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Chemical Structure| 252916-29-3 Chemical Structure| 252916-29-3

Structure of Orantinib
CAS No.: 252916-29-3

Chemical Structure| 252916-29-3

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TSU-68 is a multiple receptor tyrosine kinase inhibitor with IC50 of 2.1 μM, 8 nM and 1.2 μM for VEGF-R1, PDGF-Rβ and FGF-R1, respectively and has greatest potency against PDGFR autophosphorylation.

Synonyms: SU6668; TSU-68; NSC 702827

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Product Details of Orantinib

CAS No. :252916-29-3
Formula : C18H18N2O3
M.W : 310.35
SMILES Code : O=C(O)CCC1=C(C)NC(/C=C2C(NC3=C/2C=CC=C3)=O)=C1C
Synonyms :
SU6668; TSU-68; NSC 702827
MDL No. :MFCD09743433

Safety of Orantinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Orantinib

RTK

Isoform Comparison

Biological Activity

Target
  • PDGFRβ

    PDGFRβ, Ki:8 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human Umbilical Vein Endothelial Cells (HUVECs) 10 ng/ml 3 days To investigate the effect of SU6668 on bFGF-induced HUVEC proliferation, results showed that SU6668 significantly inhibited the mitogenic effects of both bFGF and VEGF. PMC1850845

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice RIP1Tag2 transgenic mice Oral 200 mg/kg Once daily, from 5 to 10.5 weeks of age (prevention trial), from 10 to 13.5 weeks of age (intervention trial), and from 12 to 16 weeks of age (regression trial) SU6668 was less effective in the prevention trial, but was much better in the regression trial, producing a condition of 'stable disease', reducing tumor burden and disrupting tumor vascularity. PMC154450

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.22mL

0.64mL

0.32mL

16.11mL

3.22mL

1.61mL

32.22mL

6.44mL

3.22mL

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

References

 

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