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676487 VEGFR2 Kinase Inhibitor III - CAS 204005-46-9 - Calbiochem

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

Synonyms: 3-[(2,4-Dimethylpyrrol-5-yl)methylidene]-indolin-2-one, SU5416, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor III, VEGFR Tyrosine Kinase Inhibitor XIV

Primary Target: VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases
676487
  
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
204005-46-9C₁₅H₁₄N₂O
Description
Overview

This product has been discontinued.



A cell-permeable indolinone compound that acts as a selective, reversible, and ATP-competitive inhibitor of VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases (IC50 = 1.04 µM and 20 µM in NIH 3T3 cells overexpressing Flk-1; Km = 530 nM for ATP). Also potently inhibits the proliferation of HUVECs induced by VEGF, bFGF, or ECGS (IC50 = 50 nM, 5.3 µM and 30.5 µM, respectively). Blocks the autophosphorylation of internal tandem duplication (ITD) and wild type Fms-like tyrosine kinase 3 (FLT3) with an IC50 of 0.1 µM. Does not affect the EGF- or FGF- receptor tyrosine kinases activities even at 100 µM concentration. Reported to induce apoptosis and inhibit VEGF-dependent mitogenesis of human endothelial cells. A 10 mM (500 µg/210 µl) solution of VEGF Receptor 2 Kinase Inhibitor III (Cat. No. 676498) in DMSO is also available.
Catalogue Number676487
Brand Family Calbiochem®
Synonyms3-[(2,4-Dimethylpyrrol-5-yl)methylidene]-indolin-2-one, SU5416, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor III, VEGFR Tyrosine Kinase Inhibitor XIV
References
ReferencesTille, J.C., et al. 2003. Exp. Cell Res. 285, 286.
Itokawa, T., et al. 2002. Mol. Cancer Ther. 1, 295.
Ma, J., et al. 2002. J. Pharmacol. Exp. Ther. 305, 833.
Yee, K.W., et al. 2002. Blood 100, 2941.
Mendel, D.B., et al. 2000. Clin. Cancer Res. 6, 4848.
Fong, T.A.T., et al. 1999. Cancer Res. 59, 99.
Sun, L., et al. 1999. J. Med. Chem. 42, 5120.
Product Information
CAS number204005-46-9
ATP CompetitiveY
FormYellow orange solid
Hill FormulaC₁₅H₁₄N₂O
Chemical formulaC₁₅H₁₄N₂O
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetVEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases
Primary Target IC<sub>50</sub>1.04 and 20 µM against VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases, respectively, in NIH 3T3 cells overexpressing Flk-1; ; Km = 530 nM for ATP
Purity≥97% 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 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 Item Number
Catalogue Number GTIN
676487 0

Documentation

VEGFR2 Kinase Inhibitor III - CAS 204005-46-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

VEGFR2 Kinase Inhibitor III - CAS 204005-46-9 - Calbiochem Certificates of Analysis

TitleLot Number
676487

References

Reference overview
Tille, J.C., et al. 2003. Exp. Cell Res. 285, 286.
Itokawa, T., et al. 2002. Mol. Cancer Ther. 1, 295.
Ma, J., et al. 2002. J. Pharmacol. Exp. Ther. 305, 833.
Yee, K.W., et al. 2002. Blood 100, 2941.
Mendel, D.B., et al. 2000. Clin. Cancer Res. 6, 4848.
Fong, T.A.T., et al. 1999. Cancer Res. 59, 99.
Sun, L., et al. 1999. J. Med. Chem. 42, 5120.
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.

Revision27-September-2010 RFH
Synonyms3-[(2,4-Dimethylpyrrol-5-yl)methylidene]-indolin-2-one, SU5416, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor III, VEGFR Tyrosine Kinase Inhibitor XIV
DescriptionA cell-permeable, selective, reversible, and ATP-competitive inhibitor of VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases (IC50 = 1 µM and 20 µM, respectively in NIH3T3 cells over-expressing Flk-1; Km = 530 nM for ATP). Also reported to potently inhibit the proliferation of HUVECs induced by VEGF, bFGF or ECGS (IC50 = 50 nM, 5.3 µM and 30 µM, respectively). Shown to block the autophosphorylation of internal tandem duplication (ITD) and wild type Fms-like tyrosine kinase 3 (FLT3) (IC50 = 100 nM). Does not affect the activities of EGFR or FGFR tyrosine kinases even at a concentration of 100 µM. Reported to induce apoptosis and inhibit VEGF-dependent mitogenesis of endothelial cells.
FormYellow orange solid
Intert gas (Yes/No) Packaged under inert gas
CAS number204005-46-9
Chemical formulaC₁₅H₁₄N₂O
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (5 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
ReferencesTille, J.C., et al. 2003. Exp. Cell Res. 285, 286.
Itokawa, T., et al. 2002. Mol. Cancer Ther. 1, 295.
Ma, J., et al. 2002. J. Pharmacol. Exp. Ther. 305, 833.
Yee, K.W., et al. 2002. Blood 100, 2941.
Mendel, D.B., et al. 2000. Clin. Cancer Res. 6, 4848.
Fong, T.A.T., et al. 1999. Cancer Res. 59, 99.
Sun, L., et al. 1999. J. Med. Chem. 42, 5120.