2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. 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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VEGFR-2-IN-43 Related Antibodies

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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.

VEGFR-2-IN-43 Related Antibodies

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
Unlabeled CAS

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.

Keywords:

VEGFR-2-IN-43VEGFRVascular endothelial growth factor receptorLX-2 cellsHUVEC cellsWater solubilityICR micew-AMDOral administrationBaF3-TEL-VEGFR2 cellsHergCardiac safetyliver microsomal stabilityplasma stabilityHalf timeInhibitorinhibitorinhibit

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