1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase

CCT129202 

Cat. No.: HY-12049 Purity: >95.0%
Data Sheet SDS Handling Instructions

CCT 137690 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.

For research use only. We do not sell to patients.
CCT129202 Chemical Structure

CCT129202 Chemical Structure

CAS No. : 942947-93-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 125 In-stock
5 mg USD 114 In-stock
10 mg USD 216 In-stock
50 mg USD 624 In-stock
100 mg USD 1126 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

CCT 137690 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.

IC50 & Target

IC50: 142 nM (Aurora A), 198 nM (Aurora B), 227 nM (Aurora C)[1]

Ki: 49.8 nM (Aurora A)[1]

In Vitro

CCT129202 causes the accumulation of human tumor cells with z4N DNA content, leading to apoptosis. CCT129202 is found to induce apoptosis with GI50 values that ranges between 0.08 and 1.7 μM. CCT120202-treated human tumor cells shows a delay in mitosis, abrogation of nocodazole-induced mitotic arrest, and spindle defects. CCT129202 Causes p21Up-regulation, Rb Hypophosphorylation, and H2F-DependentTK1Down-regulation[1].

In Vivo

Growth of HCT116 xenografts in nude mice is inhibited after i.p. administration of CCT129202. p21, the cyclin-dependent kinase inhibitor, is induced by CCT129202. Up-regulation of p21 by CCT129202 in HCT116 cells led to Rb hypophosphorylation and E2F inhibition, contributing to a decrease in thymidine kinase 1 transcription[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.0120 mL 10.0600 mL 20.1199 mL
5 mM 0.4024 mL 2.0120 mL 4.0240 mL
10 mM 0.2012 mL 1.0060 mL 2.0120 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

The effects of CCT129202 on cell proliferation are analyzed with the MTT assay. Cells are plated in 96-well plates at 2,500 per well and are treated with a range of 0 to 50 μM of CCT129202 for 72 h. The absorbance is measured at 570 nm[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

CCT129202 is dissolved in DMSO[1].

Mice: For efficacy studies, human HCT116 colon carcinoma xenografts are established in female mice. CCT129202 is dissolved in DMSO and injected i.p in vehicle, which comprises 10% DMSO, 5% Tween 20, and 85% sterile saline at 0.1 mL/10 g body weight. Dosing with CCT129202 commenced when tumors are well established (f5 mm mean diameter); control animals receive an equivalent volume of vehicle. Mouse body weights and condition are monitored throughout the study. Tumors are measured thrice weekly[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

497.02

Formula

C₂₃H₂₅ClN₈OS

CAS No.

942947-93-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CCT129202
Cat. No.:
HY-12049
Quantity: