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Chemical Structure| 1095382-05-0 Chemical Structure| 1095382-05-0

Structure of CCT 137690
CAS No.: 1095382-05-0

Chemical Structure| 1095382-05-0

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CCT 137690 is an effective, orally active aurora kinase inhibitor with IC50 values of 15, 25, and 19 nM for aurora kinases A, B, and C, respectively.

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Product Details of CCT 137690

CAS No. :1095382-05-0
Formula : C26H31BrN8O
M.W : 551.48
SMILES Code : CC1=CC(CN2CCN(C3=C4C(NC(C5=CC=C(N6CCN(C)CC6)C=C5)=N4)=NC=C3Br)CC2)=NO1
MDL No. :MFCD18206879
InChI Key :GFLQCBTXTRCREJ-UHFFFAOYSA-N
Pubchem ID :25154041

Safety of CCT 137690

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of CCT 137690

epigenetics
DNA

Isoform Comparison

Biological Activity

Target
  • Aurora A

    Aurora A, IC50:15 nM

  • Aurora B

    Aurora B, IC50:25 nM

  • Aurora C

    Aurora C, IC50:19 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HT1080 cells 5 μM 24 h To detect DCN release induced by CCT137690 Autophagy. 2022 Sep;18(9):2036-2049.
SW48 cells 157 nM 48 h To evaluate the inhibitory effect of CCT137690 on the proliferation of SW48 cells, results showed that CCT137690 significantly inhibited the proliferation of SW48 cells. J Exp Clin Cancer Res. 2014 Jan 29;33(1):13.
SW620 cells 430 nM 48 h To evaluate the inhibitory effect of CCT137690 on the proliferation of SW620 cells, results showed that CCT137690 significantly inhibited the proliferation of SW620 cells. J Exp Clin Cancer Res. 2014 Jan 29;33(1):13.
HCT116 cells 0.5 or 1 μM 24 h Induced polyploidy and apoptosis Mol Cancer Ther. 2011 Nov;10(11):2115-23.
HeLa cells 0.5 μM 24 h Inhibited Aurora A and B activity Mol Cancer Ther. 2011 Nov;10(11):2115-23.
Lepto cells 100 nM 24 h To evaluate the effect of CCT137690 on Lepto cell apoptosis, results showed that CCT137690 significantly induced cell apoptosis. Cancer Res. 2021 Sep 15;81(18):4723-4735.
HCT116 cells 0.5 μM, 1 μM 24 h Induced polyploidy and apoptosis Mol Cancer Ther. 2011 Nov;10(11):2115-23.
HeLa cells 0.5 μM 24 h Induced multipolar spindle formation and chromosome misalignment Mol Cancer Ther. 2011 Nov;10(11):2115-23.
KELLY cells 0.33 μM 6 h, 24 h Inhibited MYCN protein expression and GSK3β phosphorylation Mol Cancer Ther. 2011 Nov;10(11):2115-23.
Lepto cells 100 nM 72 h To evaluate the effect of CCT137690 on Lepto cell viability, results showed that CCT137690 significantly inhibited cell viability. Cancer Res. 2021 Sep 15;81(18):4723-4735.
M1 macrophages 1.25 μM 24 h AURKA inhibitor CCT137690 restored the sensitivity of M1 cells to TAK1 inhibitor-induced cell death. Cancer Immunol Immunother. 2020 Nov;69(11):2193-2207.
M2 macrophages 1.25 μM 24 h AURKA inhibitor CCT137690 had no significant effect on M2 cells' sensitivity to TAK1 inhibitor-induced cell death. Cancer Immunol Immunother. 2020 Nov;69(11):2193-2207.
MOLM-13 cells 0.023 μM 72 h To evaluate the inhibitory effect of CCT137690 on the viability of FLT3-ITD+ AML cell line MOLM-13. Results showed that CCT137690 effectively inhibited the growth of MOLM-13 cells. Leukemia. 2012 Jul;26(7):1462-70.
MV4-11 cells 0.062 μM 72 h To evaluate the inhibitory effect of CCT137690 on the viability of FLT3-ITD+ AML cell line MV4-11. Results showed that CCT137690 effectively inhibited the growth of MV4-11 cells. Leukemia. 2012 Jul;26(7):1462-70.
MOLM-13-RES cells 0.08 μM 72 h To evaluate the inhibitory effect of CCT137690 on the viability of selective FLT3 inhibitor-resistant MOLM-13-RES cells. Results showed that CCT137690 effectively inhibited the growth of MOLM-13-RES cells. Leukemia. 2012 Jul;26(7):1462-70.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice TH-MYCN transgenic mice Oral gavage 100 mg/kg Twice daily for 10 days Significantly inhibited tumor growth Mol Cancer Ther. 2011 Nov;10(11):2115-23.
NOD/SCID mice HER2+ LC xenograft models Intrathecal injection 50 mg/kg Administered on days 5, 10, and 15 To evaluate the inhibitory effect of CCT137690 combined with anti-GM-CSF neutralizing antibodies on HER2+ LC tumor growth, results showed that the combination treatment significantly inhibited tumor growth and increased survival. Cancer Res. 2021 Sep 15;81(18):4723-4735.
Mice TH-MYCN transgenic mice Oral 100 mg/kg Twice daily for 10 days Significantly inhibited tumor growth Mol Cancer Ther. 2011 Nov;10(11):2115-23.
Athymic mice MOLM-13 subcutaneous xenograft model Oral 75 mg/kg Twice daily for 5 days To evaluate the inhibitory effect of CCT137690 on the growth of FLT3-ITD+ AML xenografts in vivo. Results showed that CCT137690 significantly inhibited tumor growth, and compared to the selective FLT3 inhibitor MLN518, CCT137690 demonstrated stronger anti-tumor effects. Leukemia. 2012 Jul;26(7):1462-70.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.07mL

1.81mL

0.91mL

18.13mL

3.63mL

1.81mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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