A potent and selective VEGF receptor inhibitor
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Vatalanib (hydrochloride)

Item No. 14868

Technical Information
Formal Name
N-(4-chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine, dihydrochloride
CAS Number
212141-51-0
Synonyms
  • CGP 79787
  • PTK787
  • PTK/ZK
Molecular Formula
C20H15ClN4 • 2HCl
Formula Weight
Purity
≥98%
A crystalline solid
DMSO: 25 mg/mlDMSO:PBS (pH 7.2) (1:10): 0.09 mg/mlEthanol: PBS: 0.3 mg/ml
λmax
218, 320 nm
SMILES
ClC(C=C1)=CC=C1NC2=NN=C(CC3=CC=NC=C3)C4=CC=CC=C42.Cl.Cl
InChi Code
InChI=1S/C20H15ClN4.2ClH/c21-15-5-7-16(8-6-15)23-20-18-4-2-1-3-17(18)19(24-25-20)13-14-9-11-22-12-10-14;;/h1-12H,13H2,(H,23,25);2*1H
InChi Key
AZUQEHCMDUSRLH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Vatalanib is an antagonist of the VEGF receptors, inhibiting the receptor tyrosine kinase activities of VEGFR1 (Flt1), VEGFR2 (KDR), and VEGFR3 (Flt4) with IC50 values of 77, 37, and 190 nM, respectively.1,2 It less potently inhibits PDGF and c-Kit (IC50 = 600 and 700 nM) and has no effect on a large panel of additional kinases.1,3,2 Vatalanib completely blocks retinal neovascularization in oxygen-induced ischemic retinopathy in mice, suggesting its use in diabetic retinopathy and other diseases featuring aberrant vascular development.4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bold, G., Altmann, K.H., Frei, J., et alNew 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(16), 3200 (2000).

    2. Fabian, M.A., Biggs, W.H., III, Treiber, D.K., et alA small molecule-kinase interaction map for clinical kinase inhibitors. Nat. Biotechnol. 23(3), 329-336 (2005).

    3. Furet, P., Bold, G., Hofmann, F., et alIdentification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg. Med. Chem. Lett. 13(18), 2967-2971 (2003).

    4. Ozaki, H., Seo, M.S., Ozaki, K., et alBlockade of vascular endothelial cell growth factor receptor signaling is sufficient to completely prevent retinal neovascularization. Am. J. Pathol. 156(2), 697-707 (2000).

    5. Giatromanolaki, A., Koukourakis, M., Sivridis, E., et alVascular density analysis in colorectal cancer patients treated with vatalanib (PTK787/ZK222584) in the randomised CONFIRM trials. Br. J. Cancer 107(7), 1044-1050 (2012).