1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
  2. Aurora Kinase
    Apoptosis
  3. CCT 137690

CCT 137690 

Cat. No.: HY-10804 Purity: 99.10%
Handling Instructions

CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.

For research use only. We do not sell to patients.

CCT 137690 Chemical Structure

CCT 137690 Chemical Structure

CAS No. : 1095382-05-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 103 In-stock
Estimated Time of Arrival: December 31
5 mg USD 85 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 400 In-stock
Estimated Time of Arrival: December 31
100 mg USD 625 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.

IC50 & Target[1]

Aurora A

15 nM (IC50)

Aurora B

25 nM (IC50)

Aurora C

19 nM (IC50)

In Vitro

CCT 137690 displays antiproliferative activity in a range of human tumor cell lines, including SW620 colon carcinoma (GI50=0.30 μM) and A2780 ovarian cancer cell line (GI50=0.14 μM). CCT 137690 inhibits in vitro phosphorylation of histone H3. CCT 137690 is a moderate inhibitor of the hERG ion-channel (IC50=3.0 μM)[1]. CCT137690 efficiently inhibits histone H3 and TACC3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells. Continuous exposure of tumour cells to the inhibitor causes multipolar spindle formation, chromosome misalignment, polyploidy and apoptosis[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CCT 137690 slows the growth of the SW620 xenografts with no observed toxicity[1]. CCT 137690 significantly inhibits tumour growth in a transgenic mouse model of neuroblastoma (TH-MYCN) that overexpresses MYCN protein and is predisposed to spontaneous neuroblastoma formation[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

551.48

Formula

C₂₆H₃₁BrN₈O

CAS No.

1095382-05-0

SMILES

CC1=CC(CN(CC2)CCN2C3=C4C(NC(C5=CC=C(N6CCN(C)CC6)C=C5)=N4)=NC=C3Br)=NO1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (30.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8133 mL 9.0665 mL 18.1330 mL
5 mM 0.3627 mL 1.8133 mL 3.6266 mL
10 mM 0.1813 mL 0.9067 mL 1.8133 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (3.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (3.03 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (3.03 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

Cells are plated in 96-well plates at 3,000 cells per well and are treated with a range of 0 to 25 mol/L of CCT137690 for 72 h. Cell proliferation assays are performed by colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice: Animals are randomized into two groups, group 1: treatment with 100 mg/kg CCT137690 n=4 or group 2: vehicle control n=4. Treatment is administered via oral gavage twice daily. Tumour volumes are measured at day 0, 3 (48 hours after treatment started), 7 and 10 using 1H MRI[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

CCT 137690CCT137690CCT-137690Aurora KinaseApoptosisInhibitorinhibitorinhibit

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CCT 137690
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