HOOC-OXA-COOH
HOOC-OXA-COOH is an anionic prodrug of Oxaliplatin (HY-17371). HOOC-OXA-COOH can be loaded onto nanomotors via electrostatic interaction, and undergoes cascade activation by H2S and endogenous glutathione in the tumor microenvironment to release cytotoxic Pt2+. HOOC-OXA-COOH can be used in the research of colon cancer.
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- CAS No.: 1002722-97-5
- Formule: C16H24N2O12Pt
- Masse moléculaire:631.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
HOOC-OXA-COOH is released from F1O LNM1-RGD nanomotors in an H2S concentration-dependent manner, and nearly complete release is achieved after treatment with 150 μM NaHS for 3 h[1].
HOOC-OXA-COOH (48 h) delivered by F1O LNM1-RGD potently inhibits the viability of CT26 cells, with an IC50 of 24.9 μM, while irradiation with 780 nm laser further reduces the IC50 to 5.92 μM; this formulation shows low toxicity to HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CT26 mouse colorectal carcinoma cells, HEK293 human embryonic kidney cells
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Concentration:/
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Incubation Time:48 h
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Result:Exhibited an IC50 of 24.9 μM against CT26 cells when delivered via F1O LNM1-RGD, which was significantly lower than the IC50 of free HOOC-OXA-COOH (151.8 μM) against CT26 cells.
Showed an even lower IC50 of 5.92 μM against CT26 cells when F1O LNM1-RGD was combined with 780 nm laser irradiation.
Resulted in significantly higher viability in HEK293 cells compared to CT26 cells when delivered via F1O LNM1-RGD.
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 (tumor-bearing)[1]
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Dosage:2.5 mg/kg Pt (equivalent to HOOC-OXA-COOH loading)
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Administration:i.v.; on day 0, 2, 4, and 6; with or without 780 nm laser irradiation (5 min, 0.5 W cm-2) 1 hour post-injection on the same days
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Result:Eradicated subcutaneous CT26 colon tumors when combined with light treatment.
Significantly prolonged survival rate compared to control groups.
Induced stronger immunogenic cell death effects than free OXA.
Significantly upregulated pro-inflammatory cytokine levels (TNF-α, IL-6, IFN-γ) in tumor tissues and increased dendritic cell maturation in draining lymph nodes, with greater effects seen with light treatment.
Enhanced intratumoral infiltration of CD4+ and CD8+ cytotoxic T lymphocytes, while reduced regulatory T cell populations; light treatment amplified these changes.
Induced robust immune memory.
Chemical Information
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CAS No. 1002722-97-5
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Masse moléculaire 631.45
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Formule C16H24N2O12Pt
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SMILES
OC(CCC([O-][Pt+4]12([NH2][C@@]3([H])[C@](CCCC3)([H])[NH2]1)([O-]C(C([O-]2)=O)=O)[O-]C(CCC(O)=O)=O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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