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Chemical Structure| 244240-24-2 Chemical Structure| 244240-24-2

Structure of (Z)-LFM-A13
CAS No.: 244240-24-2

Chemical Structure| 244240-24-2

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LFM-A13 is a potent and selective inhibitor of Btk with IC50 of 17.2 μM and also inhibits PLK3 with IC50 of 7.2 μM.

Synonyms: LFM-A13

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Product Details of (Z)-LFM-A13

CAS No. :244240-24-2
Formula : C11H8Br2N2O2
M.W : 360.00
SMILES Code : BrC1=C(NC(/C(C#N)=C(C)\O)=O)C=C(Br)C=C1
Synonyms :
LFM-A13
MDL No. :MFCD09878279
InChI Key :UVSVTDVJQAJIFG-VURMDHGXSA-N
Pubchem ID :54676905

Safety of (Z)-LFM-A13

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H312-H332
Precautionary Statements:P280

Related Pathways of (Z)-LFM-A13

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • BTK

    BTK, Ki:1.4 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Osteoclast precursors 25 μM 4 h Inhibited migration and differentiation of osteoclast precursors PMC3971999
Myeloma cells (INA6) 25 μM 6 h Inhibited SDF-1-induced migration of myeloma cells PMC3971999
MDA-MB-231 10, 30, 100 μM 48 h To evaluate the effect of Epo and LFM-A13 on the proliferation of MDA-MB-231 cells. The results showed that the combination of Epo and LFM-A13 significantly reduced cell viability. PMC7717683
MCF-7 10, 30, 100 μM 48 h To evaluate the effect of Epo and LFM-A13 on the proliferation of MCF-7 cells. The results showed that the combination of Epo and LFM-A13 significantly reduced cell viability. PMC7717683
HT-29 human colon adenocarcinoma cells 30, 100 μM 48 h To assess the effects of LFM-A13 on colon cancer cell growth, results showed that LFM-A13 inhibited the growth of HT-29 cells, and the effect was more significant when combined with Epo. PMC5811618
DLD-1 human colon adenocarcinoma cells 30, 100 μM 48 h To assess the effects of LFM-A13 on colon cancer cell growth, results showed that LFM-A13 inhibited the growth of DLD-1 cells, and the effect was more significant when combined with Epo. PMC5811618
C3H 10T1/2 mouse fibroblasts 20 μM 0, 1, 6, 24, or 48 h LFM-A13 inhibits Stat3 phosphorylation PMC3156164

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SCID mice SCID-rab model Intraperitoneal injection 40 mg/kg Twice daily for 3 weeks Inhibited homing of myeloma cells to bone and myeloma-induced bone disease PMC3971999
Mice Stress models Intraperitoneal injection 50 mg/kg Every 24 hours until the end of the experiment To validate the observations from ibrutinib studies, it was found that BTK inhibition led to anxiolysis and attenuated neuroinflammation, as indicated by significant reduction of NLRP3 inflammasome and proinflammatory IL-1β in hippocampus and amygdala. PMC8665324

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.89mL

2.78mL

1.39mL

27.78mL

5.56mL

2.78mL

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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