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Chemical Structure| 859212-16-1 Chemical Structure| 859212-16-1

Structure of Bafetinib
CAS No.: 859212-16-1

Chemical Structure| 859212-16-1

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Bafetinib is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit.

Synonyms: INNO-406; NS-187

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Product Details of Bafetinib

CAS No. :859212-16-1
Formula : C30H31F3N8O
M.W : 576.62
SMILES Code : O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CN=CN=C3)=N2)=C1)C4=CC=C(CN5C[C@@H](N(C)C)CC5)C(C(F)(F)F)=C4
Synonyms :
INNO-406; NS-187
MDL No. :MFCD18633200
InChI Key :ZGBAJMQHJDFTQJ-DEOSSOPVSA-N
Pubchem ID :11387605

Safety of Bafetinib

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

Related Pathways of Bafetinib

RTK

Isoform Comparison

Biological Activity

Target
  • Abl

    Abl, IC50:5.8 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293 2.138 μM To assess intracellular engagement and inhibition of BRAF activity. PMC10840709
forskolin-responsive clones 0.5, 1, 2, and 10 µM 18 h The purpose was to assess the responsiveness of Bafetinib compared to other TKIs using luciferase assay; results showed unique reactivity patterns. PMC10530646
SW620/Ad300 cells 3 μM 72 hours Bafetinib significantly sensitized ABCB1 overexpressing MDR cells to their anticancer substrates and increased the intracellular accumulation of anticancer drugs, particularly doxorubicin and [3H]-paclitaxel in ABCB1 overexpressing cells. PMC4860574
NCI-H460/MX20 cells 3 μM 72 hours Bafetinib significantly decreased the IC50 values of mitoxantrone and SN-38 in HEK/ABCG2-R482, HEK/ABCG2-R482G and HEK/ABCG2-R482T cells in a concentration dependent pattern. PMC4860574

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01215799 Hormone Refractory Prostate Ca... More >>ncer Less << PHASE2 COMPLETED 2025-12-11 City of Hope Medical Center, D... More >>uarte, California, 91010, United States Less <<
NCT00352677 Chronic Myeloid Leukemia|Acute... More >> Lymphocytic Leukemia Less << PHASE1 COMPLETED 2025-05-08 H. Lee Moffitt Cancer Center a... More >>nd Research Institute, Tampa, Florida, 33612, United States|University of Texas MD Anderson Cancer Center, Houston, Texas, 77030, United States|Charite University of Medicine, Berlin, 13353, Germany|Johann Wolfgang Goethe Universit?t, Frankfurt am Main, 60590, Germany|University of Heidelberg Medical Clinic, Mannheim, 68305, Germany|Chaim Sheba Medical Center, Tel Hashomer, 52621, Israel Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.67mL

1.73mL

0.87mL

17.34mL

3.47mL

1.73mL

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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