2. Protein Tyrosine Kinase/RTK Apoptosis
  3. VEGFR Apoptosis
  4. VEGFR-2-IN-85

VEGFR-2-IN-85 is a strong VEGFR-2 inhibitor, with an IC50 value of 0.23 μM. VEGFR-2-IN-85 exhibits potent cytotoxic activity against multiple cancer cell lines with minimal toxicity toward normal cells. VEGFR-2-IN-85 also impairs cancer cell migration, likely through modulation of the VEGFR-2/p-Akt pathway. VEGFR-2-IN-85 can induce apoptosis through modulation of Caspase-3, Bax and Bcl-2. VEGFR-2-IN-85 arrests cell cycle at the G2/M phase and has anti-angiogenic activity. VEGFR-2-IN-85 is a targeted radiosensitizer enhancing radiation-induced cytotoxicity. VEGFR-2-IN-85 can be used for research on cancers such as non-small cell lung cancer, breast cancer, and liver cancer.

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

VEGFR-2-IN-85

VEGFR-2-IN-85 Chemical Structure

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VEGFR-2-IN-85 Related Antibodies

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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Description

VEGFR-2-IN-85 is a strong VEGFR-2 inhibitor, with an IC50 value of 0.23 μM. VEGFR-2-IN-85 exhibits potent cytotoxic activity against multiple cancer cell lines with minimal toxicity toward normal cells. VEGFR-2-IN-85 also impairs cancer cell migration, likely through modulation of the VEGFR-2/p-Akt pathway. VEGFR-2-IN-85 can induce apoptosis through modulation of Caspase-3, Bax and Bcl-2. VEGFR-2-IN-85 arrests cell cycle at the G2/M phase and has anti-angiogenic activity. VEGFR-2-IN-85 is a targeted radiosensitizer enhancing radiation-induced cytotoxicity. VEGFR-2-IN-85 can be used for research on cancers such as non-small cell lung cancer, breast cancer, and liver cancer[1].

IC50 & Target[1]

VEGFR-2

0.23 μM (IC50)

In Vitro

VEGFR-2-IN-85 (compound 9a) (48 h) exhibits IC50s of 5.02 μM, 4.78 μM, 4.13 μM, 95.87 μM and 62.95 μM in A549, MDA-MB-231, HepG-2, WI-38 and MCF10A cell lines, respectively[1].
VEGFR-2-IN-85 (4.13 μM; 48 h) can effectively interfere with cellular migration associated with angiogenic signaling in HepG-2 cells[1].
VEGFR-2-IN-85 (4.13 μM; 24 h) reduces p-Akt expression in HepG-2 cells, confirming inhibition of VEGFR-2-mediated signaling[1].
VEGFR-2-IN-85 (4.13 μM; 48 h) substantially modulates apoptosis-related markers in HepG-2 cells, emphasized by caspase-3 activation, Bax upregulation and Bcl-2 suppression[1].
VEGFR-2-IN-85 (4.13 μM; 24 h) disrupts cell cycle progression at the G2/M checkpoint in HepG-2 cells, preventing completion of mitosis and limiting proliferation[1].
VEGFR-2-IN-85 (48 h) effectively enhances gamma-induced cytotoxicity in malignant cells while exerting much lower impact on normal cells, with IC50s of 2.10 μM in A549 cells, 1.89  μM in MDA-MB-231 cells, 1.75 μM in HepG-2 cells and 68.74  μM in WI-38 cells[1].

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

VEGFR-2-IN-85 Related Antibodies

Cell Migration Assay [1]

Cell Line: HepG-2 cells
Concentration: 4.13 μM
Incubation Time: 48 h
Result: Limited wound closure to 56.30%, compared with 97.04% in control group.

Western Blot Analysis[1]

Cell Line: HepG-2 cells
Concentration: 4.13 μM
Incubation Time: 24 h
Result: Decreased p-Akt level compared with control cells, indicating effective suppression of Akt phosphorylation.

Apoptosis Analysis[1]

Cell Line: HepG-2 cells
Concentration: 4.13 μM
Incubation Time: 48 h
Result: Upregulated the expression of Caspase-3 and Bax.
Suppressed the expression of Bcl-2.

Cell Cycle Analysis[1]

Cell Line: HepG-2 cells
Concentration: 4.13 μM
Incubation Time: 24 h
Result: Increased the proportion of G2/M cells from 1.35% in untreated controls to 9.57%.
Decreased the G0/G1 population from 87.14% to 78.13%.
Slightly elevated the S phase fraction (12.21% vs. 11.84% in control).
Molecular Weight

574.60

Formula

C25H23FN4O7S2
SMILES

COC1=C(C(OC)=C2N=C(N(C(C2=C1)=O)C3=CC=C(C=C3)S(N)(=O)=O)SCC(NC4=CC=CC=C4F)=O)OC
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-85 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-85VEGFRApoptosisVascular endothelial growth factor receptorVEGFR-2 inhibitorcytotoxic activityVEGFR-2/p-Akt pathwayapoptosisarrest cell cycletargeted radiosensitizernon-small cell lung cancerbreast cancerliver cancerInhibitorinhibitorinhibit

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