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343021 Flt-3 Inhibitor II - CAS 896138-40-2 - Calbiochem

343021
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₁₇H₁₂N₂O₃896138-40-2

Products

Catalogue NumberPackaging Qty/Pack
343021-1MG Plastic ampoule 1 mg
Description
Overview

This product has been discontinued.



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.

Catalogue Number343021
Brand Family Calbiochem®
SynonymsBis-(5-hydroxy-1H-indol-2-yl)methanone, PDGFR Tyrosine Kinase Inhibitor XI
References
ReferencesMahboobi, S., et al. 2006. J. Med. Chem. 49, 3101.
Product Information
CAS number896138-40-2
ATP CompetitiveN
FormYellowish brown solid
Hill FormulaC₁₇H₁₂N₂O₃
Chemical formulaC₁₇H₁₂N₂O₃
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetFlt-3
Primary Target IC<sub>50</sub>40 nM against Flt3 in cell-based receptor autophosphorylation; 33 nM against Flt3 in cell-free kinase reactions
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Irritant
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

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

Title

Safety Data Sheet (SDS) 

Flt-3 Inhibitor II - CAS 896138-40-2 - Calbiochem Certificates of Analysis

TitleLot Number
343021

References

Reference overview
Mahboobi, S., et al. 2006. J. Med. Chem. 49, 3101.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision14-September-2007 JSW
SynonymsBis-(5-hydroxy-1H-indol-2-yl)methanone, PDGFR Tyrosine Kinase Inhibitor XI
DescriptionA 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.
FormYellowish brown solid
Intert gas (Yes/No) Packaged under inert gas
CAS number896138-40-2
Chemical formulaC₁₇H₁₂N₂O₃
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (100 mg/ml) or Ethanol (5 mg/ml)
Storage -20°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Irritant
ReferencesMahboobi, S., et al. 2006. J. Med. Chem. 49, 3101.