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VEGFR-2/P-gp-IN-1

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Catalog No. T211172

VEGFR-2/P-gp-IN-1 is a derivative of Licochalcone A, functioning as an orally active inhibitor of VEGFR-2 (IC50= 0.885 μM) and P-glycoprotein (P-gp). It combats tumor proliferation and overcomes chemotherapy resistance by simultaneously inhibiting VEGFR-2 kinase activity and the P-gp drug efflux pump. This compound suppresses the phosphorylation of VEGFR-2 and proteins in the downstream PI3K/AKT signaling pathway, induces apoptosis, arrests cells in the S phase, and inhibits invasive migration. Additionally, VEGFR-2/P-gp-IN-1 demonstrates potent in vivo antitumor activity in HeLa/DDP cell xenograft models and is applicable in cervical cancer research.

VEGFR-2/P-gp-IN-1

VEGFR-2/P-gp-IN-1

😃Good
Catalog No. T211172
VEGFR-2/P-gp-IN-1 is a derivative of Licochalcone A, functioning as an orally active inhibitor of VEGFR-2 (IC50= 0.885 μM) and P-glycoprotein (P-gp). It combats tumor proliferation and overcomes chemotherapy resistance by simultaneously inhibiting VEGFR-2 kinase activity and the P-gp drug efflux pump. This compound suppresses the phosphorylation of VEGFR-2 and proteins in the downstream PI3K/AKT signaling pathway, induces apoptosis, arrests cells in the S phase, and inhibits invasive migration. Additionally, VEGFR-2/P-gp-IN-1 demonstrates potent in vivo antitumor activity in HeLa/DDP cell xenograft models and is applicable in cervical cancer research.
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Product Introduction

Bioactivity
Description
VEGFR-2/P-gp-IN-1 is a derivative of Licochalcone A, functioning as an orally active inhibitor of VEGFR-2 (IC50= 0.885 μM) and P-glycoprotein (P-gp). It combats tumor proliferation and overcomes chemotherapy resistance by simultaneously inhibiting VEGFR-2 kinase activity and the P-gp drug efflux pump. This compound suppresses the phosphorylation of VEGFR-2 and proteins in the downstream PI3K/AKT signaling pathway, induces apoptosis, arrests cells in the S phase, and inhibits invasive migration. Additionally, VEGFR-2/P-gp-IN-1 demonstrates potent in vivo antitumor activity in HeLa/DDP cell xenograft models and is applicable in cervical cancer research.
In vitro
VEGFR-2/P-gp-IN-1 (Compound A20) significantly inhibits the proliferation of cervical cancer cells, including resistant strains, at concentrations of 1-100 μM over 48 hours. This compound, applied at 1-6 μM for 24 hours, overcomes cervical cancer resistance by dual-targeting the inhibition of VEGFR-2 phosphorylation and P-gp efflux functionality. In the HeLa/DDP cell line, VEGFR-2/P-gp-IN-1 at 1-4 μM for 24 hours induces cancer cell apoptosis, blocks cell cycle progression in the S phase to inhibit proliferation, and significantly restrains cancer cell invasion and migration.
In vivo
VEGFR-2/P-gp-IN-1 (Compound A20), administered orally at doses of 10 mg/kg, 20 mg/kg, and 40 mg/kg once daily for 14 days, demonstrates potential in treating cisplatin-resistant cervical cancer within a HeLa/DDP cell xenograft mouse model. It also exhibits a favorable safety profile, showing no significant toxicity.
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Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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