521238

PDGFRβ/RAF Kinase Inhibitor

The PDGFRβ/RAF Kinase Inhibitor controls the biological activity of PDGFRβ/RAF Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): PDGFRβ/RAF Kinase Inhibitor, PDGFR Tyrosine Kinase Inhibitor XXII, 6-(4-(5-(3-(Trifluoromethyl)phenylamino)-4 H-1,2,4-triazol-3-yl)phenoxy)-2-(methylthio)pyrimidin-4-amine
• Empirical Formula (Hill Notation): C₂₀H₁₆F₃N₇OS
• CAS Number: 877874-85-6
• Molecular Weight: 459.45
• MDL number: MFCD27665470
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: beige
• solubility: DMSO: soluble
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: NC1=CC(OC2=CC=C(C3=NN=C(NC4=CC(C(F)(F)F)=CC=C4)N3)C=C2)=NC(SC)=N1

Description

General description

An orally bioavailable amino-triazole compound that is shown to bind to the inactive conformations of both PDGFRβ and Raf kinases (allosteric, Type II inh), and acts as a potent inhibitor of Flt3, Kit, PDGFRα and PDGFRβ (K_d = 52, 170, 300 and 520 nM, respectively) with selectivity over B-Raf, p38α, FGFR2 and VEGFR2 (K_d >10 µM) in a multi-kinase panel. Completely blocks the phosphorylations of MEK-1/2 S217/S221, ERK-1/2 T202/Y204 in FGF-stimulated HUVECs, PDGFRβ in PDGF-BB-stimulated VSMCs, ERK-1/2 T202/Y204 in 1205Lu-B Raf V600E cells, and C-Raf S338 at 10 µM. Reduces FGF-induced angiogenesis in mouse Matrigel model (50 mg/kg, i.p., bid) and selectively induces apoptosis in the endothelium; further, suppresses orthotopic renal cell carcinoma growth in mice (100 mg/kg, p.o., qd).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Murphy, E.A., et al. 2010. Proc. Natl. Acad. Sci. USA107, 4299.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable