KG5

SKU: orb1303161

Description

KG5 is a dual allosteric inhibitor targeting PDGFRβ and B-Raf, with additional activity against FLT3, KIT, and c-Raf. It exhibits anticancer and antiangiogenic properties, making it a useful compound for oncology research in both cellular and animal models of relevant cancers.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 877874-85-6
• MW: 459.45
• Purity: 98.32% (May vary between batches)
• Formula: C₂₀H₁₆F₃N₇OS
• SMILES: CSc1nc(N)cc(Oc2ccc(cc2)-c2nnc(Nc3cccc(c3)C(F)(F)F)[nH]2)n1
• Target: FLT,c-Kit,Raf,PDGFR
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (7.18 mM);DMSO:95 mg/mL (206.77 mM)

Bioactivity

• Target IC50:
  PDGFRα:300 nM (Kd)|c-Kit:170 nM (Kd)|PDGFRβ:520 nM (Kd)|FLT3:52 nM (Kd)
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cluster of differentiation antigen 135, CD135, CD117, c-Kit, cKit, c-Raf, C-Raf, anticancer, antiangiogenic, B-Raf, KG 5, KG5, KG-5, Kit, KIT, inhibit, metastasis, Platelet-derived growth factor receptor, PDGFR, Inhibitor, Fms like tyrosine kinase 3, FLT3, SCFR, PDGFRβ, PDGFRα, Raf, Raf kinases, phosphorylation

Compound Identifiers

PubChem CID

53328059