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KG5

Catalog No. T41003   CAS 877874-85-6

KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.

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KG5 Chemical Structure
KG5, CAS 877874-85-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
5 mg In stock $ 113.00
10 mg In stock $ 178.00
25 mg In stock $ 358.00
50 mg In stock $ 549.00
100 mg In stock $ 788.00
1 mL * 10 mM (in DMSO) In stock $ 136.00
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Purity: 98.2%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.
Targets&IC50 Kit:170 nM (Kd), PDGFRα:300 nM (Kd), PDGFRβ:520 nM (Kd), FLT3:52 nM (Kd)
In vitro KG5 inhibits FLT3 and KIT at 52 and 170 nM, respectively. In endothelial cells stimulated with bFGF or VEGF, KG5 (5 μM) inhibits phosphorylation of MEK and ERK. KG5 inhibits vascular smooth muscle cells (VSMCs) and endothelial cell viability with EC50 values of 0.59 μM and 0.54 μM, respectively. KG5 selectively blocks S338 phosphorylation, yet does not influence S259[1].
In vivo KG5 (1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis. In male Nu/Nu mice injected with SN12C-RFP cells, KG5 (100 mg/kg; oral) prevents tumor growth. KG5 (50 mg/kg; i.p.) completely blocks angiogenesis in mice injected with Matrigel containing bFGF with a Cmax of 3.6 μg/mL, T1/2 of 11.5 h, and an AUC0-12h of 14.7 μg•h/mL[1].
Molecular Weight 459.45
Formula C20H16F3N7OS
CAS No. 877874-85-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (206.77 mM), sonification is recommended.

TargetMolReferences and Literature

1. Eric A Murphy, et al. 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 Mar 2;107(9):4299-304.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Prostate Cancer Compound Library Anti-Ovarian Cancer Compound Library Anti-Liver Cancer Compound Library Inhibitor Library Bioactive Compounds Library Max Anti-Obesity Compound Library Kinase Inhibitor Library Bioactive Compound Library

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Keywords

KG5 877874-85-6 Angiogenesis MAPK Tyrosine Kinase/Adaptors FLT Raf PDGFR c-Kit B-Raf antiangiogenic KIT CD135 Raf kinases Cluster of differentiation antigen 135 Platelet-derived growth factor receptor Fms like tyrosine kinase 3 metastasis c-Raf FLT3 PDGFRβ inhibit anticancer phosphorylation SCFR Inhibitor KG 5 KG-5 CD117 inhibitor

 

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