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Chemical Structure| 1627856-64-7 Chemical Structure| 1627856-64-7

Structure of GSK3179106
CAS No.: 1627856-64-7

Chemical Structure| 1627856-64-7

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GSK3179106 is a potent, selective and gut-restricted RET kinase inhibitor with IC50 value of 0.4nM.

Synonyms: RET KInase inhibitor 1

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Product Details of GSK3179106

CAS No. :1627856-64-7
Formula : C22H21F4N3O4
M.W : 467.41
SMILES Code : O=C(NC1=NOC(C(C)(C)C(F)(F)F)=C1)CC2=CC=C(C(C(OCC)=C3)=CNC3=O)C=C2F
Synonyms :
RET KInase inhibitor 1
MDL No. :MFCD30747847
InChI Key :IDXKJSSOUXWLDB-UHFFFAOYSA-N
Pubchem ID :78427026

Safety of GSK3179106

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of GSK3179106

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
RAW264.7 macrophages 0.625, 1.25, 2.5, 5 μM 24 hours To evaluate the effect of GSK3179106 on cell viability, results showed no obvious cytotoxicity at concentrations ranging from 0.625 to 5 μM. Respir Res. 2024 Oct 28;25(1):388
J774A.1 macrophages 0.625, 1.25, 2.5, 5 μM 24 hours To evaluate the effect of GSK3179106 on cell viability, results showed no obvious cytotoxicity at concentrations ranging from 0.625 to 5 μM. Respir Res. 2024 Oct 28;25(1):388
SK-N-AS cells 10 mM 3 days To evaluate the effect of GSK3179106 on SK-N-AS cell proliferation J Pharmacol Exp Ther. 2019 Feb;368(2):299-307
TT cells 10 mM 8 days To evaluate the effect of GSK3179106 on TT cell proliferation J Pharmacol Exp Ther. 2019 Feb;368(2):299-307

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice LPS-induced sepsis and acute lung injury model Intraperitoneal injection 3 mg/kg and 6 mg/kg 12 hours and 1 hour before administration To evaluate the protective effect of GSK3179106 on LPS-induced lung injury, results showed that GSK3179106 significantly attenuated LPS-induced lung injury, inhibited infiltration of inflammatory cells and reduced expression of inflammatory cytokines. Respir Res. 2024 Oct 28;25(1):388
Rats Colonic hypersensitivity models Oral 3 and 10 mg/kg Twice daily for 3.5 days To evaluate the inhibitory effect of GSK3179106 on colonic hypersensitivity J Pharmacol Exp Ther. 2019 Feb;368(2):299-307
Rats Colonic hypersensitivity model Oral 10 mg/kg 7 doses over 3.5 days Evaluate the ameliorative effect of GSK3179106 on colonic hypersensitivity ACS Med Chem Lett. 2018 May 24;9(7):623-628

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.70mL

2.14mL

1.07mL

21.39mL

4.28mL

2.14mL

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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