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.

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 120 In stock
USD 370 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

1 Customer Review

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

     

     

    CYC116 purchased from Selleck.

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

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 MX;DfZRwfG:6aXPpeJkh[XO|YYm= M37xUlk3KGh? NFfWTW9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 M2HOeFIxPDZ{Mk[z
MIAPaCa2 cells MlTTR5l1d3SxeHnjbZR6KGG|c3H5 M{XrWFk3KGh? NV7t[Ik3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUmDUHHDZVIh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IF3UWEBie3OjeR?= M2j6ZVIxPDZ{Mk[z
HT-29 cells NEjVOHFEgXSxdH;4bYNqfHliYYPzZZk> NGG4NZc6PiCq M3vUe2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> M1TDeVIxPDZ{Mk[z
MCF7 cells MU\DfZRwfG:6aXPpeJkh[XO|YYm= NXLWdmpjQTZiaB?= M3LlTmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JG1VXCCjc4PhfS=> NHG0coozODR4MkK2Ny=>
HeLa cells M{[4[mN6fG:2b4jpZ4l1gSCjc4PhfS=> NIfGRlc6PiCq NYXsV3NXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6 M2jjNlIxPDZ{Mk[z
COLO205 cells M1vtbWN6fG:2b4jpZ4l1gSCjc4PhfS=> MYK5OkBp NHiwbG1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBEV0yRMkC1JINmdGy|IHHmeIVzKDl4IHjyd{BjgSCPVGSgZZN{[Xl? MXGyNFQ3OjJ4Mx?=
HCT116 cells M4XvR2N6fG:2b4jpZ4l1gSCjc4PhfS=> MYe5OkBp MoXIR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> MXeyNFQ3OjJ4Mx?=
K562 cells NGjBUVFEgXSxdH;4bYNqfHliYYPzZZk> NHzaU4g6PiCq MnrGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 NFnGNIozODR4MkK2Ny=>
CCRF-CEM cells NYLmbXp3S3m2b4TvfIlkcXS7IHHzd4F6 NFHRN5I6PiCq NIqzVoVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBES1KILVPFUUBk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7 MYWyNFQ3OjJ4Mx?=
MV4-11 cells M1TBRWN6fG:2b4jpZ4l1gSCjc4PhfS=> NGnC[4g6PiCq MmXhR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1NTFzIHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> NE\SPFQzODR4MkK2Ny=>
HL60 cells NYLUUYNJS3m2b4TvfIlkcXS7IHHzd4F6 NEjTdG86PiCq MlPOR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 MmK1NlA1PjJ{NkO=
NCI-H460 cells MXrDfZRwfG:6aXPpeJkh[XO|YYm= MVe5OkBp NXi3RppFS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVi0OlAh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IF3UWEBie3OjeR?= MYSyNFQ3OjJ4Mx?=
MESSA cells Ml\YR5l1d3SxeHnjbZR6KGG|c3H5 MUK5OkBp MV\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSXNUSSClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5 MYqyNFQ3OjJ4Mx?=
U2OS cells M{naR2Z2dmO2aX;uJIF{e2G7 NYi5eWg5OC5yNz2xNEB2VQ>? NFrPW2QzKGh? NF3MVZFKdmirYnn0bY9vKG:oIFH1do9z[SCtaX7hd4UhcW5ibn;jc4Rigm:uZT3zfY5kcHKxbnn6[YQhcHWvYX6gWVJQWyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gbIl{fG:wZTDIN{B{\XKrbnWtNVAheGixc4Doc5J6dGG2aX;uJIF1KDBwMEegeI8hOTBidV2gZYZ1\XJiMjDodpMhcW2vdX7v[ox2d3Knc3PlcoNmKG2rY4Lvd4NweHl? MUKyNFQ3OjJ4Mx?=
A549 cells NH3MdotHfW6ldHnvckBie3OjeR?= MVSwMlUuOiEQvF2= MnHZO{Bp NIrBOmNE\WyuIHP5Z4xmKGG{cnXzeEBqdiCjc4nuZ4hzd26xdYOgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25ib3[gZ5lkdGmwIFKxMY5m\2G2aY\lJJRmfHKjcHzvbYQh[2WubIOgZZQhTzFicHjhd4Uh[XRiMD61JJRwKDJidV2gZYZ1\XJiNzDodpMh[nliRlHDV{BidmGueYPpdy=> NUDjWFBsOjB2NkKyOlM>
SW620 cells NX2yWoNQTnWwY4Tpc44h[XO|YYm= NWTyVGk{OSEQvF2= MYW0PEBp NVPoWWk{TW[oZXP0JI9vKG2rdH;0bYMhcW6mZYigbY4hcHWvYX6gV3c3OjBiY3XscJMh[XO|ZYPz[YQh[XNiYYDw[YFz[W6lZTDv[kBxd2y7cHzvbYQh[2WubIOgZZQhOSC3TTDh[pRmeiB2ODDodpMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBHSUOVIHHuZYx6e2m| M{GwbVIxPDZ{Mk[z
HeLa cells NWDNSotDTnWwY4Tpc44h[XO|YYm= MYSxMlI2KM7:TR?= MnHXO{Bp MmjpTY5pcWKrdHnvckBw\iCDdYLvdoEhc2mwYYPlJIlvKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNiY3;tdIxmfGViaX7obYJqfGmxbjDv[kBpcXO2b37lJGg{KHCqb4PwbI9zgWyjdHnvckBifCBzLkK1JJVOKGGodHXyJFchcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MlTXNlA1PjJ{NkO=
A549 cells M2LPd2Z2dmO2aX;uJIF{e2G7 NF;BWIE4KGh? NHj1O41KdmirYnn0bY9vKG:oIFH1do9z[SCtaX7hd4UhcW5iaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDjc45k\W62cnH0bY9vKHKncYXpdoVlKG[xcjDoZYxnNW2jeHntZYwhcW6qaXLpeIlwdiCxZjDobZN1d26nIFizJJNmemmwZT2xNEBxcG:|cHjvdplt[XSrb36gZYZ1\XJiNzDodpMhcW2vdX7v[ox2d3Knc3PlcoNmKG2rY4Lvd4NweHl? MoC5NlA1PjJ{NkO=
BxPC3 cells NFzOR2tEgXSxdH;4bYNqfHliYYPzZZk> MofNPVYhcA>? M1vCSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJ5WEN|IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> MmC0NlA1PjJ{NkO=
HUPT4 cells NIroNI5EgXSxdH;4bYNqfHliYYPzZZk> Mkn5PVYhcA>? NUHVXHFtS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFWSVESgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KE2WVDDhd5NigQ>? M3r4VlIxPDZ{Mk[z
Saos2 cells MYfDfZRwfG:6aXPpeJkh[XO|YYm= M3\aeFk3KGh? M2HZU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNid3N{IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZk> NWD3WI52OjB2NkKyOlM>

... 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Aurora Kinase Signaling Pathway Map

Related Aurora Kinase Products

Tags: buy CYC116 | CYC116 supplier | purchase CYC116 | CYC116 cost | CYC116 manufacturer | order CYC116 | CYC116 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID