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

Rhamnazin Chemical Structure

CAS No. : 552-54-5

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Rhamnazin

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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.
Appearance

Solid

Color

Off-white to light yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (302.76 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0276 mL 15.1382 mL 30.2764 mL
5 mM 0.6055 mL 3.0276 mL 6.0553 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.00%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0276 mL 15.1382 mL 30.2764 mL 75.6911 mL
5 mM 0.6055 mL 3.0276 mL 6.0553 mL 15.1382 mL
10 mM 0.3028 mL 1.5138 mL 3.0276 mL 7.5691 mL
15 mM 0.2018 mL 1.0092 mL 2.0184 mL 5.0461 mL
20 mM 0.1514 mL 0.7569 mL 1.5138 mL 3.7846 mL
25 mM 0.1211 mL 0.6055 mL 1.2111 mL 3.0276 mL
30 mM 0.1009 mL 0.5046 mL 1.0092 mL 2.5230 mL
40 mM 0.0757 mL 0.3785 mL 0.7569 mL 1.8923 mL
50 mM 0.0606 mL 0.3028 mL 0.6055 mL 1.5138 mL
60 mM 0.0505 mL 0.2523 mL 0.5046 mL 1.2615 mL
80 mM 0.0378 mL 0.1892 mL 0.3785 mL 0.9461 mL
100 mM 0.0303 mL 0.1514 mL 0.3028 mL 0.7569 mL
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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.

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Rhamnazin
Cat. No.:
HY-N8342
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