CYC116

Catalog No.S1171

CYC116 Chemical Structure

Molecular Weight(MW): 368.46

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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In DMSO USD 160 In stock
USD 120 In stock
USD 370 In stock
USD 970 In stock
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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.
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)
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 MnTPR5l1d3SxeHnjbZR6KGG|c3H5 MWe5OkBp M2PpZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> M3:wO|IxPDZ{Mk[z
MIAPaCa2 cells MmL6R5l1d3SxeHnjbZR6KGG|c3H5 MXi5OkBp MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 NGjIXoUzODR4MkK2Ny=>
HT-29 cells NUD2[ms{S3m2b4TvfIlkcXS7IHHzd4F6 Mkm3PVYhcA>? NFTCVIpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 NGDI[2MzODR4MkK2Ny=>
MCF7 cells NFTCNFhEgXSxdH;4bYNqfHliYYPzZZk> M4X4Tlk3KGh? MknmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 MorrNlA1PjJ{NkO=
HeLa cells Mly2R5l1d3SxeHnjbZR6KGG|c3H5 NVG3bZFEQTZiaB?= Mn6yR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 Mnz1NlA1PjJ{NkO=
COLO205 cells MVfDfZRwfG:6aXPpeJkh[XO|YYm= NVOyRWg6QTZiaB?= MlrYR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR29NVzJyNTDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 MoHONlA1PjJ{NkO=
HCT116 cells MU\DfZRwfG:6aXPpeJkh[XO|YYm= NIXsO5E6PiCq MlzOR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> NILTdJkzODR4MkK2Ny=>
K562 cells MX7DfZRwfG:6aXPpeJkh[XO|YYm= NGn0Z2o6PiCq NIXweJNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> MknXNlA1PjJ{NkO=
CCRF-CEM cells NHzUPXZEgXSxdH;4bYNqfHliYYPzZZk> MU[5OkBp M1uwVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNEWkZvQ1XNJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCPVGSgZZN{[Xl? Ml3SNlA1PjJ{NkO=
MV4-11 cells NWfOb|ZnS3m2b4TvfIlkcXS7IHHzd4F6 MYC5OkBp Moe2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1NTFzIHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> Mnm1NlA1PjJ{NkO=
HL60 cells Mmq3R5l1d3SxeHnjbZR6KGG|c3H5 M1rnO|k3KGh? MkfCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 NEOyV2kzODR4MkK2Ny=>
NCI-H460 cells NVHNSY9yS3m2b4TvfIlkcXS7IHHzd4F6 MoPxPVYhcA>? NGDnR2ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSES2NEBk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7 M3\iSVIxPDZ{Mk[z
MESSA cells NYn5cZhIS3m2b4TvfIlkcXS7IHHzd4F6 M33mSlk3KGh? NYnzVVRbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUWVU1GgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>? NFf5PYIzODR4MkK2Ny=>
U2OS cells MmOwSpVv[3Srb36gZZN{[Xl? M1v4NVAvODdvMUCgeW0> MmDKNkBp NILRV3pKdmirYnn0bY9vKG:oIFH1do9z[SCtaX7hd4UhcW5ibn;jc4Rigm:uZT3zfY5kcHKxbnn6[YQhcHWvYX6gWVJQWyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gbIl{fG:wZTDIN{B{\XKrbnWtNVAheGixc4Doc5J6dGG2aX;uJIF1KDBwMEegeI8hOTBidV2gZYZ1\XJiMjDodpMhcW2vdX7v[ox2d3Knc3PlcoNmKG2rY4Lvd4NweHl? M2LRdVIxPDZ{Mk[z
A549 cells NXjT[oQyTnWwY4Tpc44h[XO|YYm= MYiwMlUuOiEQvF2= NIm3NpA4KGh? M3ric2NmdGxiY4njcIUh[XK{ZYP0JIlvKGG|eX7jbJJwdm:3czDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCxZjDjfYNtcW5iQkGtcoVo[XSrdnWgeIV1emGybH;p[EBk\WyuczDheEBIOSCyaHHz[UBifCByLkWgeI8hOiC3TTDh[pRmeiB5IHjyd{BjgSCIQVPTJIFv[Wy7c3nz M3nnflIxPDZ{Mk[z
SW620 cells M4nQZmZ2dmO2aX;uJIF{e2G7 MYOxJO69VQ>? NIXxb|k1QCCq NFXZd2RG\m[nY4Sgc44hdWm2b4TpZ{BqdmSneDDpckBpfW2jbjDTW|YzOCClZXzsd{Bie3Onc4Pl[EBieyCjcIDlZZJidmOnIH;mJJBwdHmybH;p[EBk\WyuczDheEAyKHWPIHHmeIVzKDR6IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJGZCS1NiYX7hcJl{cXN? MkezNlA1PjJ{NkO=
HeLa cells NH;GSJdHfW6ldHnvckBie3OjeR?= NWfV[mR5OS5{NTFOwG0> NEK4RpU4KGh? MYnJcohq[mm2aX;uJI9nKEG3cn;yZUBscW6jc3WgbY4hcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyClb33wcIV1\SCrbnjpZol1cW:wIH;mJIhqe3SxbnWgTFMheGixc4Doc5J6dGG2aX;uJIF1KDFwMkWgeW0h[W[2ZYKgO{BpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ Mn[1NlA1PjJ{NkO=
A549 cells NGrNfGRHfW6ldHnvckBie3OjeR?= M{LmdVchcA>? Mn;6TY5pcWKrdHnvckBw\iCDdYLvdoEhc2mwYYPlJIlvKGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiY3;uZ4VvfHKjdHnvckBz\XG3aYLl[EBnd3JiaHHs[k1u[XirbXHsJIlvcGmkaYTpc44hd2ZiaHnzeI9v\SCKMzDz[ZJqdmVvMUCgdIhwe3Cqb4L5cIF1cW:wIHHmeIVzKDdiaILzJIludXWwb3\seY9z\XOlZX7j[UBucWO{b4Pjc5B6 M2ftcVIxPDZ{Mk[z
BxPC3 cells MX7DfZRwfG:6aXPpeJkh[XO|YYm= NGTsNJk6PiCq NVnnWlk2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSniSQ{OgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>? M2PxWVIxPDZ{Mk[z
HUPT4 cells M{SxWGN6fG:2b4jpZ4l1gSCjc4PhfS=> NFPNZpQ6PiCq NGXpUYVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXVCWNDDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 NHTlSY0zODR4MkK2Ny=>
Saos2 cells NYn4OVR7S3m2b4TvfIlkcXS7IHHzd4F6 MnXhPVYhcA>? NHjVWHREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBU[W:|MjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 MVSyNFQ3OjJ4Mx?=

... 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

Kinase Assay:[1]
+ Expand

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: NCI-H460 cells are implanted intraperitoneally into the mice.
  • Formulation: CYC116 is dissolved in DMSO and then diluted in water.
  • 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 individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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 powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00560716 Terminated Solid Tumors Cyclacel Pharmaceuticals, Inc. June 2007 Phase 1

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID