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343021 Millipore

Flt-3 Inhibitor II - CAS 896138-40-2 - Calbiochem

The Flt-3 Inhibitor II, also referenced under CAS 896138-40-2, controls the biological activity of Flt-3.

Synonym: Bis-(5-hydroxy-1H-indol-2-yl)methanone, PDGFR Tyrosine Kinase Inhibitor XI, Bis-(5-hydroxy-1H-indol-2-yl)methanone, PDGFR Tyrosine Kinase Inhibitor XI

  • CAS Number 896138-40-2

  • Empirical Formula (Hill Notation) C17H12N2O3

  • Molecular Weight 292.29

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Properties

Related Categories Biochemicals and Reagents, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, P to Q,
color   yellow-brown
form   solid
shipped in   ambient
solubility   DMSO: 100 mg/mL
  ethanol: 5 mg/mL
storage condition   OK to freeze
  protect from light
brand family   Calbiochem
primary target IC50   40 nM against Flt3 in cell-based receptor autophosphorylation; 33 nM against Flt3 in cell-free kinase reactions
purity   ≥95% by HPLC
storage conditions   -20C

Description

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Flt-3

Product does not compete with ATP.

Reversible: no

Target IC50: 40 nM against Flt3 in cell-based receptor autophosphorylation; 33 nM against Flt3 in cell-free kinase reactions

General description

A cell-permeable symmetrical indolylmethanone kinase inhibitor that is more selective toward Flt3 over PDGFR either in cell-based receptor autophosphorylation (IC50 = 40 nM vs. 300 nM) or in cell-free kinase reactions (IC50 = 33 nM vs. 171 nM) and potently induces apoptosis in Flt3-expressing primary AML patient blasts. Affects Abl- or Kit-dependent cell growth only at much higher concentrations (IC50 = 4.2 and ≥0.5 µM, respectively), while exhibiting little effect against IL-3-mediated cellular signaling. The molecular mechanism of inhibition is presumably due to interaction at the enzyme′s ATP-binding site.

Other Notes

Mahboobi, S., et al. 2006. J. Med. Chem.49, 3101.

Packaging

Packaged under inert gas

Reconstitution

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

Warning

B

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.

Documents

Certificate of Analysis

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Protocols & Articles
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