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448103 Met/Flt-3/VEGFR2 Tyrosine Kinase Inhibitor - CAS 888719-03-7 - Calbiochem

The Met/Flt-3/VEGFR2 Tyrosine Kinase Inhibitor controls the biological activity of Met/Flt-3/VEGFR2 Tyrosine Kinase. Primarily used for Phosphorylation & Dephosphorylation applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(4-(1H-Pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorophenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide, Flt-3 Inhibitor VI, VEGFR Tyrosine Kinase Inhibitor XXVI, VEGFR2 Kinase Inhibitor XXIV

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448103
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
888719-03-7C₂₅H₁₆F₂N₄O₃

Products

Catalog NumberPackaging Qty/Pack
448103-5MG Plastic ampoule 5 mg
Description
OverviewA cell-permeable pyrrolopyridine-pyridone compound that acts as a potent ATP-competitive inhibitor of Met, Flt-3 and VEGFR2 (IC50 = 1.9, 4.0 and 27 nM, respectively), while exhibiting much reduced potency against Lck and c-Kit (IC50 = 290 and 610 nM, respectively) and little or no activity agaisnt Cdk2/CycE, IGF-1R, InsR, MK-2, PKA, and PKCα (IC50 >1 µM). Shown to selectively inhibit the Met-dependent, but not Met-independent, proliferation of gastric carcinoma cultures (IC50 = 60 nM vs. >5 µM against GTL-6 and N87 cells, respectively) in vitro and effectively abolish GTL-6-derived tumor growth (110% reduction of control tumor mass 39 days after tumor implant) by daily oral dosing (50 mg/kg) in mice in vivo.
Catalogue Number448103
Brand Family Calbiochem®
SynonymsN-(4-(1H-Pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorophenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide, Flt-3 Inhibitor VI, VEGFR Tyrosine Kinase Inhibitor XXVI, VEGFR2 Kinase Inhibitor XXIV
References
ReferencesKim, K.S., et al. 2008. J. Med. Chem. 51, 5330.
Product Information
CAS number888719-03-7
FormWhite to beige solid
Hill FormulaC₂₅H₁₆F₂N₄O₃
Chemical formulaC₂₅H₁₆F₂N₄O₃
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
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 Standard Handling
Storage +2°C to +8°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
Global Trade Identification Number
Catalog Number GTIN
448103-5MG4055977204650

Documentation

Met/Flt-3/VEGFR2 Tyrosine Kinase Inhibitor - CAS 888719-03-7 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Met/Flt-3/VEGFR2 Tyrosine Kinase Inhibitor - CAS 888719-03-7 - Calbiochem Certificates of Analysis

TitleLot Number
448103

References

Reference overview
Kim, K.S., et al. 2008. J. Med. Chem. 51, 5330.
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-June-2019 JSW
SynonymsN-(4-(1H-Pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorophenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide, Flt-3 Inhibitor VI, VEGFR Tyrosine Kinase Inhibitor XXVI, VEGFR2 Kinase Inhibitor XXIV
DescriptionA cell-permeable pyrrolopyridine-pyridone compound that acts as a potent ATP-competitive inhibitor of Met, Flt-3 and VEGFR2 (IC50 = 1.9, 4.0 and 27 nM, respectively), while exhibiting much reduced potency against Lck and c-Kit (IC50 = 290 and 610 nM, respectively) and little or no activity agaisnt Cdk2/CycE, IGF-1R, InsR, MK-2, PKA, and PKCα (IC50 >1 µM). Shown to selectively inhibit the Met-dependent, but not Met-independent, proliferation of gastric carcinoma cultures (IC50 = 60 nM vs. >5 µM against GTL-6 and N87 cells, respectively) in vitro and effectively abolish GTL-6-derived tumor growth (110% reduction of control tumor mass 39 days after tumor implant) by daily oral dosing (50 mg/kg) in mice in vivo.
FormWhite to beige solid
Intert gas (Yes/No) Packaged under inert gas
CAS number888719-03-7
Chemical formulaC₂₅H₁₆F₂N₄O₃
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (10 mg/ml) or Ethanol (1 mg/ml
Storage Protect from light
+2°C to +8°C
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 Standard Handling
ReferencesKim, K.S., et al. 2008. J. Med. Chem. 51, 5330.