1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    PDGFR
  3. Vorolanib

Vorolanib (Synonyms: CM082; X-82)

Cat. No.: HY-109019 Purity: 99.80%
Handling Instructions

Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).

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

Vorolanib Chemical Structure

Vorolanib Chemical Structure

CAS No. : 1013920-15-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895)[1][2].

In Vitro

Vorolanib (CM082; 1-100 μM) can specifically enhance the sensitivity of a substrate chemotherapeutical agent in overexpressing ABCG2 cells, but not in overexpressing ABCB1 cells. Vorolanib (1.25, 2.5, 5.0, 20 μM) does not influence the expression of ABCG2 in mRNA or protein Levels[1].
Vorolanib (0.001-10 μM) inhibits the growth of VEGF‐stimulated HUVECs (IC50=0.031 μM) and FBS‐stimulated HUVEC growth (IC50=29.9 μM)[2].
Vorolanib (0.01, 0.1, 1 μM) exhibits a concentration‐dependent inhibition on VEGF‐induced (40 ng/mL) phosphorylation of VEGFR2 and its downstream signaling molecules ERK1/2, AKT, and STAT3 in HUVECs. Vorolanib (0.1, 1 μM) inhibits FBS‐stimulated tube formation and cell migration of HUVECs in a concentration‐dependent manner[2].

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

In Vivo

Vorolanib (CM082; 20 mg/kg; gavage; once every 2 days; 1 h before SKF 104864A; for 23 days) enhances the anti-tumor effect of SKF 104864A (HY-13768; 2 mg/kg; i.p.; once every 2 days) on xenografts of ABCG2-overexpressing cells (nude mice aged 5-6 weeks and weighing 15-17 g constructed by injecting H460/MX20 cells). There is no significant difference in the tumor weight and size among the control group, the SKF 104864A group, and the Vorolanib group[1].
Vorolanib (80 mg/kg; twice daily; for 21 days) has antitumor activity combined with ZD1839 (10 mg/kg; q.d; for 21 days) on H3255 tumor xenograft (female BALB/c nude mice aged five weeks)[2].

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

Clinical Trial
Molecular Weight

439.48

Formula

C₂₃H₂₆FN₅O₃

CAS No.

1013920-15-4

SMILES

O=C1/C(C2=CC(F)=CC=C2N1)=C/C(NC(C)=C3C(N[[email protected]@H]4CN(C(N(C)C)=O)CC4)=O)=C3C

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 : 27 mg/mL (61.44 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2754 mL 11.3771 mL 22.7542 mL
5 mM 0.4551 mL 2.2754 mL 4.5508 mL
10 mM 0.2275 mL 1.1377 mL 2.2754 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.25 mg/mL (5.12 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.80%

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Keywords:

VorolanibCM082 X-82CM 082CM-082X82X 82X-82VEGFRPDGFRVascular endothelial growth factor receptorPlatelet-derived growth factor receptororallyATP-bindingcassetteABCtransporterangiogenesisABCG2HUVECstyrosinekinaseTKIInhibitorinhibitorinhibit

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