CYC116

Catalog No.S1171

For research use only.

CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki 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.

CYC116 Chemical Structure

CAS No. 693228-63-6

Selleck's CYC116 has been cited by 7 Publications

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Biological Activity

Description CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki 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.
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)
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
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.

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.

30 mg/mL

Chemical Information

Molecular Weight 368.46
Formula

C18H20N6OS

CAS No. 693228-63-6
Storage 3 years -20°C powder
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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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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