A PDGFRα and PDGFRβ inhibitor
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PDGFR TKI III

Item No. 14925

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(6,7-dimethoxy-4-quinazolinyl)-N-(4-phenoxyphenyl)-1-piperazinecarboxamide
CAS Number
205254-94-0
Synonyms
  • PDGFR Tyrosine Kinase Inhibitor III
  • Platelet-derived Growth Factor Receptor TKI III
  • Platelet-derived Growth Factor Receptor Tyrosine Kinase Inhibitor III
Molecular Formula
C27H27N5O4
Formula Weight
485.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(N(C1=CC=C(OC2=CC=CC=C2)C=C1)[H])N3CCN(C4=NC=NC5=C4C=C(OC)C(OC)=C5)CC3
InChi Code
InChI=1S/C27H27N5O4/c1-34-24-16-22-23(17-25(24)35-2)28-18-29-26(22)31-12-14-32(15-13-31)27(33)30-19-8-10-21(11-9-19)36-20-6-4-3-5-7-20/h3-11,16-18H,12-15H2,1-2H3,(H,30,33)
InChi Key
INTPTKHSGKBHHW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    PDGFR TKI III is an inhibitor of PDGFRα and PDGFRβ (IC50s = 0.05 and 0.13 µM, respectively).1 It is selective for PDGFRα and PDGFRβ over FGFR, EGFR, PKA, and PKC (IC50s = 29.7, >30, >30, and >30 µM, respectively) but does inhibit c-Kit and FMS-related tyrosine kinase 3 (FLT3; IC50s = 0.05 and 0.23 µM, respectively). PDGFR TKI III inhibits PDGF homodimer-induced proliferation of pig aorta smooth muscle cells (IC50 = 0.25 µM). It inhibits the migration of primary mouse dorsal aorta mesenchymal stem cells (DA-MSCs) induced by embryonic mouse blood when used at a concentration of 2 µM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Matsuno, K., Ichimura, M., Nakajima, T., et al. Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives. J. Med. Chem. 45(14), 3057-3066 (2002).

    2. Yan, X.-L., Lan, Y., Wang, X.-Y., et al. Migration of dorsal aorta mesenchymal stem cells induced by mouse embryonic circulation. Dev. Dyn. 240(1), 65-74 (2011).