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Fig. 1 · Structure
Cat. No.
A11146
CAS No.
1137868-52-0
Formula
C27H34F3N7O3
Mol. Weight
561.6

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TAK-960

Cat. No. A11146 CAS 1137868-52-0

PLK1 inhibitor

TAK-960 is a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity.

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Biological Activity

Target & Activity

Target Activity Value
PLK1 IC50 0.8 nM
PLK2 IC50 16.9 nM
PLK3 IC50 50.2 nM
FAK/PTK2 IC50 19.6 nM
MLCK/MYLK IC50 25.6 nM
FES/FPS IC50 58.2 nM

6 targets · Scroll to view more

Cellular Effect

Cell Line Activity Value Description Reference
HT-29 EC50 3 nM Antiproliferative activity against human HT-29 cells after 72 hrs by Cell Titer-Glo Assay [PMID: 23664874]

In Vitro Studies

DLD1 cultures were exposed to increasing concentrations of TAK-960 for 72 h. Colony area coverage was < 10% at concentrations greater than 20 nM. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

TAK-960 Exposure and DLD1 Colony Area

Cell-based study · DLD1 [1]

DLD1 cells were exposed to increasing concentrations of TAK-960 for 72 h, with a mock treated control. Colony area coverage was < 10% at concentrations greater than 20 nM.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Colony areacolony area coverage < 10% area coverage[1]

Literature-Reported Treatment Conditions

Treatment concentration
greater than 20 nM
Exposure duration
72 h
Method
exposed to increasing concentrations of TAK-960
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: TAK-960

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Methods > Clonogenic colony formation assay (S29, S30); Results > TAK-960 inhibits colony growth and regrowth (S60); Fig. 2 legend (S116, S118)

Colony area: Colony area; comparator: mock treated control — Methods > Clonogenic colony formation assay (S30); Results > TAK-960 inhibits colony growth and regrowth (S60)

In Vivo Studies

In mice bearing subcutaneous HeLa tumor xenografts, TAK-960 alone administered orally at 10 mg/kg yielded a tumor growth doubling time that was not significantly longer than after sham treatment. In female athymic nude (nu/nu) mice bearing CUCRC026 tumors, oral gavage at 10 mg/kg daily for at least 28 days demonstrated minor tumor regression (TGII< 0) compared with vehicle control. [2,1]

Tumor growth doubling time in HeLa xenografts

Animal study · mice bearing a subcutaneous HeLa tumor xenograft [2]

Model: mice bearing a subcutaneous HeLa tumor xenograft. Treatment: 10 mg/kg. Result: Tumor growth doubling time (TGDT) after the TAK-960 treatment alone was 8.3 ± 1.6 days and was not significantly longer than that after the sham treatment (9.1 ± 1.7 days; P = 0.33)..

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Tumor growth doubling time (TGDT)Tumor growth doubling time (TGDT) 10 mg/kg TAK-960; 0 Gy 24 hours after the oral administration: 8.3 ± 1.6 days[2]

Conditions shared by the study groups

Route
oral administration
Vehicle
0.5% (w/v) hydroxylpropyl methylcellulose solution
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
TAK-960 10 mg/kgsham treatmentTumor growth doubling time (TGDT) after the TAK-960 treatment alone was 8.3 ± 1.6 days and was not significantly longer than that after the sham treatment (9.1 ± 1.7 days; P = 0.33).[2]
TAK-960 10 mg/kg
Model: mice bearing a subcutaneous HeLa tumor xenograft
Reported limits: Not stated in the sentences used: schedule.
Methods and source locations

Compound reported in the paper: TAK-960

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Radiosensitizing effects of TAK-960 in vivo (S43, S45); Methods > Cell culture and reagents (S57); Methods > Tumor-bearing mice, TAK-960 treatment, and radiation treatment in vivo (S74); Figure 4 legend (S121)

Tumor growth doubling time (TGDT): Tumor growth doubling time (TGDT); comparator: sham treatment — Results > Radiosensitizing effects of TAK-960 in vivo (S43, S45)

TAK-960 10 mg/kg · Results > Radiosensitizing effects of TAK-960 in vivo (S43, S45)

Minor Tumor Regression in CUCRC026

Animal study · Female athymic nude (nu/nu) mice; CUCRC026 [1]

Female athymic nude (nu/nu) mice bearing CUCRC026 tumors received treatment by oral gavage at 10 mg/kg daily for at least 28 days, with a vehicle control. CUCRC026 demonstrated minor tumor regression (TGII< 0).

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Tumor Growth Inhibition Index (TGII)Reported result (CUCRC026) demonstrated minor tumor regression (TGII< 0)[1]

Conditions shared by the study groups

Route
oral gavage
Treatment course
daily; for at least 28 days
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
TAK-960 10 mg/kgvehicle control(CUCRC026) demonstrated minor tumor regression (TGII< 0)[1]
TAK-960 10 mg/kg
Model: Female athymic nude (nu/nu) mice; CUCRC026
Reported limits: Not stated in the sentences used: vehicle. Removed after verification: value.
Methods and source locations

Compound reported in the paper: TAK-960

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Methods > Patient derived xenograft models (S34, S35, S38); Results > TAK-960 is active against colorectal cancer patient derived xenograft models (S99); Fig. 5 legend (S127)

Tumor Growth Inhibition Index (TGII): Tumor Growth Inhibition Index (TGII); comparator: vehicle control — Results > TAK-960 is active against colorectal cancer patient derived xenograft models (S99); Fig. 5 legend (S127)

TAK-960 10 mg/kg · Methods > Patient derived xenograft models (S38); Results > TAK-960 is active against colorectal cancer patient derived xenograft models (S99)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 1137868-52-0
Applications PLK1 inhibitor
Formula C27H34F3N7O3
Molecular Weight 561.6
SMILES
CN1CCC(CC1)NC(=O)C2=CC(=C(C=C2F)NC3=NC=C4C(=N3)N(CC(C(=O)N4C)(F)F)C5CCCC5)OC

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Klauck PJ, Bagby SM, Capasso A, et al. Antitumor activity of the polo-like kinase inhibitor, TAK-960, against preclinical models of colorectal cancer. BMC Cancer (2018). PMID: 29402316 DOI: 10.1186/s12885-018-4036-z Source material
  2. [2] Inoue M, Yoshimura M, Kobayashi M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep (2015). PMID: 26503893 DOI: 10.1038/srep15666 Source material

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