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Chemical Structure| 1158838-45-9 Chemical Structure| 1158838-45-9

Structure of TCS7010
CAS No.: 1158838-45-9

Chemical Structure| 1158838-45-9

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Aurora an inhibitor I is a potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold selective for Aurora A than Aurora B.

Synonyms: Aurora A Inhibitor I

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Product Details of TCS7010

CAS No. :1158838-45-9
Formula : C31H31ClFN7O2
M.W : 588.08
SMILES Code : CCN1CCN(CC1)C(=O)CC1=CC=C(NC2=NC(NC3=CC=C(C=C3)C(=O)NC3=C(Cl)C=CC=C3)=C(F)C=N2)C=C1
Synonyms :
Aurora A Inhibitor I
MDL No. :MFCD16495816
InChI Key :AKSIZPIFQAYJGF-UHFFFAOYSA-N
Pubchem ID :44139710

Safety of TCS7010

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P305+P351+P338-P280

Related Pathways of TCS7010

epigenetics
DNA

Isoform Comparison

Biological Activity

Target
  • Aurora A

    Aurora A, IC50:3.4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
NCI-H82 cells 1.0 μM 24 hours To evaluate the effect of the compound on cMYC and MYCN protein levels, results showed that compound 13 significantly reduced cMYC and MYCN levels at 1.0 μM concentration. PMC8279414
SK-N-BE(2) cells 1.0 μM 24 hours To evaluate the effect of the compound on cMYC and MYCN protein levels, results showed that compound 13 significantly reduced cMYC and MYCN levels at 1.0 μM concentration. PMC8279414
A673 cells 2 μM 72 h To screen compounds with anticancer activity, TCS7010 exhibited significant anticancer activity. PMC10825207

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Athymic nude (nu/nu) mice NCI-H446 xenograft model Intravenous injection 50 mg/kg 5-on-2-off dosing schedule for two consecutive weeks To evaluate the in vivo antitumor efficacy of compound 13, results showed that at a dose of 50 mg/kg, tumor growth inhibition exceeded 90%. PMC8279414
Nude mice A673 xenograft model Intraperitoneal injection 40 mg/kg/d Once daily for 14 days TCS7010 significantly inhibited ES growth in vivo. PMC10825207

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.50mL

1.70mL

0.85mL

17.00mL

3.40mL

1.70mL

References

 

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