Ozekibart  (Synonyms: INBRX-109)

Ozekibart (INBRX-109) is a DR5 agonist and antitumor agent with a human DR5 IC₅₀ of 0.17 nmol/L and human DR5 K_a of 0.11 nmol/L. Ozekibart can be used for the research of unresectable/metastatic chondrosarcoma^[1].

[G1 VH-VH-h-CH2-CH3]-dimer

Human IgG1 kappa, Isotype Control

Human

TNFRSF10B/TRAILR2/CD262

Ozekibart (0.00001-100 nmol/L; 1 hour at 4°C) binds specifically to DR5 expressed on DR5-transfected ExpiCHO-S cells with an apparent K_d of 0.107 nmol/L^[1].
Ozekibart (0.00001-100 nmol/L, with 3.5 nmol/L TRAIL; 1 hour at 4°C) competes with TRAIL for DR5 binding on DR5-transfected ExpiCHO-S cells with an IC₅₀ of 0.17 nmol/L^[1].
Ozekibart (0.00001-100 nmol/L, with 50 μmol/L Z-VAD-FMK; 5.5 hours at 37°C) does not mediate ADCC activity against DR5-transfected ExpiCHO-S cells in a Jurkat CD16a^V158 ADCC reporter assay^[1].
Ozekibart (10 μg/mL; overnight at 4°C for immobilization, 1 hour at room temperature for complement serum incubation) does not bind complement component C1q, confirming lack of CDC activity^[1].
Ozekibart (titrated concentrations; 1 hour at room temperature) binds specifically to human DR5, with no cross-reactivity to DR4, Decoy R1, or Decoy R2 in an ELISA binding assay^[1].
Ozekibart (0.0001-100 nmol/L; 16 hours) induces caspase-dependent cytotoxicity in H-EMC-SS chondrosarcoma cells with an EC₅₀ of 3.3 pmol/L^[1].
Ozekibart (0.0001-100 nmol/L; 16 hours, imaged every 30 minutes) induces rapid, caspase-dependent activation of caspase-3/7 in H-EMC-SS chondrosarcoma cells^[1].
Ozekibart (tested concentrations; 20 minutes at 37°C, 5% CO₂ followed by 42 hours incubation with media or 10 mg/mL IVIG) does not induce significant hepatotoxicity in HepaRG hepatic progenitor cells, even in the presence of IVIG as a source of preexisting antidrug antibodies^[1].
Ozekibart (0.000001-10 nmol/L; 7 days) does not induce cytotoxicity in 3D human liver microtissues at concentrations up to 10 nmol/L after 7 days of treatment^[1].

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

8795  [NCBI]

O14763

ELISA, FACS, Functional assay

Unconjugated

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

105.46 kDa

2539847-03-3

Liquid

Colorless to light yellow

[Ozekibart]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

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

• 
  (VH-VH-h-CH2-CH3)2_S

• 
  Flow Cytometry analysis of HepG2 cells with Ozekibart (HY-P990715, red) . Cells were fixed with 4% paraformaldehyde and permeabilised with 90% methanol. Then cells were stained with the primary antibody at 1/200 dilution for an hour at 4℃. Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG1 kappa(HY-P99001, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).

• [1]. Subbiah V, et al. Preclinical Characterization and Phase I Trial Results of INBRX-109, A Third-Generation, Recombinant, Humanized, Death Receptor 5 Agonist Antibody, in Chondrosarcoma. Clin Cancer Res. 2023;29(16):2988-3003.  [Content Brief]