2. Stem Cell/Wnt TGF-beta/Smad
  3. TGF-beta/Smad
  4. Trabedersen sodium

Trabedersen sodium  (Synonyms: AP 12009 sodium)

Cat. No.: HY-142118A Purity: 98.81%
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Trabedersen (AP 12009) sodium is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen sodium blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen sodium exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen sodium is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma.

For research use only. We do not sell to patients.

DNA, d(P-thio)(C-G-G-C-A-T-G-T-C-T-A-T-T-T-T-G-T-A), sodium salt

Trabedersen sodium Chemical Structure

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Based on 1 publication(s) in Google Scholar

Other Forms of Trabedersen sodium:

Trabedersen sodium Related Antibodies

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1 Publications Citing Use of MCE Trabedersen sodium

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Description

Trabedersen (AP 12009) sodium is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen sodium blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen sodium exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen sodium is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma[1][2][3][4].

In Vitro

Trabedersen sodium (1, 5, 10 μM) reduces TGFβ2 secretion by 49-73% and cell proliferation by 24-41%, inhibits migration, and enhances LAK cell-mediated cytotoxicity in human high-grade astrocytoma (III/IV) cells[1].
Trabedersen sodium inhibits TGFβ2 secretion by 43%, reduces cell proliferation by up to 77%, blocks migration, and increases LAK cell cytotoxicity 4-fold in human pancreatic cancer cell lines (Hup-T3, PA-TU 8902)[1].
Trabedersen sodium (1-80 μM; 7 days) potently suppresses TGF-β2 secretion from human pancreatic cancer Hup-T3 cells, with an IC50 of 1.7 μM and complete inhibition at concentrations ≥60 μM after 7 days of treatment[3].
Trabedersen sodium (2.5-80 μM; 7 days) strongly inhibits proliferation of human pancreatic cancer Hup-T3 cells, with an IC50 of 4.6 μM and >90% inhibition at 40 μM after 7 days of treatment[3].
Trabedersen sodium (5 μM; up to 7 days) completely inhibits migration of human pancreatic cancer PA-TU-8902 cells in a spheroid model when treated with 5 μM for up to 7 days[3].
Trabedersen sodium (200 nM, 5 μM; 6 h, variable) efficiently reverses TGF-β2-mediated immunosuppression of human pancreatic cancer Hup-T3 cells, resulting in significantly increased LAK cell-mediated cytotoxicity against Hup-T3 target cells[3].
Trabedersen sodium (10-80 μM) potently inhibits TGF-β2 secretion in human glioblastoma multiforme cells, with 10 μM trabedersen acting to a greater extent than 80 μM trabedersen[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Trabedersen sodium Related Antibodies

ELISA Assay[3]

Cell Line: human pancreatic cancer Hup-T3 cells
Concentration: 1, 10, 20, 60, 80 μM
Incubation Time: 7 days (with medium replacement on days 2 and 4)
Result: Caused a concentration-dependent reduction of TGF-β2 secretion.
Achieved >30% reduction with 1 μM trabedersen.
Achieved >95% reduction with 20 μM trabedersen.
Resulted in no detectable TGF-β2 at concentrations ≥60 μM.
Had an IC50 of 1.7 μM for TGF-β2 secretion inhibition.

Cell Proliferation Assay[3]

Cell Line: human pancreatic cancer Hup-T3 cells
Concentration: 2.5, 10, 20, 40, 60, 80 μM
Incubation Time: 7 days (with medium replacement on days 2 and 4)
Result: Caused a concentration-dependent reduction in Hup-T3 cell number.
Achieved >90% reduction in cell number with 40 μM trabedersen.
Had an IC50 of 4.6 μM for inhibition of Hup-T3 cell proliferation.
In Vivo

Trabedersen sodium (1.4-50 nmol; intrathecal administration; single bolus dose; 5 nmol/h; intracerebral administration; continuous infusion; 1 week) is well tolerated in rabbits and cynomolgus monkeys at single intrathecal bolus doses up to 50 nmol, whereas continuous intracerebral infusion at a rate of 5 nmol/h for 1 week induces mild to moderate local leukocyte infiltration in rabbits[1].
Trabedersen (30-1000 mg/kg; intravenous injection; single bolus dose) is well tolerated in mice and rats at single intravenous bolus doses up to 100 mg/kg, with an LD50 value of 706 mg/kg in mice and 1175 mg/kg in rats[1].
Continuous intravenous infusion of Trabedersen sodium at a dose of 1 mg/kg/day is well tolerated in rats and monkeys, whereas continuous infusion at higher doses induces reversible inflammation and tissue damage; intravenous infusion at a dose of 8 mg/kg every other day for 4 weeks is also well tolerated in monkeys[1].
In cynomolgus monkeys, trabedersen sodium (5-160 mg/kg; intravenous infusion; 2 h duration; single dose) is well tolerated at intravenous doses up to 20 mg/kg over a 2-hour infusion with respect to cardiovascular and complement activation endpoints; it is well tolerated at doses below 5 mg/kg with respect to hematological indices[1].
Trabedersen (0.25-50 mg/kg; i.p.; three times per week; approximately 32-35 days) sodium exhibits potent dose-dependent antitumor activity in orthotopic xenograft melanoma mouse models, reduces lung metastasis, and shows evidence of immunomodulatory effects as well as cellular/nuclear uptake; among these, the 50/16 mg/kg dosing regimen significantly reduces the average tumor weight to 0.395 g[2].
Trabedersen sodium significantly reduces the tumor weight, tumor cell proliferation level, tumor vascularization degree, and incidence of lymph node metastasis of primary pancreatic cancer in orthotopic xenograft mouse models[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: New Zealand White rabbits; Cynomolgus monkeys[1]
Dosage: 1.4 nmol (intrathecal bolus); 50 nmol (intrathecal bolus); 5 nmol/h (continuous intracerebral infusion)
Administration: intrathecal; single bolus dose; intracerebral; continuous infusion; 1 week
Result: Reported no clinical signs of toxicity after single intrathecal bolus doses of 1.4 nmol or 50 nmol.
Detected no macroscopic drug-related toxicity after continuous intracerebral infusion of 5 nmol/h for 1 week, but histopathology revealed mild-to-moderate leukocyte infiltration near the injection site.
Animal Model: Rats; Cynomolgus monkeys[1]
Dosage: 1 mg/kg/day (continuous intravenous infusion); 4 mg/kg/day (continuous intravenous infusion); 16 mg/kg/day (continuous intravenous infusion); 8 mg/kg (intravenous over 4 h)
Administration: intravenous; continuous infusion; 2 weeks (rats); 2-4 weeks (monkeys); intravenous; over 4 h; every other day; 4 weeks
Result: Detected no adverse effects in rats or monkeys treated with 1 mg/kg/day continuous intravenous infusion.
Observed evidence of inflammation and tissue damage at higher continuous infusion doses (4 mg/kg/day, 16 mg/kg/day), including increased erythrocyte sedimentation rate, increased activated partial thromboplastin time, decreased platelet counts, increased blood AST levels, decreased albumin and calcium levels, decreased albumin/globulin ratio, and histological lesions in the liver and kidneys; these lesions were almost completely repaired after a 4-week recovery period.
Noted no significant hematological or biochemical changes in monkeys treated with 8 mg/kg intravenous over 4 h every other day for 4 weeks.
Animal Model: BALB/c nu/nu mice[2]
Dosage: 50 mg/kg initial dose followed by 16 mg/kg subsequent doses; 16 mg/kg; 4 mg/kg; 1 mg/kg; 0.25 mg/kg
Administration: i.p.; thrice weekly; approximately 32-35 days
Result: Reduced mean tumor weight to 0.395 g in mice treated with 50/16 mg/kg regimen compared to controls.
Exhibited dose-dependent reduction in tumor weight and tumor growth at doses of 1 mg/kg, 4 mg/kg, and 16 mg/kg.
Significantly inhibited lung metastasis.
Showed a trend toward fewer monocytic MDSCs in spleens, with no differences in granulocytic MDSCs or NK cells compared to controls.
Demonstrated clear intracellular and intranuclear fluorescence in all tumor sections from mice receiving intratumoral fluorescently labeled trabedersen, confirming cellular and nuclear uptake.
Animal Model: BALB/Cnu/nu mice (8-week-old male, orthotopic pancreatic cancer xenograft model)[3]
Dosage: 50 mg/kg (initial loading dose); 16 mg/kg (maintenance)
Administration: i.p.; single initial loading dose on day 2 post-tumor implantation; three times weekly (Monday, Wednesday, Friday)
Result: Reduced mean primary tumor.
Significantly decreased tumor cell proliferation.
Reduced tumor vascularization to approximately one-third of control levels (CD31+ vessel area).
Reduced lymph node metastasis incidence from 7 out of 9 to 2 out of 10.
Showed no significant effect on liver metastasis incidence.
Molecular Weight

5768.7 (free acid)

Formula

C177H217N60Na18O94P17S17
Appearance

Solid

Color

White to off-white

SMILES

[Trabedersen (sodium)]
Shipping

Room temperature in continental US; may vary elsewhere.
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

Purity: 98.81%

SDS (252 KB)

COA (243 KB) LCMS (315 KB)

Handling Instructions (2242 KB)
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Trabedersen sodium Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TrabedersenAP 12009AP12009AP-12009TGF-beta/SmadTransforming growth factor betaxenograft modelspancreatic cancermyeloid-derived suppressor cellsanaplastic astrocytomacolorectal tumortumor cellshuman TGFβ2 mRNAmelanomaglioblastomaTGFβ2Inhibitorinhibitorinhibit

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