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Chemical Structure| 630124-46-8 Chemical Structure| 630124-46-8

Structure of AST 487
CAS No.: 630124-46-8

Chemical Structure| 630124-46-8

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AST-487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM. AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM.

Synonyms: NVP-AST 487

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Product Details of AST 487

CAS No. :630124-46-8
Formula : C26H30F3N7O2
M.W : 529.56
SMILES Code : O=C(NC1=CC=C(OC2=NC=NC(NC)=C2)C=C1)NC3=CC=C(CN4CCN(CC)CC4)C(C(F)(F)F)=C3
Synonyms :
NVP-AST 487
MDL No. :MFCD11983171
InChI Key :ODPGGGTTYSGTGO-UHFFFAOYSA-N
Pubchem ID :11409972

Safety of AST 487

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

Related Pathways of AST 487

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MZ-CRC-1 cells 5 nM to 100 nM 24 hours Inhibited RET phosphorylation, profoundly suppressed mTOR signaling, leading to growth inhibition Endocr Relat Cancer. 2013 Aug 21;20(5):659-67.
TPC-1 cells 5 nM to 100 nM 24 hours Inhibited RET phosphorylation, profoundly suppressed mTOR signaling, leading to growth inhibition Endocr Relat Cancer. 2013 Aug 21;20(5):659-67.
TT cells 5 nM to 100 nM 24 hours Inhibited RET phosphorylation, profoundly suppressed mTOR signaling, leading to growth inhibition Endocr Relat Cancer. 2013 Aug 21;20(5):659-67.
Primary hippocampal neurons 5 µM 6 hours Inhibits Ret autophosphorylation and activation of downstream effectors, markedly inhibits expression of both GDNF and GFRα1 Front Cell Neurosci. 2019 Aug 13;13:351.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Tg-RET/PTC3 transgenic mice Oral gavage 50 mg/kg 5 days a week for 2 weeks Suppressed thyroid cell proliferation and reduced mTOR signaling activity Endocr Relat Cancer. 2013 Aug 21;20(5):659-67.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.44mL

1.89mL

0.94mL

18.88mL

3.78mL

1.89mL

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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