1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. Rhamnazin

Rhamnazin is an orally active inhibitor of VEGFR2 signaling with an IC50 of 4.68 μM against VEGFR2 kinase. Rhamnazin shows potent antiangiogenic activity and antitumor efficacy. Rhamnazin shows antioxidant and anti-inflammatory properties.

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Rhamnazin Chemical Structure

Rhamnazin Chemical Structure

CAS No. : 552-54-5

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Description

Rhamnazin is an orally active inhibitor of VEGFR2 signaling with an IC50 of 4.68 μM against VEGFR2 kinase. Rhamnazin shows potent antiangiogenic activity and antitumor efficacy[1]. Rhamnazin shows antioxidant and anti-inflammatory properties[2].

IC50 & Target[1]

VEGFR2

4.68 μM (IC50)

In Vitro

Rhamnazin (5-40 μM) inhibits proliferation, migration and tube formation of HUVECs induced by VEGF[1].
Rhamnazin (0-20 μM) attenuates VEGFR-2 tyrosine kinase activity and VEGFR-2 signaling pathway[1].
Rhamnazin (0-40 μM; 24 h) inhibits the proliferation and VEGFR2 signaling pathway of breast cancer cells[1].

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

Cell Migration Assay [1]

Cell Line: HUVECs
Concentration: 0, 10, 15 and 20 μM
Incubation Time: 6 h
Result: Strongly inhibited the migration of HUVECs.

Western Blot Analysis[1]

Cell Line: HUVECs
Concentration: 0, 10, 15 and 20 μM
Incubation Time: 24 h
Result: Decreased VEGF binding to VEGFR2. Reduced VEGF-stimulated phosphorylation of VEGFR2 and its downstream MAPK, AKT, and STAT3 in HUVECs in a concentrationdependent manner.

Cell Proliferation Assay[1]

Cell Line: HCC1937, T-47D, SK-BR-3, MCF-7 and MDA-MB-231
Concentration: 0, 10, 15, 20, 30 and 40 μM
Incubation Time: 24 h
Result: Inhibited cell growth with IC50s of 19, 27, 32, 41 and 64 μM against MDA-MB-231, MCF-7, SK-BR-3, T-47D and HCC1937 in the presence of VEGF, respectively.
In Vivo

Rhamnazin (200 mg/kg; i.g.; daily for 25 days) inhibits breast cancer growth and angiogenesis in mice[1].
Rhamnazin (5-20 mg/kg; i.p.; once) shows strong antioxidant and anti-inflammatory properties in the rat acute lung injury model[2].

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

Animal Model: BALB/c nude mice, breast cancer xenograft model[1]
Dosage: 200 mg/kg
Administration: Intragastric administration, daily for 25 days
Result: Dramatically suppressed tumor volumes by 47% compared with the vehicle group. Showed a significant reduction of pVEGFR2Tyr951-positive cells in tumors. Resulted in downregulation of VEGFR2 downstream molecules phosphorylation including MAPK, AKT and STAT3.
Molecular Weight

330.29

Formula

C17H14O7

CAS No.
SMILES

O=C1C(O)=C(C2=CC=C(O)C(OC)=C2)OC3=CC(OC)=CC(O)=C13

Structure Classification
Initial Source
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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    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.

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Rhamnazin
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HY-N8342
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