2. Protein Tyrosine Kinase/RTK Membrane Transporter/Ion Channel Apoptosis
  3. VEGFR P-glycoprotein Apoptosis
  4. VEGFR-2/P-gp-IN-1

VEGFR-2/P-gp-IN-1, a Licochalcone A (HY-N0372) derivative, is an orally active VEGFR-2 (IC50 = 0.885 μM) and P-gp inhibitor. VEGFR-2/P-gp-IN-1 achieves anti-tumor proliferation and overcomes chemotherapy resistance by synchronously inhibiting VEGFR-2 kinase activity and P-gp drug efflux pump function. VEGFR-2/P-gp-IN-1 inhibits phosphorylation of VEGFR-2 and downstream PI3K/AKT signaling pathway proteins, induces apoptosis, blocks cells in the S phase, and inhibits invasive migration. VEGFR-2/P-gp-IN-1 exerts potent in vivo anti-tumor effects in the HeLa/DDP cell xenograft tumor model. VEGFR-2/P-gp-IN-1 is used in cervical cancer research.

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VEGFR-2/P-gp-IN-1 Chemical Structure

VEGFR-2/P-gp-IN-1 Chemical Structure

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VEGFR-2/P-gp-IN-1 Related Antibodies

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Description

VEGFR-2/P-gp-IN-1, a Licochalcone A (HY-N0372) derivative, is an orally active VEGFR-2 (IC50 = 0.885 μM) and P-gp inhibitor. VEGFR-2/P-gp-IN-1 achieves anti-tumor proliferation and overcomes chemotherapy resistance by synchronously inhibiting VEGFR-2 kinase activity and P-gp drug efflux pump function. VEGFR-2/P-gp-IN-1 inhibits phosphorylation of VEGFR-2 and downstream PI3K/AKT signaling pathway proteins, induces apoptosis, blocks cells in the S phase, and inhibits invasive migration. VEGFR-2/P-gp-IN-1 exerts potent in vivo anti-tumor effects in the HeLa/DDP cell xenograft tumor model. VEGFR-2/P-gp-IN-1 is used in cervical cancer research[1].

In Vitro

VEGFR-2/P-gp-IN-1 (Compound A20) (1-100 μM, 48 h) significantly inhibits proliferation of cervical cancer cells (including drug-resistant strains)[1].

VEGFR-2/P-gp-IN-1 (1-6 μM, 24 h) overcomes cervical cancer drug resistance through dual-target inhibition of VEGFR-2 phosphorylation and P-gp efflux function[1].

VEGFR-2/P-gp-IN-1 (1-4 μM, 24 h) induces apoptosis through activation of apoptotic pathways, blocks cell cycle progression at S phase, and significantly suppresses invasion and migration in HeLa/DDP cells[1].

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

VEGFR-2/P-gp-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HeLa-DDP cells, HUVEC cells
Concentration: 1 μM, 2 μM, 4 μM, 6μM
Incubation Time: 24 h
Result: Dose-dependently inhibited VEGFR-2 and downstream PI3K/AKT phosphorylation.
Upregulated the pro-apoptotic protein Bax, downregulated the anti-apoptotic protein Bcl-2, and did not alter the expression level of P-gp protein.

Cell Viability Assay[1]

Cell Line: HeLa/DDP drugresistant cells, HeLa/PTX drugresistant cells, HeLa/ADR drugresistant cells
Concentration: 1.0 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
Incubation Time: 48 h
Result: Showed the most significant inhibitory activity against these three drug-resistant cervical cancer cell lines, with IC50 values of 3.69 μM (HeLa/DDP), 4.81 μM (HeLa/PTX), and 5.98 μM (HeLa/ADR), compared with HeLa cells, the resistance indices (RIs) were 1.16, 1.51, and 1.87, respectively.

Apoptosis Analysis[1]

Cell Line: HeLa/DDP cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Induced apoptosis in HeLa cells at a rate of 92.3% at a concentration of 4 μM.
Induced apoptosis in HeLa/DDP cells at a rate of 94.5% at a concentration of 4 μM.

Cell Cycle Analysis[1]

Cell Line: HeLa/DDP cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Induced S-phase arrest in HeLa cells at 39.32% at a concentration of 4 μM.
Induced S-phase arrest in HeLa/DDP cells at 39.04% at a concentration of 4 μM.

Immunofluorescence[1]

Cell Line: HeLa/DDP cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Reduced the fluorescence intensity of p-VEGFR-2 in HeLa/HeLa-DDP cells in a dose-dependent manner.

Cell Invasion Assay[1]

Cell Line: HeLa/DDP cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Reduced invasive potential of HeLa/DDP cells to 209, 142, and 54 cells at concentrations of 1, 2, and 4 μM.
Reduced invasive potential of HeLa cells to 360, 219, and 106 cells at concentrations of 1, 2, and 4 μM.

Cell Migration Assay [1]

Cell Line: HeLa/DDP cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Reduced penetration capacity of HeLa/DDP cells into the ventricular membrane to 268, 178, and 85 cells at concentrations of 1, 2, and 4 μM, respectively.
Reduced penetration capacity of HeLa cells through the ventricular membrane to 583, 286, and 226 cells at concentrations of 1, 2, and 4 μM.
In Vivo

VEGFR-2/P-gp-IN-1 (Compound A20) (10-40 mg/kg, i.g., daily for 14 days) demonstrates therapeutic potential against cisplatin-resistant cervical cancer in HeLa/DDP cell xenograft mouse models, with a favorable safety profile and no significant toxicity observed[1].

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

Animal Model: HeLa/DDP cell xenograft model established in BALB/C nude female mice (4-5 weeks)[1]
Dosage: 10 mg/kg, 20 mg/kg, 40 mg/kg
Administration: Daily intragastric gavage (i.g.), at the corresponding doses for 14 days.
Result: Suppressed grafted tumors by 70.9%, 72.2%, and 89.5% at doses of 10, 20, and 40 mg/kg (positive control sorafenib 20 mg/kg: 36.1% reduction).
Inhibited growth of drug-resistant cervical cancer xenografts dose-dependently via oral administration.
Maintained comparable body weight across all groups.
Animal Model: Female Kunming mice (5 weeks, 20-22 g)[1]
Dosage: 200 mg/kg
Administration: Daily intragastric gavage (i.g.), at the corresponding doses for 14 days.
Result: Caused no mortality or significant body weight changes versus controls in acute mouse toxicity testing.
Induced normal liver/kidney function without necrosis, structural disorder, or inflammatory infiltration in acute mouse toxicity testing.
Demonstrated safety at 200 mg/kg without significant toxicity.
Molecular Weight

502.45

Formula

C24H24F6N2O3
SMILES

COC1=C(C=C(C(O)=C1)C(/C=C/C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)=O)CN3CCN(CC3)C
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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/P-gp-IN-1 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/P-gp-IN-1VEGFRP-glycoproteinApoptosisVascular endothelial growth factor receptorP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243VEGFR-2Cisplatin-resistant cervical cancerHeLa cellsBALB/C nude miceInhibitorinhibitorinhibit

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