PeptideDB

VEGFR-2-IN-58

VEGFR-2-IN-58

CAS No.:

VEGFR-2-IN-58 (Compound 7b) inhibits VEGFR-2 with IC50 of 42.5 nM. VEGFR-2-IN-58 is selectively cytotoxic to cancer cell
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VEGFR-2-IN-58 (Compound 7b) inhibits VEGFR-2 with IC50 of 42.5 nM. VEGFR-2-IN-58 is selectively cytotoxic to cancer cells. VEGFR-2-IN-58 shows G2/M phase cell cycle arrest in cancer cells. VEGFR-2-IN-58 induces apoptosis, increases BAX expression, and decreases Bcl2 expression. VEGFR-2-IN-58 inhibits wound closure in cancer cells.

Physicochemical Properties


Molecular Formula C24H16CLN3O
Molecular Weight 397.86
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets VEGFR2 42.5 nM (IC50)
ln Vitro VEGFR-2-IN-58 inhibits the proliferation of HepG2, MCF-7, A549, HT-29, PC3 and WI-38 cells with IC50 values of 7.28, 6.72, 6.66, 8.51, 14.5 and 30 μM, respectively[1]. In addition to inducing apoptosis, VEGFR-2-IN-58 (8.51 μM, 24 h) also exhibited G2/M phase cell growth inhibition in the HT-29 cell line [1]. VEGFR-2-IN-58 (0.85, 4.26 μM, 48 h) exhibited significant inhibition of wound healing in HT-29 cells[1].
Cell Assay Western Blot Analysis[1]
Cell Types: HT-29 cells Tested
Tested Concentrations: 0.85,4.26, 8.51 μM
Incubation Duration: 24 h
Experimental Results: Reduced p-VEGFR-2 expression in a dose-dependent manner.

Cell Cycle Analysis[1]
Cell Types: HT-29 cells Tested
Tested Concentrations: 8.51 μM
Incubation Duration: 24 h
Experimental Results: Caused cell growth arrest at G2/M based on accumulation of DNA content inHT-29 cells.

Apoptosis Analysis[1]
Cell Types: HT-29 cells Tested
Tested Concentrations: 8.51 μM
Incubation Duration: 24 h
Experimental Results: Elevated apoptotic gene BAX expression and suppressed anti-apoptotic gene Bcl-2 expression. Elevated total apoptosis percentage.
References

[1]. Furan- and Furopyrimidine-Based Derivatives: Synthesis, VEGFR-2 Inhibition, and In Vitro Cytotoxicity. ACS Med Chem Lett. 2024 Nov 25;15(12):2150-2157.


Solubility Data


Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5134 mL 12.5672 mL 25.1345 mL
5 mM 0.5027 mL 2.5134 mL 5.0269 mL
10 mM 0.2513 mL 1.2567 mL 2.5134 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.