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Cat. No. M6104
Ipilimumab Structure

MDX-010, BMS-734016;Yervoy

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5mg USD 1550  USD1550 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: Ipilimumab, is a fully humanized IgG1k monoclonal antibody produced by recombinant DNA technology in a CHO mammalian cell expression system, binding with high affinity to the extracellular domain of human (and Cynomolgus monkey) CTLA-4, and acting as an inhibitor of its complex functions. This essentially results in T-cell activation and proliferation, and in lymphocyte infiltration leading to tumor cell death. However, the enhancement of T effector cell function, combined with the inhibition of CD4+ Treg and CD8+ suppressive cell types, are considered essential for mediating the full therapeutic effects of ipilimumab. Ipilimumab can improve ATC proliferation, enhance the BiAb-mediated tumor-specific cytotoxicity, and increase cytokine synthesis, while it attenuates Treg activity as shown by decreased level of IL-10 secretion and reduced Treg population. Ipilimumab and nivolumab treatments could collaboratively enhance effector and memory T cell responses without inappropriately activating naive T cells.

In vivo: Ipilimumab is shown in phase III clinical trials to have a survival benefit in metastatic melanoma that is durable in 10% to 20% of patients. Conceivably, the main adverse effects of ipilimumab are autoimmunein nature. Ipilimumab enhances antitumor immunity by inhibiting immunosuppressive activity of regulatory T cells (Treg).

Cell Experiment
Cell lines PBMCs
Preparation method Add ipilimumab at the initiation of ATC expansion cultures from healthy donors at various concentrations ranging from 0 to 50 μg/mL. ATC(activated T cells) are harvested on day 14, armed with EGFRBi or CD20Bi, and co-cultured at 25:1 E:T(effector:target) ratio for 18 hours with EGFR positive pancreatic cancer cell line (COLO356/FG) or 4 hours with CD20 positive Burkitt's lymphoma cell line (Daudi) for cytotoxicity assay. BiAb-mediated tumor specific cytotoxicity is measured by 51Cr release assay.
Concentrations 0, 0.5, 5.0, and 50 μg/mL
Incubation time 14 days
Animal Experiment
Animal models Purpose-bred cynomolgus monkeys
Formulation Saline
Dosages 3 mg/kg or 10 mg/kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 148631.92
Formula C6742H9972N1732O2004S40
CAS Number 477202-00-9
Purity >98%
Storage -80°C for long term

[1] Wai Nam Liu, et al. Cancers (Basel). Establishment and Characterization of Humanized Mouse NPC-PDX Model for Testing Immunotherapy

[2] Antonia SJ, et al. Lancet Oncol. Nivolumab alone and nivolumab plus ipilimumab in recurrent small-cell lung cancer (CheckMate 032): a multicentre, open-label, phase 1/2 trial.

[3] Pascale Bardo-Brouard, et al. Eur J Cancer. Stability of ipilimumab in its original vial after opening allows its use for at least 4 weeks and facilitates pooling of residues

[4] Robert C, et al. N Engl J Med. Pembrolizumab versus Ipilimumab in Advanced Melanoma.

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Keywords: Ipilimumab, MDX-010, BMS-734016;Yervoy supplier, Checkpoint, inhibitors

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