Home Protein Tyrosine Kinase VEGFR inhibitor ZD-4190

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ZD-4190 VEGFR inhibitor

Cat.No.S6543

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.
ZD-4190 VEGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 459.27

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Quality Control

Batch: S654301 DMSO]12 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.65%
99.65

Solubility

In vitro
Batch:

DMSO : 12 mg/mL (26.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 459.27 Formula

C19H16BrFN6O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 413599-62-9 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(C=C2C(=C1)C(=NC=N2)NC3=C(C=C(C=C3)Br)F)OCCN4C=CN=N4

Mechanism of Action

Targets/IC50/Ki
KDR
Flt-1
In vitro

ZD4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with greatest effect against KDR. Selectivity versus FGFR1 tyrosine kinase activity is demonstrated, with at least a 30-fold difference in the IC50 required to inhibit HUVEC proliferation stimulated by VEGF or bFGF, respectively. No effects on basal HUVEC growth are observed, even at the maximum ZD4190 concentration examined in these assays (10 μM).
In vivo

Chronic once-daily oral dosing of ZD4190 to young rats produces a dose-dependent increase in the femoral epiphyseal growth plate area. Once-daily oral dosing of ZD4190 to mice bearing established (∼0.5 cm3) human tumor xenografts (breast, lung, prostate, and ovarian) elicits significant antitumor activity and at doses that would not be expected to have any direct antiproliferative effect on tumor cells. In a PC-3 xenograft model, 10 weeks of ZD4190 dosing prolongs tumor cytostasis and upon withdrawal of therapy, tumor growth resumed after a short delay.
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