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Chemical Structure| 451492-95-8 Chemical Structure| 451492-95-8

Structure of AV-412 free base
CAS No.: 451492-95-8

Chemical Structure| 451492-95-8

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AV-412 is a potent dual inhibitor of EGFR and ErbB2 (IC50=19 nM) tyrosine kinases, including the mutant EGFR (L858R IC50=0.51 nM, T790M IC50=0.79 nM). It inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.

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Product Details of AV-412 free base

CAS No. :451492-95-8
Formula : C27H28ClFN6O
M.W : 507.00
SMILES Code : C=CC(NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1C#CC(N4CCN(C)CC4)(C)C)=O
MDL No. :MFCD16038939
InChI Key :ZAJXXUDARPGGOC-UHFFFAOYSA-N
Pubchem ID :9806229

Safety of AV-412 free base

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

Related Pathways of AV-412 free base

RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • EGFR/ErbB1

    EGFR, IC50:0.75 nM

  • HER2/ErbB2

    ErbB2, IC50:19 nM

  • mutant EGFR

    EGFRT790M, IC50:0.79 nM

    EGFRL858R/T790M, IC50:0.51 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
T-47D cells 0.3 µM 2 h inhibition of ErbB2 autophosphorylation and downstream signaling Cancer Sci. 2007 Dec;98(12):1977-84

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nu/nu mice A431 xenograft model Oral 30 mg/kg Once daily for 14 days Complete inhibition of tumor growth Cancer Sci. 2007 Dec;98(12):1977-84
BALB/c AJcl nude mice NCI-H1650 and NCI-H1975 xenograft models Oral 150 mg/kg Once daily for 14 days MP-412 completely inhibited the tumor growth of both H1650 and H1975 xenografts Cancer Sci. 2009 Aug;100(8):1526-31

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.86mL

1.97mL

0.99mL

19.72mL

3.94mL

1.97mL

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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