VEGFR2 Kinase Inhibitor III (CAS 204005-46-9)

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Alternate Names: Semaxanib; SU 5416

Application: VEGFR2 Kinase Inhibitor III is a VEGFR2, Met, RET, PDGFR, and ALK inhibitor

CAS Number: 204005-46-9

Purity: ≥97%

Molecular Weight: 238.28

Molecular Formula: C₁₅H₁₄N₂O

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

* Refer to Certificate of Analysis for lot specific data (including water content).

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VEGFR2 Kinase Inhibitor III: sc-202851...

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VEGFR2 Kinase Inhibitor III is a cell-permeable ATP-competitive inhibitor of Flk-1 (VEGFR2/KDR, kinase insert domain receptor), which is the major growth factor for vascular endothelial cells. This receptor is a type III tyrosine kinase receptor that functions as the main mediator of VEGF-induced endothelial proliferation, survival, and migration. Studies suggest that VEGFR2 Kinase Inhibitor III also inhibits a variety of other receptors such as Met, Flt-3/Flk-2 (FLT-3 receptor tyrosine kinases), Ret, c-Kit, PDGFR, c-Abl and Arg (ABL), and ALK. In addition, VEGFR2 kinase inhibitor III regulates the signaling pathways used by oncogenic RET-transfected cells by regulating the extracellular signal regulated kinase (ERK) and JNK pathways.

References

1. Vajkoczy, P., et al. 1999. Neoplasia. 1: 31-41. PMID: 10935468
2. Mologni, L., et al. 2006. J. Mol. Endocrinol. 37: 199-212. PMID: 17032739
3. Komi, Y., et al. 2009. Cancer Sci. 100: 269-277. PMID: 19200258

Physical State :

Solid

Solubility :

Soluble in DMSO (5 mg/ml), and ethanol (100 mM). Insoluble in water.

Storage :

Store at 4° C

Melting Point :

221-222° C

Boiling Point :

481.41° C at 760 mmHg (Predicted)

Density :

1.26 g/cm³ (Predicted)

Refractive Index :

n²⁰_D 1.68 (Predicted)

IC50 :

proliferation of HUVEC₅₀s induced by VEGF: IC₅₀ = 50 nM; autophosphorylation of internal tandem duplication: IC₅₀ = 0.1 µM; autophosphorylation of wild type Fms-like tyrosine kinase 3: IC₅₀ = 0.1 µM; VEGF-R: IC₅₀ = 1.04 µM (NIH 3T3 cells overexpressing Flk-1); Oxytocin-R: EC₅₀50 = 11.47 µM (human); AVP Receptor V1a: EC₅₀50 = 12.07 µM (human); PDGF-R tyrosine kinases: IC₅₀ = 20 µM (NIH 3T3 cells overexpressing Flk-1); proliferation of HUVEC₅₀s induced by EC₅₀GS: IC₅₀ = 30.5 µM; proliferation of HUVEC₅₀s induced by bFGF: IC₅₀ = 5.3 µM

pK Values :

pK_a: 13.18 (Predicted), pK_b: 1.53 (Predicted)

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

WGK Germany :

PubChem CID :

5329098

MDL Number :

MFCD01940922

SMILES :

CC1=CC(=C(N1)/C=C\\2/C3=CC=CC=C3NC2=O)C

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Certificate of Analysis

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VEGFR2 Kinase Inhibitor III (CAS 204005-46-9) Product Citations

See how others have used VEGFR2 Kinase Inhibitor III (CAS 204005-46-9). Click on the entry to view the PubMed entry .

Citations 1 to 6 of 6 total

PMID: # 26699078 Giordano, A. et al. 2016. Vascul. Pharmacol. 80: 67-74.

PMID: # 25450973 Lahiani, A. et al. 2015. Biochim. Biophys. Acta. 1853: 422-30.

PMID: # 25886469 Cui, HJ. et al. 2015. BMC Complement Altern Med. 15: 91.

PMID: # 30028964 Chem Biol Interact. 110-120.

PMID: # 24751361 Giordano, A. et al. Vascul. Pharmacol. 61: 63-71.

Citations 1 to 6 of 6 total

Rated 5 out of 5 by JL from Lahiani Lahiani, et al. (PubMed ID 25450973) found that pre-treating mesenchymal stem cells with 240ng/ml of Semaxanib (VEGFR2 Kinase Inhibitor III) reduced the growth factors and co-culture conditioned medium effects by 70% and 20% respectively. -SCBT Publication Review

Date published: 2015-03-06

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