KG 5

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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 for KG 5

KG 5 is a 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.

Compound Libraries for KG 5

KG 5 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for KG 5

M. Wt 459.45
Formula C20H16F3N7OS
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 877874-85-6
PubChem ID 53328059
Smiles NC1=NC(SC)=NC(OC(C=C4)=CC=C4C3=NN=C(N3)NC2=CC(C(F)(F)F)=CC=C2)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for KG 5

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 45.94 100
ethanol 45.94 100

Preparing Stock Solutions for KG 5

The following data is based on the product molecular weight 459.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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References for KG 5

References are publications that support the biological activity of the product.

Murphy et 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

Mielgo et al (2011) A MEK-independent role for CRAF in mitosis and tumor progression. Nat.Med. 17 PMID: 22081024

If you know of a relevant reference for KG 5, please let us know.

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Keywords: KG 5, KG 5 supplier, KG5, KIT, FLT3, B-Raf, C-Raf, PDGFRbeta, PDGFRB, β, inhibitors, inhibits, anticancers, angiogenesis, antiangiogenics, PDGFR, Other, RTKs, Raf, Kinase, Antiangiogenics, 5260, Tocris Bioscience

Citations for KG 5

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