Conbercept  (Synonyms: KH902)

Conbercept (KH902) is a recombinant fusion protein composed of VEGFR-1 (second domain) and VEGFR-2 (third and fourth domains) regions fused to human IgG1 Fc. Conbercept is a VEGF inhibitor (IC₅₀ = 8.8 pM) and is a soluble receptor decoy that blocks all isoforms of VEGF-A (K_d = 0.5 pM), VEGF-B (K_d = 8 pM), VEGF-C, and PlGF (K_d = 5 pM). Conbercept has anti-inflammatory effects, can lower the levels of VEGF, TNF-α and IL-6, and reduce the infiltration of inflammatory cells. Conbercept decreases tumor growth in several oncology studies. Conbercept can be used for various eye diseases such as polypoidal choroidal vasculopathy (PCV), diabetic macular edema (DME) and pathologic myopia choroidal neovascularization (pmCNV)^{[1][2][3][4][5]}.

Conbercept (0-586.9 pM, 4 d) shows an inhibition effect on VEGF-induced HUVEC proliferation with an EC₅₀ value of 28 pM^[3][5].
Conbercept inhibits VEGF-induced HUVEC migration and tube formation and suppressed the high glucose-induced migration and sprouting of human retinal endothelial cells^[3].

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

Conbercept (10 mg/kg, i,v., once every other day for 2 weeks) significantly reduces the paw edema volume and the arthritis index in type II Collagen (HY-NP010)-induced rat rheumatoid arthritis (CIA) model^[1].
Conbercept (10-50 mg/kg, i,v., single dose) significantly inhibits xylene-induced ear edema in mice^[1].
Conbercept (0.64 mg, 40 μL, intravitreally injection, 4 times a week or 2 times every 2 weeks, for 2 weeks) has an inhibitory effect against VEGF over the course of 81 days in rabbit^[3].
Conbercept (0.5 mg, intravitreally injection, single dose) is effective to prevent the formation of experimental choroidal neovascularization (CNV) and also to treat preexisted CNV without evidence of toxicity in monkey model^[3][5].
Conbercept inhibits tumor growth in human hepatocellular carcinoma (HepG2), breast cancer (MCF-7), gastric carcinoma (A549), and colorectal cancer (LoVo) tumor xenograft models^[3].

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

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

117.45 kDa

1227158-72-6

Liquid

Colorless to light yellow

[Conbercept]

Shipping with dry ice.

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

• 
  [FLT1 (fms-related tyrosine kinase 1, vascular endothelial growth factor receptor 1, VEGFR-1, VEGFR, FLT, FRT, vascular permeability factor receptor)-KDR (kinase insert domain receptor, vascular endothelial growth factor receptor 2, VEGFR2, VEGF-R2, FLK1, CD309)]2-IGHG1 Fc (Fragment constant)

• 
  Immobilized VEGF165 Protein, Human can bind Conbercept. The EC₅₀ for this effect is 4.31 ng/mL.

• [1]. Liu Y, Fu H, Zuo L. Anti-inflammatory activities of a new VEGF blocker, Conbercept. Immunopharmacol Immunotoxicol. 2021 Oct;43(5):594-598.  [Content Brief]

  [2]. Liu H, et al. Updates on the Management of Ocular Vasculopathies with VEGF Inhibitor Conbercept. Curr Eye Res. 2020 Dec;45(12):1467-1476.  [Content Brief]

  [3]. Lu X, Sun X. Profile of conbercept in the treatment of neovascular age-related macular degeneration. Drug Des Devel Ther. 2015 Apr 22;9:2311-20.  [Content Brief]

  [4]. de Oliveira Dias JR, et al. Fusion proteins for treatment of retinal diseases: aflibercept, ziv-aflibercept, and conbercept. Int J Retina Vitreous. 2016 Feb 1;2:3.  [Content Brief]

  [5]. Zhang M, et al. The pharmacology study of a new recombinant human VEGF receptor-fc fusion protein on experimental choroidal neovascularization. Pharm Res. 2009 Jan;26(1):204-10.  [Content Brief]