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  3. HOOC-OXA-COOH

HOOC-OXA-COOH 是一种阴离子 Oxaliplatin (HY-17371) 前药。HOOC-OXA-COOH 可通过静电作用负载于纳米马达,在肿瘤微环境中经 H2S 与内谷胱甘肽级联激活,释放具有细胞毒性的 Pt2+。HOOC-OXA-COOH 可用于结肠癌的研究。

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HOOC-OXA-COOH

HOOC-OXA-COOH Chemical Structure

CAS No. : 1002788-96-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

HOOC-OXA-COOH 可从 F1O LNM1-RGD 纳米马达中以 H2S 浓度依赖的方式释放,在 150 μM NaHS 作用 3 小时后可实现近乎完全的释放[1]
HOOC-OXA-COOH (48 h) 经 F1O LNM1-RGD 递送可强效抑制 CT26 细胞活力,其 IC50 为 24.9 μM,而 780 nm 激光照射可进一步将 IC50 降至 5.92 μM;该制剂对 HEK293 细胞的毒性较低[1]

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.
体内研究
(In Vivo)

HOOC-OXA-COOH (按 Pt 计 2.5 mg/kg;静脉注射;4 次给药) 经 F1O LNM1-RGD 递送后,在联合 780 nm 激光照射的情况下可抑制小鼠 CT26 结肠肿瘤[1]

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.
分子量

629.44

Formula

C16H22N2O12Pt2-

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 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.

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产品名称:
HOOC-OXA-COOH
目录号:
HY-186158
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