Vorolanib

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).

Product information

CAS Number: 1013920-15-4

Molecular Weight: 439.48

Formula: C23H26FN5O3

Chemical Name: N-[(3S)-1-(dimethylcarbamoyl)pyrrolidin-3-yl]-5-{[(3E)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide

Smiles: CN(C)C(=O)N1C[C@H](CC1)NC(=O)C1C(C)=C(/C=C2\C3=CC(F)=CC=C3NC\2=O)NC=1C

InChiKey: KMIOJWCYOHBUJS-ADFUCPMPSA-N

InChi: InChI=1S/C23H26FN5O3/c1-12-19(10-17-16-9-14(24)5-6-18(16)27-21(17)30)25-13(2)20(12)22(31)26-15-7-8-29(11-15)23(32)28(3)4/h5-6,9-10,15,25H,7-8,11H2,1-4H3,(H,26,31)(H,27,30)/b17-10+/t15-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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. 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).

Products are for research use only. Not for human use.