1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. VEGFR-2-IN-43

VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research.

For research use only. We do not sell to patients.

VEGFR-2-IN-43 Chemical Structure

VEGFR-2-IN-43 Chemical Structure

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Description

VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research[1].

IC50 & Target[1]

VEGFR2

39.91 μM (IC50)

In Vitro

VEGFR-2-IN-43 (compound 16) (0-50 μM, 72 h) demonstrates a weak inhibitory effect on proliferation of LX-2 cells, and significantly inhibits the proliferation of BaF3-Tel-VEGFR2 cells[1].
VEGFR-2-IN-43 (0-10 μM, 48 h) exhibits a concentrationdependent inhibition of VEGFR2 phosphorylation in HUVECs [1].
VEGFR-2-IN-43 (1 μM, 0-120 min) shows remarkable plasma stability and moderate liver microsomal stability[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: BaF3-Tel-VEGFR2 cells, BaF3 cells (BaF3-Tel-VEGFR2 cells were constructed through viral transgene technology using BaF3 cells as a template, and their proliferation was dependent on VEGFR2 kinase.)
Concentration: 0-50 μM
Incubation Time: 72 h
Result: The GI50 value of VEGFR-2-IN-43 (compound 16) for BAF3-tel-VEGFR2 cells was 22.9 nM, and the proliferation of BaF3 cells was almost not inhibited.
In Vivo

VEGFR-2-IN-43 (compound 16) (2/10 mg/kg, i.v. and p.o.) exhibits acceptable oral bioavailability in ICR mice (F = 20.2%)[1].

Pharmacokinetic study of VEGFR-2-IN-43 (compound 16) on mice[1]

Route Dose (mg/kg) AUC0-t (ng·h/mL) AUC0-∞ (ng·h/mL) MRT0-t (h) Cmax (ng/mL) Tmax (h) T1/2 (h) F (%)
i.v. 2 508 512 0.665 853 0.0833 1.32 /
p.o. 10 506 518 0.72 321 0.417 1.58 20.2

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

470.49

Formula

C24H27FN4O5

SMILES

CCO[C@@H]1CN(C[C@H]1NC(C2=C(NC(/C=C3C(NC4=CC=C(C=C4\3)F)=O)=C2C)C)=O)C(CO)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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VEGFR-2-IN-43 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
VEGFR-2-IN-43
Cat. No.:
HY-163403
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