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Nivolumab (BMS-936558) Catalog No.GC34218

A PD-1 antibody inhibitor

Size Price Stock Qty
1mg
$103.00
In stock
10mg
$556.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

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

Chemical Properties

Cas No. 946414-94-4 SDF Download 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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Background

Nivolumab 是一种程序性死亡受体-1 (PD-1) 阻断抗体,用于治疗晚期(转移性)非小细胞肺癌。

Nivolumab 与表达 PD-1 的 CHO 细胞结合,EC50 为 1.66 nM,但不与亲本 CHO 细胞系结合。Nivolumab 与活化 T 细胞上的 PD-1 结合,EC50 为 0.64 nM。Nivolumab 还抑制 PD-1 与其配体 PD-L1 和 PD-L2 之间的相互作用,IC50 值分别为 2.52 和 2.59 nM。Nivolumab (1.5 ng/mL) 可在存在 T 细胞受体刺激时增强 T 细胞反应性[1]。

Nivolumab(10 和 50 mg/kg,静脉注射)在食蟹猴中具有良好的耐受性。在用 50 mg/kg 治疗的雌性中,血清化学变化仅限于在第 13 周时 T3 可逆性降低 28%。T4 和 TSH 水平没有变化。在用 50 mg/kg 治疗的雄性中,T3、T4 或 TSH 水平没有变化。Nivolumab 暴露量在 10 至 50 mg/kg 之间以大致与剂量成比例的方式增加,没有明显的性别差异[1]。

[1]。王 C,等。抗 PD-1 抗体 nivolumab、BMS-936558 的体外表征和非人类灵长类动物的体内毒理学。癌症免疫研究。2014 年 9 月;2(9):846-56。