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Chemical Structure| 193000-39-4 Chemical Structure| 193000-39-4

Structure of ZM323881 HCl
CAS No.: 193000-39-4

Chemical Structure| 193000-39-4

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ZZZM 323881 HCl is a potent and selective VEGFR2 inhibitor with IC50 of < 2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.

Synonyms: ZM 323881 (hydrochloride); ZM323881 hydrochloride

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Product Details of ZM323881 HCl

CAS No. :193000-39-4
Formula : C22H19ClFN3O2
M.W : 411.86
SMILES Code : CC1=C(O)C=C(NC2=C3C=CC(OCC4=CC=CC=C4)=CC3=NC=N2)C(F)=C1.Cl
Synonyms :
ZM 323881 (hydrochloride); ZM323881 hydrochloride
MDL No. :MFCD08703130

Safety of ZM323881 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of ZM323881 HCl

RTK

Isoform Comparison

Biological Activity

Target
  • VEGFR2

    VEGFR2, IC50:<2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
ARPE-19 cells 10 nM 1 hour Blocked the VEGF-E-induced decrease in TER PMC2199266
Primary porcine RPE cells 10 nM 1 hour Blocked the VEGF-E-induced decrease in TER PMC2199266
rat primary cortical neurons 10 nM 24 hours To investigate the effect of ZM323881 on ketamine or VEGF 164-induced increase in dendritic branching, results showed that ZM323881 completely blocked these effects. PMC6494682
ARPE-19 cells 10 nM 5 days Inhibition of VEGF signaling pathway, induction of EMT and up-regulation of CCN2 expression PMC11183261
ARPE19 cells 10 nM 6 hours To evaluate the effect of ZM323881 on Glyc-alb-induced RPE barrier dysfunction, results showed that pretreatment with ZM323881 reversed the TEER reduction caused by Glyc-alb PMC4523492
hfRPE cells 10 nM 6 hours To evaluate the effect of ZM323881 on Glyc-alb-induced RPE barrier dysfunction, results showed that pretreatment with ZM323881 reversed the TEER reduction caused by Glyc-alb PMC4523492
Wistar rat glomeruli 10 nM 60 minutes To study the effect of ZM323881 on VEGF-induced elevation of glomerular ultrafiltration coefficient (LpA/Vi), results showed that ZM323881 significantly inhibited the VEGF-induced increase in LpA/Vi PMC1464281
NCI-H460/MX20 cells 5 μM and 10 μM 72 hours ZM323881 significantly decreased the cytotoxic doses of mitoxantrone and SN-38 in BCRP-overexpressing NCI-H460/MX20 cells, reversing BCRP-mediated multidrug resistance. PMC7841404
HEK/ABCG2-R482 cells 5 μM and 10 μM 72 hours ZM323881 significantly decreased the IC50 values of mitoxantrone and SN-38 in HEK/ABCG2-R482 cells, reversing BCRP-mediated multidrug resistance. PMC7841404
HEK/ABCG2-R482G cells 5 μM and 10 μM 72 hours ZM323881 significantly decreased the IC50 values of mitoxantrone and SN-38 in HEK/ABCG2-R482G cells, reversing BCRP-mediated multidrug resistance. PMC7841404
HEK/ABCG2-R482T cells 5 μM and 10 μM 72 hours ZM323881 significantly decreased the IC50 values of mitoxantrone and SN-38 in HEK/ABCG2-R482T cells, reversing BCRP-mediated multidrug resistance. PMC7841404

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Dutch Belted rabbits subretinal bleb resorption model intravitreal injection 10 µM single dose 1 hour prior To inhibit the effect of VEGF on subretinal fluid resorption, results showed that ZM323881 reversed the VEGF-induced decrease in fluid resorption PMC3985404
Frogs Mesenteric microvessels Perfusion 10 nM Single administration, lasting 5 minutes To determine whether VEGF165b increases permeability via VEGF-R2 signaling, results showed that ZM323881 does not block the VEGF165b-induced increase in permeability. PMC1779637
Dutch-belted rabbits Diabetic retinopathy model Intravitreal injection 1 μM Single injection, assessed after 48 hours To evaluate the effect of ZM323881 on Glyc-alb-induced RPE dysfunction, results showed that ZM323881 reversed the reduction in RPE fluid resorption caused by Glyc-alb PMC4523492

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.14mL

2.43mL

1.21mL

24.28mL

4.86mL

2.43mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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