Home>>Denosumab

Denosumab (Synonyms: D03684; Denosumab; Denosumab (usan))

Catalog No.GC19535

Denosumab is a fully human IgG2 monovlonal antibody

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Denosumab Chemical Structure

Cas No.: 615258-40-7

Size Price Stock Qty
1mg
$165.00
In stock
5mg
$495.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

RAW 264.7, MCF-7 cells

Preparation Method

RAW 264.7 and MCF-7 cells were all cultured in Dulbecco’s Modified Eagle Medium (DMEM) solutions, into which 10% fetal bovine serum was added, while RAW 264.7 cells were co-cultured with MCF-7 cells in a non-contact system.

Reaction Conditions

1 mg/mL, 5 days

Applications

Denosumab inhibits MCF-7 cell line-induced spontaneous osteoclastogenesis, and the inhibition of denosumab was found to be more pronounced after MALAT1 downregulation and miR-124 overexpression

References:

[1]. Feng, Qi et al. Denosumab inhibits MCF-7 cell line-induced spontaneous osteoclastogenesis via the RANKL/MALAT1/miR-124 axis. Translational cancer research vol. 9,4 (2020): 2482-2491.

Background

Denosumab is a fully human IgG2 monovlonal antibody that binds human RANKL with a high affinity, exhibiting a dissociation equilibrium binding constant (Kd) of 3 pM as determined by immunoaffinity exclusion chromatography. Denosumab binds both soluble and membrane-bound primate RANKL but fails to recognize mouse or rat RANKL- a finding that is supported by sequence analysis of RANKL from diverse mammalian species. [2]

Initial screening of RANKL antibodies for in vivo bioactivity leveraged the crossreactivity of Denosumab with cynomolgus RANKL. Single-dose testing in cynomolgus monkeys revealed that infrequent dosing regimens in humans may be possible. The primary in vivo testing in primates accelerated the developmental timeframe of this molecule, which normally would have been preceded by extensive testing in animal models of bone loss in which recombinant OPG was active. [2]

Denosumab does not bind to other TNF family members, such as TRAIL, CD40 ligand (CD40L), TNFα and THFβ. Denosumab binds to the DE loop region of human RANKL, which is one of the surface loop structures that forms contacts with RANK on responding cells. Owing to the different terminology used for the loop regions, the human DE loop region corresponds to the CD loop regions of the murine RANKL structure. Both Denosumab and OPG-Fc bind to soluble or membrane-bound human RANKL and block it from binding to and oligomerizing its receptor, RANK. Denosumab, however, is more specific than human OPG-Fc because Denosumab recognizes only human and non-human primate RANKL, in contrast to OPG, which also binds to mouse and rat RANKL as well as TRAIL. [1,2]

References:
[1]. Feng, Qi et al. Denosumab inhibits MCF-7 cell line-induced spontaneous osteoclastogenesis via the RANKL/MALAT1/miR-124 axis.” Translational cancer research vol. 9,4 (2020): 2482-2491.
[2]. Lacey, David L et al. Bench to bedside: elucidation of the OPG-RANK-RANKL pathway and the development of Denosumab. Nature reviews. Drug discovery vol. 11,5 (2012): 401-19.

Chemical Properties

Cas No. 615258-40-7 SDF
Synonyms D03684; Denosumab; Denosumab (usan)
Formula C6404H9908N1724O2004S50 M.Wt 144716.86
Solubility Storage Store at 4°C, Do not freeze
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 0.0069 mL 0.0346 mL 0.0691 mL
5 mM 0.0014 mL 0.0069 mL 0.0138 mL
10 mM 0.0007 mL 0.0035 mL 0.0069 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 8 reference(s) in Google Scholar.)

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