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Tocris/Vatalanib succinate/5680/50/50 mg

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货号: 5680/50

品牌: Tocris

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Description: Potent VEGFR inhibitor; also aromatase inhibitor

Alternative Names: CGP 79787D, PTK787/ZK222584

Chemical Name: N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine succinate

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent VEGFR inhibitor (IC₅₀ values are 37 and 77 nM for VEGFR-2 and -1, respectively). Inhibits proliferation, migration and survival of HUVECs in vitro and inhibits growth, vascularization and metastasis of tumors expressing VEGFR in mouse models. Also inhibits PDGFR-β, c-Kit and c-Fms. Potent aromatase inhibitor (IC₅₀ = 50 nM). Orally available.

Compound Libraries

Vatalanib succinate is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	464.9
Formula	C₂₀H₁₅ClN₄.C₄H₆O₄
Storage	Store at -20°C
Purity	≥99% (HPLC)
CAS Number	212142-18-2
PubChem ID	151193
InChI Key	LLDWLPRYLVPDTG-UHFFFAOYSA-N
Smiles	ClC(C=C1)=CC=C1NC2=NN=C(CC3=CC=NC=C3)C4=CC=CC=C42.OC(CCC(O)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	46.49	100

Preparing Stock Solutions

The following data is based on the product molecular weight 464.9. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.15 mL	10.76 mL	21.51 mL
5 mM	0.43 mL	2.15 mL	4.3 mL
10 mM	0.22 mL	1.08 mL	2.15 mL
50 mM	0.04 mL	0.22 mL	0.43 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Banerjee et al (2009) The vascular endothelial growth factor receptor inhibitor PTK787/ZK222584 inhibits aromatase. Cancer Res. 69 4716 PMID: 19435899

Wood et al (2000) PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 60 2178 PMID: 10786682

Bold et al (2000) New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. J.Med.Chem. 43 2310 PMID: 10956229

Keywords: Vatalanib succinate, supplier, CGP79787D, PTK787, ZK222584, aromatase, inhibitors, inhibits, vascular, endothelial, growth, factor, receptors, tyrosine, kinases, cancer, anticancer, VEGFR, angiogenesis, metastasis, CGP, 79787D, PTK787/ZK222584, VEGFR, Cytochrome, P450, VEGFR, Tocris Bioscience

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