1. MAPK/ERK Pathway
    Protein Tyrosine Kinase/RTK
  2. Raf
    PDGFR
    FLT3
    c-Kit
  3. KG5

KG5 

Cat. No.: HY-15198
Handling Instructions

KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.

For research use only. We do not sell to patients.

KG5 Chemical Structure

KG5 Chemical Structure

CAS No. : 877874-85-6

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Description

KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities[1].

IC50 & Target[1]

B-Raf

 

PDGFRβ

520 nM (Kd)

FLT3

52 nM (Kd)

KIT

170 nM (Kd)

PDGFRα

300 nM (Kd)

c-Raf

 

In Vitro

KG5 (Compound 6) inhibits vascular smooth muscle cells (VSMCs) and endothelial cells viability with EC50 values of 0.59 μM and 0.54 μM, respectively[1].
Compound 6 selectively blocks S338 phosphorylation, yet does not influence S259[1].
KG5 (Compound 6) inhibits only PDGFRα and β with Kds of 300 and 520 nM, respectively, and Flt3 and KIT at 52 and 170 nM, respectively[1].
KG5 (Compound 6; 5 μM) inhibits phosphorylation of MEK and ERK in endothelial cells stimulated with bFGF or VEGF[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

KG5 (Compound 6; 100 mg/kg; oral administration; daily; for 26 days) treatment prevents tumor growth in an orthotopic renal cell carcinoma model[1].
KG5 (Compound 6; 50 mg/kg; i.p.; twice daily) treatment completely blocks angiogenesis relative to vehicle control in mice (injected with Matrigel containing bFGF). Pharmacokinetic analysis of the dose and formulation of KG5 used indicated a Cmax of 3.6 μg/mL, T1/2 of 11.5 h, and an area under the concentration time curve (AUC0-12h) of 14.7 μg•h/mL[1].
KG5 (Compound 6; 1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Nu/Nu mice injected with SN12C-RFP cells[1]
Dosage: 100 mg/kg
Administration: Oral administration; daily; for 26 days
Result: Prevented tumor growth in an orthotopic renal cell carcinoma model.
Molecular Weight

459.45

Formula

C₂₀H₁₆F₃N₇OS

CAS No.

877874-85-6

SMILES

CSC1=NC(OC2=CC=C(C=C2)C3=NN=C(N3)NC4=CC=CC(C(F)(F)F)=C4)=CC(N)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

KG5KG 5KG-5RafPDGFRFLT3c-KitRaf kinasesPlatelet-derived growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3SCFRCD117PDGFRβB-RafmetastasisanticancerantiangiogenicphosphorylationFlt3KITc-RafInhibitorinhibitorinhibit

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