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Vatalanib

In stock
Catalog No.
A3969
VEGFR-1/-2 inhibitor,cell-permeable
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
10mg
$50.00
In stock
50mg
$150.00
In stock
100mg
$255.00
In stock

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Background

Vatalanib is a novel and potent inhibitor of VEGFR with IC50 value of 77 nM, 27 nM and 37 nM for VEGFR-1 (Flt-1), VEGFR-2 (FLK-1) and VEGFR-2 (KDR), respectively [1].
The vascular endothelial growth factor receptors (VEGFRs) are tyrosine kinases and are receptors for VEGF. VEGF acts as a key factor in pathological situations that involve in pathological situations that involve enhancing vascular permeability as well as neovascularization [1].
In CHO and HUVECs cells transfected with the KDR receptor, Vatalanib inhibited the VEGF-induced phosphorylation of KDR with an IC50 of 34 nM and 17 nM for the CHO and HUVECs cells, respectively. Also, Vatalanib inhibited thymidine incorporation induced by VEGF with IC50 value of 7.1 nM in HUVECs cells. Vatalanib inhibited VEGF-induced endothelial cell proliferation in a dose-dependant way [1].
In a growth factor implant mice model, Vatalanib (12.5, 25 or 50 mg/kg, 6 days) inhibited the angiogenic response around the implant induced by VEGF and PDGF [1]. In a xenograft mouse model, treatment mice with Vatalanib through gastric tube daily caused tumor inhibition rate of 76% [2].  
References:
[1]. Wood JM, Bold G, Buchdunger E, et al. 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, 2000, 60(8): 2178-2189.
[2]. Paesler J, Gehrke I, Gandhirajan RK, et al. The vascular endothelial growth factor receptor tyrosine kinase inhibitors vatalanib and pazopanib potently induce apoptosis in chronic lymphocytic leukemia cells in vitro and in vivo. Clin Cancer Res, 2010, 16(13): 3390-3398.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt346.81
Cas No.212141-54-3
FormulaC20H15ClN4
SynonymsCGP-79787; PTK 787; ZK222584
Solubility≥16.85 mg/mL in DMSO, ≥3.0125 mg/mL in EtOH with ultrasonic and warming, ≥32.53 mg/mL in H2O with ultrasonic and warming
Chemical NameN-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine
SDFDownload SDF
Canonical SMILESC1=CC=C2C(=C1)C(=NN=C2NC3=CC=C(C=C3)Cl)CC4=CC=NC=C4
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

Vatalanib

Related Biological Data

Vatalanib