Disitamab vedotin

Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) and a HER2-targeted cytotoxic agent, consisting of an anti-HER2 monoclonal antibody conjugated to MMAE via a cleavable linker, used for the treatment of HER2-expressing solid tumors including gastric cancer, breast cancer, and urothelial carcinoma.

JIMT-1 cells:0.05 µg/mL, EFM-192A cells:0.033 µg/mL, N87 cells:0.028 µg/mL, BT-474 cells:0.033 µg/mL, UACC-812 cells:0.012 µg/mL, RN87 cells:0.239 µg/mL, OE19 cells:0.038 µg/mL, SKBR3 cells:0.007 µg/mL

Methods: Cell proliferation counting, cell cycle, and apoptosis detection assays were used. HER2-positive breast cancer cells BT474, SKBR3, HCC1954, HCC1419 and their drug-resistant sublines were selected and incubated with Disitamab vedotin at concentrations of 0.001–10 nM for 3 days.
Results: Disitamab vedotin significantly inhibited cell proliferation, induced G2/M phase arrest and apoptosis, efficiently released cytotoxic payload, and maintained strong activity in T-DM1, lapatinib, and neratinib-resistant cells.[1]
Methods: Transcriptome sequencing and qPCR experiments were used to detect the in vitro activity of Disitamab vedotin. Bladder cancer cells SW780 and 5637 were selected and incubated with 25 μg/mL Disitamab vedotin for 48 hours.
Results: Disitamab vedotin significantly upregulated the expression of core genes including TNF, IL1B, and CXCL8. Differentially expressed genes were mainly enriched in TNF signaling pathway and NF-κB signaling pathway, confirming that it exerts its effects by regulating the TNF pathway.[2]

Methods: Female SCID mice were used to establish an L-JIMT-1 breast cancer lung metastasis model. 1×10⁵ L-JIMT-1 cells were injected via tail vein, and a single dose of Disitamab vedotin (5 mg/kg) was administered via tail vein at week 8, with PBS as the control vehicle.
Results: Disitamab vedotin significantly inhibited the growth of lung metastases, reduced the number of metastases and decreased lesion diameter, showed superior efficacy to T-DM1 and T-DXd, prolonged mouse survival, and demonstrated prominent in vivo antitumor activity.[3]

CHO

Human

Immobilized Human HER2/ERBB2 Protein (His) (TMPJ-00778) at 1 μg/mL can bind Disitamab vedotin. The EC50 is 6.210 ng/mL.

Monoclonal

MMAE