PDGFR Tyrosine Kinase Inhibitor III CAS: 205254-94-0
MF: C27H27N5O4
MW: 485.5
An ATP-competitive PDGFR inhibitor.

PDGFR Tyrosine Kinase Inhibitor III (CAS 205254-94-0)

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Alternativa namn: 4-(6,7-dimethoxyquinazolin-4-yl)-N-(4-phenoxyphenyl)piperazine-1-carboxamide
Ansökan PDGFR Tyrosine Kinase Inhibitor III is an ATP-competitive PDGFR inhibitor
Momsregistreringsnummer :: 205254-94-0
Molecular Weight: 485.5
Molecular Formula: C27H27N5O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

PDGFR Tyrosine Kinase Inhibitor III is a cell-permeable, potent, selective, and ATP-competitive inhibitor of the PDGFR family of tyrosine kinases (IC50 = 50 nM for PDGFR-α, 80 nM for PDGFR-β, 50 nM for c-Kit, and 230 nM for Flt-3/Flk-2). PDGFR Tyrosine Kinase Inhibitor III inhibits the activities of other kinases only at much higher concentrations (IC50 > 30μM for EGFR, FGFR, Src, PKA, and PKC). Reported to block PDGF-BB-induced proliferation of porcine aorta smooth muscle cells (IC50 = 250 nM).


Konferenser

1. Matsuno, K., et al. 2002. J. Med. Chem. 45: 3057-3066. PMID: 12086491
2. Matsuno, K., et al. 2002. J. Med. Chem. 45: 4513-4523. PMID: 12238930
3. Matsuno, K., et al. 2003. Bioorg. Med. Chem. Lett. 13: 3001-3004. PMID: 12941321
4. Matsuno, K., et al. 2003. J. Med. Chem. 46: 4910-4925. PMID: 14584942

Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml).
LAGRING :
Store at 4° C
Melting Point :
292.08° C (Predicted)
Boiling Point :
~713.68° C at 760 mmHg (Predicted)
Density :
~1.31 g/cm3 (Predicted)
Refractive Index :
n20D 1.67 (Predicted)
IC50 :
α-PDGFR: IC50 = 0.05 µM; β-PDGFR: IC50 = 0.08 µM; c-Kit: IC50 = 0.05 µM; Flt3: IC50 = 0.23 µM; EGFR: IC50 = ≥30 µM; FGFR: IC50 ≥30 µM; Src: IC50 ≥30 µM; PKA: IC50 ≥30 µM; PKC: IC50 ≥30 µM; PDGF-BB induced proliferation of porcine aorta smooth muscle cells: IC50 = 0.25 µM
pK Values :
pKa: 13.18 (Predicted), pKb: 9.48 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
10907042
SMILES :
COC1=C(C=C2C(=C1)C(=NC=N2)N3CCN(CC3)C(=O)NC4=CC=C(C=C4)OC5=CC=CC=C5)OC

Download SDS (MSDS)

Certificate of Analysis

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PDGFR Tyrosine Kinase Inhibitor III (CAS 205254-94-0)  Produkt Citat

See how others have used PDGFR Tyrosine Kinase Inhibitor III (CAS 205254-94-0). Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 26461489  Friedman, AA. et al. 2015. PloS one. 10: e0140310.

PMID: # 24901498  Raz, O. et al. 2014. PloS one. 9: e95156.

Citations 1 to 2 of 2 total
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