incubated at 30°C for 30 minutes before termination with 25 μL of 75 mM H₃PO₄. Aurora B kinase assays are performed like Aurora A except that prior to use, Aurora B is activated in a separate reaction at 30°C for 60 minutes with inner centromere protein.
Cell Research: ^[1]	Cell lines: HeLa, MCF7, MV4-11 and A2780 cells Concentrations: 0-10 μM Incubation Time: 72 or 96 hours Method: Standard MTT assays are performed. In short, cells are seeded into 96-well plates according to doubling time and incubated overnight at 37°C. Test compounds are made up in DMSO, a 3-fold dilution series is prepared in 100 μL of cell medium, added to cells (in triplicates) and incubated for 72 or 96 hours at 37°C. MTT is made up as a stock of 5 mg/mL in cell medium, and the solution is filter-sterilized. Medium is removed from the cells followed by a wash with PBS. MTT solution is then added at 20 μL/well and incubated in the dark at 37°C for 4 hours. MTT solution is removed and cells are again washed with 200 μL of PBS. MTT dye is solubilized with 200 μL/well of DMSO by agitation. Absorbance is read at 540 nm and data analyzed using curve-fitting software to determine IC50 values.
Animal Research: ^[1]	Animal Models: NCI-H460 cells are implanted intraperitoneally into the mice. Dosages: 75 and 100 mg/kg Administration: Administered via p.o.

References

[1] Wang S, et al. J Med Chem. 2010, 53(11), 4367-4378.

Solubility (25°C)

In vitro


In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 1% DMSO+30% polyethylene glycol+1% Tween 80 For best results, use promptly after mixing. Click to purchase: Tween 80	30 mg/mL

Chemical Information

Molecular Weight	368.46
Formula	C₁₈H₂₀N₆OS
CAS No.	693228-63-6
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=C(SC(=N1)N)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCOCC4

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