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Chemical Structure| 451493-31-5 Chemical Structure| 451493-31-5

Structure of AV-412 mesylate
CAS No.: 451493-31-5

Chemical Structure| 451493-31-5

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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.

Synonyms: MP412 mesylate; AV-412; MP412

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Product Details of AV-412 mesylate

CAS No. :451493-31-5
Formula : C41H44ClFN6O7S2
M.W : 851.41
SMILES Code : O=S(C1=CC=C(C)C=C1)(O)=O.C=CC(NC2=CC3=C(NC4=CC=C(F)C(Cl)=C4)N=CN=C3C=C2C#CC(N5CCN(C)CC5)(C)C)=O.O=S(C6=CC=C(C)C=C6)(O)=O
Synonyms :
MP412 mesylate; AV-412; MP412
MDL No. :MFCD16038940
InChI Key :GTWJVFFZCKODEV-UHFFFAOYSA-N
Pubchem ID :11700696

Safety of AV-412 mesylate

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

Related Pathways of AV-412 mesylate

RTK
JAK-STAT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
T-47D cells 0.3 µM 2 h inhibition of ErbB2 autophosphorylation Cancer Sci. 2007 Dec;98(12):1977-84
A431 cells 43 nM 2 h inhibition of EGFR autophosphorylation Cancer Sci. 2007 Dec;98(12):1977-84
NCI-H1975 cells 0.1 μM 2 h Inhibited EGFR autophosphorylation and downstream signaling Cancer Sci. 2009 Aug;100(8):1526-31
NCI-H1781 cells 0.1 μM 3 h Inhibited phosphorylation of EGFR, ErbB2, and ErbB3 and downstream signaling Cancer Sci. 2009 Aug;100(8):1526-31

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nu/nu mice A431 and BT-474 xenograft models Oral gavage 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

1.17mL

0.23mL

0.12mL

5.87mL

1.17mL

0.59mL

11.75mL

2.35mL

1.17mL

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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