Description: PDGFRβ, B-Raf, c-Raf, FLT3 and KIT inhibitor
Chemical Name: 2-(Methylthio)-6-[4-[5-[[3-(trifluoromethyl)phenyl]amino]-1H-1,2,4-triazol-3-yl]phenoxy]-4-pyrimidinamine
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
PDGFRβ and B-Raf allosteric inhibitor. Also inhibits c-Raf, FLT3 and KIT. Disrupts blood vessel formation in zebrafish embryos and inhibits angiogenesis in a mouse angiogenesis model. Inhibits growth of renal and pancreatic tumors in mice. Also arrests cells in prometaphase. Orally available.
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
45.94
100
ethanol
45.94
100
Preparing Stock Solutions
The following data is based on the product molecular weight 459.45. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.18 mL
10.88 mL
21.77 mL
5 mM
0.44 mL
2.18 mL
4.35 mL
10 mM
0.22 mL
1.09 mL
2.18 mL
50 mM
0.04 mL
0.22 mL
0.44 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Murphyet al (2010) Disruption of angiogenesis and tumor growth with an orally active drug that stabilizes the inactive state of PDGFRbeta/B-RAF. Proc.Natl.Acad.Sci.U.S.A. 107 4299 PMID: 20154271
Mielgoet al (2011) A MEK-independent role for CRAF in mitosis and tumor progression. Nat.Med. 17 PMID: 22081024