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ZD-4190

Cat. No. M20586
ZD-4190 Structure
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Biological Activity

ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.

Chemical Information
Molecular Weight 459.27
Formula C19H16BrFN6O2
CAS Number 413599-62-9
Solubility (25°C) DMSO 12 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Min Yang, et al. Eur J Nucl Med Mol Imaging. PET imaging of early response to the tyrosine kinase inhibitor ZD4190

[2] Simon Tazzyman, et al. Int J Cancer. Inhibition of neutrophil infiltration into A549 lung tumors in vitro and in vivo using a CXCR2-specific antagonist is associated with reduced tumor growth

[3] Matthew S Morrison, et al. J Nucl Med. Use of a novel Arg-Gly-Asp radioligand, 18F-AH111585, to determine changes in tumor vascularity after antitumor therapy

[4] Quang-D Nguyen, et al. Mol Cancer Ther. Inhibition of vascular endothelial growth factor (VEGF)-165 and semaphorin 3A-mediated cellular invasion and tumor growth by the VEGF signaling inhibitor ZD4190 in human colon cancer cells and xenografts

[5] Pamela G Lloyd, et al. Am J Physiol Heart Circ Physiol. VEGF receptor antagonism blocks arteriogenesis, but only partially inhibits angiogenesis, in skeletal muscle of exercise-trained rats

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Keywords: ZD-4190 supplier, VEGFR/PDGFR, inhibitors, activators

 
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