CA IX/VEGFR-2-IN-2 

CA IX/VEGFR-2-IN-2 (compound 5e) is a dual-targeted inhibitor. CA IX/VEGFR-2-IN-2 shows strong inhibitory effects on both CA IX (K_i=3.1 μM) and VEGFR-2 (IC₅₀=32.1 nM). CA IX/VEGFR-2-IN-2 can be used for the study of pancreatic (PANC1), breast cancer (MCF7) and prostate cancer (PC3) ^[1].

CA IX/VEGFR-2-IN-2 (compound 5e) has the sequence of the selectivity toward the responsive tumor cells is PANC1, then MCF7 and PC3, and decreases PANC1 cell migration^[1].
CA IX/VEGFR-2-IN-2 (compound 5e) induces up-regulation of p53, BAX, cytochrome C and caspases 3, 8, 9, and down-regulation of Bcl-2 gene in pancreatic cancer cells^[1].
CA IX/VEGFR-2-IN-2 (compound 5e) suppresses the HIF-1α from 6.1±0.13 to 3.7±0.09 ng/mL by more than 1.5-fold in PANC1 cells^[1].
CA IX/VEGFR-2-IN-2 (compound 5e) is responsible for more than a 3.5-fold rise in the quantity of ROS to blame for seen cell cycle halt, or apoptosis, in PANC1 cells^[1].

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

CA IX/VEGFR-2-IN-2 (compound 5e) (5 and 10 mg/kg, ip.; 2 weeks) is more efficacious in reducing tumor volume and weight than the standard drug DOX at a dose of 10 mg/kg in female Swiss albino mice^[1].
CA IX/VEGFR-2-IN-2 (compound 5e) (5 and 10 mg/kg, ip.; 2 weeks) at a dosage of 10 mg/kg leads to additional decreases in the concentrations of VEGF, MMP-2, and MMP-9 in female Swiss albino mice^[1].
CA IX/VEGFR-2-IN-2 (compound 5e) (5 and 10 mg/kg, ip.; 2 weeks) at a dosage of 5 mg/kg leads to the formation of necrotic regions interspersed with distinct neoplastic cells and at a dosage of 10 mg/kg displays marked improvement, and diffuse and wide areas of necrosis were replaced in the muscle bundles with a marked decline in the quantity of neoplastic cells, indicating a substantial inhibition in viable tumor cells in female Swiss albino mice^[1].

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

423.46

C₂₂H₁₈FN₃O₃S

O=C1C(/C(C)=N/NC2=NC(C3=CC=C(F)C=C3)=CS2)=CC4=C(O1)C(OCC)=CC=C4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Hefny S M, et al. Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In Silico Investigations of Coumarin-Based Thiazoles[J]. Journal of Medicinal Chemistry, 2024.  [Content Brief]