Home Cell Cycle Aurora Kinase inhibitor - VEGFR inhibitor CYC116

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 6 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 MlXaR5l1d3SxeHnjbZR6KGG|c3H5 M2n2b|k3KGh? M2jGOGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> NEmx[IgzODR4MkK2Ny=>
MIAPaCa2 cells NG\3VIxEgXSxdH;4bYNqfHliYYPzZZk> MXO5OkBp NFLETlhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOUUGSYVPhNkBk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7 M2WwW|IxPDZ{Mk[z
HT-29 cells MoTzR5l1d3SxeHnjbZR6KGG|c3H5 Mn;HPVYhcA>? M{DYNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> Mn;1NlA1PjJ{NkO=
MCF7 cells NYHDN2ZPS3m2b4TvfIlkcXS7IHHzd4F6 NHnmS5g6PiCq NG\jNmhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> MWeyNFQ3OjJ4Mx?=
HeLa cells M3zjbWN6fG:2b4jpZ4l1gSCjc4PhfS=> MYG5OkBp MnzwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 MV[yNFQ3OjJ4Mx?=
COLO205 cells MWTDfZRwfG:6aXPpeJkh[XO|YYm= NEfoTHI6PiCq MoHNR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR29NVzJyNTDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 NEPNOFUzODR4MkK2Ny=>
HCT116 cells MlPCR5l1d3SxeHnjbZR6KGG|c3H5 NWTRPHNnQTZiaB?= NHGwc3FEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>? NWj6d3hbOjB2NkKyOlM>
K562 cells NEf1PZFEgXSxdH;4bYNqfHliYYPzZZk> NV\6fIJbQTZiaB?= NV3aWGdkS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 NXTRTYd1OjB2NkKyOlM>
CCRF-CEM cells MoXtR5l1d3SxeHnjbZR6KGG|c3H5 NIH3OmI6PiCq NIf5U5lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBES1KILVPFUUBk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7 MoHINlA1PjJ{NkO=
MV4-11 cells MV3DfZRwfG:6aXPpeJkh[XO|YYm= M3Pq[|k3KGh? NIfSd2pEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOXjRvMUGgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>? MVeyNFQ3OjJ4Mx?=
HL60 cells MlzsR5l1d3SxeHnjbZR6KGG|c3H5 MVy5OkBp NGnpTmFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> NUfYcm51OjB2NkKyOlM>
NCI-H460 cells M1nDUmN6fG:2b4jpZ4l1gSCjc4PhfS=> NHvkVpk6PiCq MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 NFmzVGczODR4MkK2Ny=>
MESSA cells NVPKVphMS3m2b4TvfIlkcXS7IHHzd4F6 NIj2bZk6PiCq NESxR|hEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTVOVQTDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 MXuyNFQ3OjJ4Mx?=
U2OS cells NH3vPFdHfW6ldHnvckBie3OjeR?= MWGwMlA4NTFyIIXN NXOyfJY5OiCq MonSTY5pcWKrdHnvckBw\iCDdYLvdoEhc2mwYYPlJIlvKG6xY3;kZZpwdGVvc4nuZ4hzd26renXkJIh2dWGwIGWyU3Mh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIHjpd5RwdmViSEOgd4VzcW6nLUGwJJBpd3OyaH;yfYxifGmxbjDheEAxNjB5IITvJFExKHWPIHHmeIVzKDJiaILzJIludXWwb3\seY9z\XOlZX7j[UBucWO{b4Pjc5B6 NHHYcJAzODR4MkK2Ny=>
A549 cells NITNXoNHfW6ldHnvckBie3OjeR?= MVWwMlUuOiEQvF2= MmLIO{Bp M2\V[mNmdGxiY4njcIUh[XK{ZYP0JIlvKGG|eX7jbJJwdm:3czDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCxZjDjfYNtcW5iQkGtcoVo[XSrdnWgeIV1emGybH;p[EBk\WyuczDheEBIOSCyaHHz[UBifCByLkWgeI8hOiC3TTDh[pRmeiB5IHjyd{BjgSCIQVPTJIFv[Wy7c3nz NHfqepYzODR4MkK2Ny=>
SW620 cells NXHOUWIyTnWwY4Tpc44h[XO|YYm= NUfHNnY3OSEQvF2= MVO0PEBp M1PoNGVn\mWldDDvckBucXSxdHnjJIlv\GW6IHnuJIh2dWGwIGPXOlIxKGOnbHzzJIF{e2W|c3XkJIF{KGGycHXhdoFv[2Vib3[gdI9tgXCub3nkJINmdGy|IHH0JFEhfU1iYX\0[ZIhPDhiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSgSmFEWyCjbnHsfZNqew>? NETBZYszODR4MkK2Ny=>
HeLa cells M{Ozc2Z2dmO2aX;uJIF{e2G7 M3nLOlEvOjVizszN MkPCO{Bp MlvGTY5pcWKrdHnvckBw\iCDdYLvdoEhc2mwYYPlJIlvKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNiY3;tdIxmfGViaX7obYJqfGmxbjDv[kBpcXO2b37lJGg{KHCqb4PwbI9zgWyjdHnvckBifCBzLkK1JJVOKGGodHXyJFchcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MViyNFQ3OjJ4Mx?=
A549 cells NHi4fFNHfW6ldHnvckBie3OjeR?= MUe3JIg> MnrvTY5pcWKrdHnvckBw\iCDdYLvdoEhc2mwYYPlJIlvKGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiY3;uZ4VvfHKjdHnvckBz\XG3aYLl[EBnd3JiaHHs[k1u[XirbXHsJIlvcGmkaYTpc44hd2ZiaHnzeI9v\SCKMzDz[ZJqdmVvMUCgdIhwe3Cqb4L5cIF1cW:wIHHmeIVzKDdiaILzJIludXWwb3\seY9z\XOlZX7j[UBucWO{b4Pjc5B6 MUKyNFQ3OjJ4Mx?=
BxPC3 cells Ml34R5l1d3SxeHnjbZR6KGG|c3H5 NH2yfmo6PiCq NXvnbYdbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSniSQ{OgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>? NF;xWFUzODR4MkK2Ny=>
HUPT4 cells MWXDfZRwfG:6aXPpeJkh[XO|YYm= NFXHWlA6PiCq MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWXBVPCClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 NHLmfYUzODR4MkK2Ny=>
Saos2 cells NITIcJNEgXSxdH;4bYNqfHliYYPzZZk> M2TZd|k3KGh? NH7DeWVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBU[W:|MjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 NVTkbWRQOjB2NkKyOlM>
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.

  • (Only for Reference)
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.
  • (Only for Reference)

Solubility (25°C)

In vitro

 DMSO 24 mg/mL warmed
(65.13 mM)
Water Insoluble
Ethanol Insoluble

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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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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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