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  3. 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.

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

HOOC-OXA-COOH

HOOC-OXA-COOH Chemical Structure

CAS No. : 1002788-96-6

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Description

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[1].

In Vitro

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.

Cell Cytotoxicity Assay[1]

Cell Line: CT26 mouse colorectal carcinoma cells, HEK293 human embryonic kidney cells
Concentration: /
Incubation Time: 48 h
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.
In Vivo

HOOC-OXA-COOH (2.5 mg/kg calculated as Pt; intravenous injection; 4 administrations), when delivered via F1O LNM1-RGD, inhibits mouse CT26 colon tumors upon combined irradiation with 780 nm laser[1].

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

Animal Model: BALB/c mice (tumor-bearing)[1]
Dosage: 2.5 mg/kg Pt (equivalent to HOOC-OXA-COOH loading)
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
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.
Molecular Weight

629.44

Formula

C16H22N2O12Pt2-

CAS No.
SMILES

[O-]C(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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Please store the product under the recommended conditions in the Certificate of Analysis.

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    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.

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HOOC-OXA-COOH
Cat. No.:
HY-186158
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