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371806 Sigma-Aldrich

GTP-14564 - CAS 34823-86-4 - Calbiochem

A cell-permeable, reversible, and ATP-competitive tricyclic benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases.

Synonym: 1-Phenyl-3-H-8-oxa-2,3-diaza-cyclopenta[a]inden, 3-Phenyl-1H-benzofuro[3,2-c]pyrazole

  • CAS Number 34823-86-4

  • Empirical Formula (Hill Notation) C15H10N2O

  • Molecular Weight 234.25

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Properties

Related Categories Biochemicals and Reagents, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, P to Q,
packaging   5 mg in Plastic ampoule (371806-5MG)
feature productdata solubility   DMSO (5 mg/ml)
brand family   CBC
form   Pale yellow solid
primary target IC50   0.3 µM for c-fms, c-kit, wt-FLT3 and ITD-FLT3; 1.0 µM for PDGFRβ
purity   ≥98% by HPLC
shipped in   3
storage conditions   15
  Y
  N

Description

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Class III receptor tyrosine kinases

Product competes with ATP.

Reversible: yes

General description

A cell-permeable, reversible, ATP-competitive, and tricyclic, benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases (IC50 = 300 nM for c-fms, c-kit, wt-FLT3, and internal tandem duplication (ITD)-FLT3; 1 µM for PDGFRβ). Does not affect the activities of KDR, EGFR, HER2, Abl, Src, PKA, Akt, PKC, MEK, or ERK1/2 (IC50 >10 µM). Inhibits FLT-3 ligand-dependent growth of Ba/F3 cells expressing wild type FLT-3. Reported to be useful in differentiating signal transduction pathways activated by wt-FLT3 and ITD-FLT3 in Ba/F3 cells.

A cell-permeable, reversible, and ATP-competitive tricyclic benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases (IC50 = 0.3 µM for c-fms, c-kit, wt-FLT3 and ITD-FLT3; 1.0 µM for PDGFRβ). Does not affect the activities of KDR, EGFR, HER2, Abl, Src, PKA, AKT, PKC, MEK, or ERK1/2 (IC50 ≥ 10 µM). Has been used successfully to differentiate between the signalling pathways activated by wt-FLT3 and ITD-FLT3 in Ba/F3 cells.

Other Notes

Murata, K., et al. 2003. J. Biol. Chem.278, 32892.

Packaging

Packaged under inert gas

Warning

Carcinogenic / Teratogenic (D)

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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