For research use only.

Catalog No.S1171

6 publications

CYC116 Chemical Structure

CAS No. 693228-63-6

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.

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10mM (1mL in DMSO) USD 160 In stock
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Selleck's CYC116 has been cited by 6 publications

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  • Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of CYC116.



    CYC116 purchased from Selleck.

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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.
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)
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 NGTj[HdEgXSxdH;4bYNqfHliYYPzZZk> MYG5OkBp NF\yN5dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 Ml\YNlA1PjJ{NkO=
MIAPaCa2 cells MlrHR5l1d3SxeHnjbZR6KGG|c3H5 NVrMU3VlQTZiaB?= MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 NUPHNVZxOjB2NkKyOlM>
HT-29 cells M4DSb2N6fG:2b4jpZ4l1gSCjc4PhfS=> NHnIUJY6PiCq MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 M3SwfVIxPDZ{Mk[z
MCF7 cells MoO0R5l1d3SxeHnjbZR6KGG|c3H5 M3S0UVk3KGh? MoLIR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 M{\JWVIxPDZ{Mk[z
HeLa cells M1;VXmN6fG:2b4jpZ4l1gSCjc4PhfS=> NWS1WWJ6QTZiaB?= M2TtW2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JG1VXCCjc4PhfS=> NEDwV2szODR4MkK2Ny=>
COLO205 cells Mof5R5l1d3SxeHnjbZR6KGG|c3H5 NX[wTGc3QTZiaB?= M1\lemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNQVE9{MEWgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>? NULHb3M5OjB2NkKyOlM>
HCT116 cells M3rJXGN6fG:2b4jpZ4l1gSCjc4PhfS=> NVnWO4xWQTZiaB?= NWXlXmo5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDl4IHjyd{BjgSCPVGSgZZN{[Xl? NWXyWYZ4OjB2NkKyOlM>
K562 cells NV7STo1QS3m2b4TvfIlkcXS7IHHzd4F6 NFvvdFU6PiCq Mnj3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 NFfocpozODR4MkK2Ny=>
CCRF-CEM cells MmPNR5l1d3SxeHnjbZR6KGG|c3H5 MkHmPVYhcA>? MmrCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2NTTi2FRV2gZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>? NYXr[ZI5OjB2NkKyOlM>
MV4-11 cells M3zURWN6fG:2b4jpZ4l1gSCjc4PhfS=> NF;aOWc6PiCq M{\XV2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1XPC1zMTDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 MknWNlA1PjJ{NkO=
HL60 cells Ml;DR5l1d3SxeHnjbZR6KGG|c3H5 NXnBOItkQTZiaB?= Ml3GR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 MXGyNFQ3OjJ4Mx?=
NCI-H460 cells MlLER5l1d3SxeHnjbZR6KGG|c3H5 M{[zclk3KGh? NHXVUIZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSES2NEBk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7 M2TLOVIxPDZ{Mk[z
MESSA cells M1LFUWN6fG:2b4jpZ4l1gSCjc4PhfS=> M2n5XFk3KGh? M{nCfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1GW1ODIHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> NFnaToIzODR4MkK2Ny=>
U2OS cells MV7GeY5kfGmxbjDhd5NigQ>? NYj0[Y06OC5yNz2xNEB2VQ>? MYSyJIg> MmL1TY5pcWKrdHnvckBw\iCDdYLvdoEhc2mwYYPlJIlvKG6xY3;kZZpwdGVvc4nuZ4hzd26renXkJIh2dWGwIGWyU3Mh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIHjpd5RwdmViSEOgd4VzcW6nLUGwJJBpd3OyaH;yfYxifGmxbjDheEAxNjB5IITvJFExKHWPIHHmeIVzKDJiaILzJIludXWwb3\seY9z\XOlZX7j[UBucWO{b4Pjc5B6 MljvNlA1PjJ{NkO=
A549 cells MVLGeY5kfGmxbjDhd5NigQ>? NYX4XVBNOC53LUKg{txO MnTqO{Bp NHe1VlJE\WyuIHP5Z4xmKGG{cnXzeEBqdiCjc4nuZ4hzd26xdYOgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25ib3[gZ5lkdGmwIFKxMY5m\2G2aY\lJJRmfHKjcHzvbYQh[2WubIOgZZQhTzFicHjhd4Uh[XRiMD61JJRwKDJidV2gZYZ1\XJiNzDodpMh[nliRlHDV{BidmGueYPpdy=> NH2xZ4MzODR4MkK2Ny=>
SW620 cells NEXMemFHfW6ldHnvckBie3OjeR?= MonONUDPxE1? NXrQZWR3PDhiaB?= NHvhUFFG\m[nY4Sgc44hdWm2b4TpZ{BqdmSneDDpckBpfW2jbjDTW|YzOCClZXzsd{Bie3Onc4Pl[EBieyCjcIDlZZJidmOnIH;mJJBwdHmybH;p[EBk\WyuczDheEAyKHWPIHHmeIVzKDR6IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJGZCS1NiYX7hcJl{cXN? MmjENlA1PjJ{NkO=
HeLa cells MoDmSpVv[3Srb36gZZN{[Xl? NXTpU3BbOS5{NTFOwG0> NUToe3dNPyCq MUTJcohq[mm2aX;uJI9nKEG3cn;yZUBscW6jc3WgbY4hcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyClb33wcIV1\SCrbnjpZol1cW:wIH;mJIhqe3SxbnWgTFMheGixc4Doc5J6dGG2aX;uJIF1KDFwMkWgeW0h[W[2ZYKgO{BpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MYSyNFQ3OjJ4Mx?=
A549 cells MV7GeY5kfGmxbjDhd5NigQ>? MYK3JIg> NIrpUJVKdmirYnn0bY9vKG:oIFH1do9z[SCtaX7hd4UhcW5iaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDjc45k\W62cnH0bY9vKHKncYXpdoVlKG[xcjDoZYxnNW2jeHntZYwhcW6qaXLpeIlwdiCxZjDobZN1d26nIFizJJNmemmwZT2xNEBxcG:|cHjvdplt[XSrb36gZYZ1\XJiNzDodpMhcW2vdX7v[ox2d3Knc3PlcoNmKG2rY4Lvd4NweHl? MY[yNFQ3OjJ4Mx?=
BxPC3 cells NHfnOXVEgXSxdH;4bYNqfHliYYPzZZk> NVi3W|l[QTZiaB?= NFHaZXVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDgFCFMzDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 NFzIVnMzODR4MkK2Ny=>
HUPT4 cells M4nxbWN6fG:2b4jpZ4l1gSCjc4PhfS=> NFnlVnQ6PiCq NGTm[oZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXVCWNDDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 NGSydYIzODR4MkK2Ny=>
Saos2 cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= MXG5OkBp NV;5U5dvS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW2Gxc{KgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>? MYqyNFQ3OjJ4Mx?=

... 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]


Kinase Assay:[1]
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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:


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  • 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:


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  • 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


CAS No. 693228-63-6
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(SC(=N1)N)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCOCC4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID