KG 5

Tocris Bioscience a Bio-Techne Brand

Catalog # 5260

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Key Product Details

Description:	PDGFRβ, B-Raf, c-Raf, FLT3 and KIT inhibitor
Chemical Name:	2-(Methylthio)-6-[4-[5-[[3-(trifluoromethyl)phenyl]amino]-1_H-1,2,4-triazol-3-yl]phenoxy]-4-pyrimidinamine
Purity:	≥98% (HPLC)
Molecular Weight:	459.45

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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
InChi Key	CMYHZFCJPORPHY-UHFFFAOYSA-N
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 for KG 5

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

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.

Mielgo A MEK-independent role for CRAF in mitosis and tumor progression. Nat.Med. 2011 PMID: 22081024
Murphy 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. 2010 PMID: 20154271

Citations for KG 5

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KG 5

Tocris Bioscience a Bio-Techne Brand

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