Olaptesed pegol sodium
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Olaptesed pegol (NOX-A12) sodium is a L-oligoribonucleotide aptamer targeting CXCL12 based on a pegylated structure. Olaptesed pegol sodium neutralizes CXCL12, and CXCL12 inhibition mobilizes chronic lymphocytic leukemia cells into the circulation and prevents their homing into the protective microenvironment. Olaptesed pegol sodium can enhances the infiltration of human primary T cells and NK cells and inhibit tumor growth companied with anti-PD-1 antibody. Olaptesed pegol sodium can be used for researches of colon cancer and lymphocytic leukemia.
For research use only. We do not sell to patients.
- Purity: 95.94%
- Molecular Weight:54656.69 (free acid)
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
CXCL12[1]
Olaptesed pegol (10-100 nM, overnight incubation) sodium dose-dependently enhances the infiltration of human primary T cells (CD8+, CD4+) and NK cells in heterotypic tumor-stroma spheroids (PSN-1/MS-5, HT-29/MS-5, H1299/MS-5, U251MG/MS-5) containing CXCL12, slightly promotes B cell infiltration, has no effect on monocyte infiltration, and results in low levels of Treg cell infiltration[2].
Olaptesed pegol (10 nM, combined with anti-PD-1 antibody, overnight incubation) sodium synergizes with anti-PD-1 antibody to enhance the activation of Jurkat PD-1/luc T cells in the MS-5/CHO-PD-L1 spheroid model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice bearing CT-26 colorectal cancer syngeneic tumors[2]
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Dosage:20 mg/kg
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Administration:Subcutaneously injection, every other day, initiated on day 5
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Result:Inhibited tumor growth with 5 out of 8 mice responding.
Olaptesed pegol alone had no significant inhibitory effect on tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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Molecular Weight 54656.69 (free acid)
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Color White to off-white
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SMILES
[Olaptesed pegol (sodium)]
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Synonyms
NOX-A12 sodium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2242 KB)
References
[1]. Steurer M, et al. Olaptesed pegol (NOX-A12) with bendamustine and rituximab: a phase IIa study in patients with relapsed/refractory chronic lymphocytic leukemia. Haematologica. 2019 Oct;104(10):2053-2060. [Content Brief]
[2]. Zboralski D, et al. Increasing Tumor-Infiltrating T Cells through Inhibition of CXCL12 with NOX-A12 Synergizes with PD-1 Blockade. Cancer Immunol Res. 2017 Nov;5(11):950-956. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)