Vorolanib free base · Synonyms: CM-082 | X-82 | CPDA601859

Vorolanib is an orally active, potent multikinase VEGFR/PDGFR inhibitor.

For research use only. Not for human or veterinary use.

Target VEGFR PDGFR

Research area Cardiovascular Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Vorolanib structure

CAS No.: 1013920-15-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 485.00	BP-01825-250mg	In stock	Get quote
500 mg	USD 785.00	BP-01825-500mg	In stock	Get quote
1 g	USD 1,185.00	BP-01825-1g	In stock	Get quote

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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.

Biological activity

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. ? 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). ? 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.

Identifiers

SMILES: O=C1/C(C2=CC(F)=CC=C2N1)=C/C(NC(C)=C3C(N[C@@H]4CN(C(N(C)C)=O)CC4)=O)=C3C
InChIKey: KMIOJWCYOHBUJS-ADFUCPMPSA-N

Specifications

MW (average): 439.4826
Formula: C₂₃H₂₆FN₅O₃
CAS No.: 1013920-15-4
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month.

Solubility

Soluble in DMSO : 27 mg/mL

Documents

References

[1]. Lejia Xu, et al. CM082 Enhances the Efficacy of Chemotherapeutic Drugs by Inhibiting the Drug Efflux Function of ABCG2. Mol Ther Oncolytics. 2019 Dec 27;16:100-110.

[2]. Kun Zhang, et al. CM082, a novel angiogenesis inhibitor, enhances the antitumor activity of ZD1839 on epidermal growth factor receptor mutant non-small cell lung cancer in vitro and in vivo. Thorac Cancer. 2020 Jun;11(6):1566-1577.

Same target

Search VEGFR

Same research area

Search Cardiovascular Disease