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Nivolumab (BMS-936558)

Catalog No.GC34218

Nivolumab (BMS-936558) Chemical Structure

A PD-1 antibody inhibitor

Size Price Stock Qty
1mg
$103.00
In stock
10mg
$556.00
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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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Protocol

Cell Experiment

Cell lines PBMCs
Preparation method In a cytomegalovirus (CMV)-restimulation assay, 2 × 10^5 PBMCs from a CMV-positive donor (Astarte) were stimulated using lysate of CMV-infected cells (Astarte), with serial dilutions of nivolumab added at the initiation of the assay. After 4 days, supernatants were assayed for IFNγ.
Concentrations 0-10 μM
Incubation time 4 days

Animal Experiment

Animal models Cynomolgus monkeys (Macaca fascicularis)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Kmfactor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg

Background

Nivolumab is a programmed death-1 (PD-1) blocking antibody used to treat advanced (metastatic) non-small cell lung cancer.

Nivolumab binds to PD-1-expressing CHO cells with an EC50 of 1.66 nM, but not to the parental CHO cell line. Nivolumab binds to PD-1 on activated T cells with EC50 of 0.64 nM. Nivolumab also inhibits the interaction between PD-1 and its ligands PD-L1 and PD-L2 with IC50 values of 2.52 and 2.59 nM, respectively. Nivolumab (1.5 ng/mL) enhances T cell responsiveness in the presence of T cell receptor stimulation [1].

Nivolumab (10 and 50 mg/kg, i.v.) was well tolerated in cynomolgus monkeys. In females treated with 50 mg/kg, serum chemistry changes were limited to a 28% reversible reduction in T3 at week 13. T4 and TSH levels were unchanged. There were no changes in T3, T4 or TSH levels in males treated with 50 mg/kg. Nivolumab exposure increased in a roughly dose-proportional manner between 10 and 50 mg/kg, with no significant gender differences [1].

References:
[1]. Wang C, et al. In vitro characterization of the anti-PD-1 antibody nivolumab, BMS-936558, and in vivo toxicology in non-human primates. Cancer Immunity Research. 2014 Sep;2(9):846-56.

Chemical Properties

Cas No. 946414-94-4 SDF
Synonyms BMS-936558, ONO-4538, MDX-1106
Chemical Name N/A
Canonical SMILES [Nivolumab]
Formula N/A M.Wt 143599.09
Solubility N/A Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 33 reference(s) in Google Scholar.)

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