1. Antibody-drug Conjugate/ADC Related Metabolic Enzyme/Protease
  2. Drug-Linker Conjugates for ADC NAMPT
  3. L2-FK866

L2-FK866 是一种 ADC 有效载荷-连接子偶联物 (Drug-linker conjugate for ADC)。L2-FK866 含有 ADC 连接子 (Val-Cit-p-aminobenzyl) 和 NAMPT 抑制剂 FK866 (HY-50876)。L2-FK866 可与 Dinutuximab (HY-P9933) 偶联形成 ADC。L2-FK866 可用于神经母细胞瘤研究。



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L2-FK866

L2-FK866 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

L2-FK866 is an ADC payload-linker conjugate (Drug-linker conjugate for ADC). L2-FK866 contains the ADC linker (Val-Cit-p-aminobenzyl) and the NAMPT inhibitor FK866 (HY-50876). L2-FK866 can be conjugated with Dinutuximab (HY-P9933) to form an ADC. L2-FK866 is applicable to neuroblastoma research[1].\n



体外研究
(In Vitro)

Cell Cytotoxicity Assay[1]

Cell Line: IMR-32, SH-SY5Y, SK-N-SH (neuroblastoma cell lines)
Concentration: 0.0064-500 nM
Incubation Time: 72 h
Result: Exhibited potent cytotoxicity in GD2-high IMR-32 and SH-SY5Y cells.
Showed minimal cytotoxicity in GD2-low SK-N-SH cells even at the highest test concentration of 500 nM.

Cell Cytotoxicity Assay[1]

Cell Line: HEK293T, peripheral blood mononuclear cells (PBMCs)
Concentration: 0.032-100 nM (HEK293T cells); 10 nM (PBMCs)
Incubation Time: 72 h
Result: Significantly reduced cytotoxicity compared to free FK866 in HEK293T cells.
Had minimal effect on cell viability in both naive and PHA-stimulated PBMCs at 10 nM for 72 h, whereas free FK866 markedly inhibited viability.

Western Blot Analysis[1]

Cell Line: SH-SY5Y neuroblastoma cells
Concentration: 10 nM
Incubation Time: 48 h
Result: Induced phosphorylation of AMPK at Thr172, a hallmark of energy stress.

Cell Proliferation Assay[1]

Cell Line: SH-SY5Y neuroblastoma cells
Concentration: 2 nM
Incubation Time: 18 days
Result: Significantly reduced colony formation area in SH-SY5Y cells compared to untreated controls.

Cell Cycle Analysis[1]

Cell Line: SH-SY5Y neuroblastoma cells
Concentration: 10 nM
Incubation Time: 36 h
Result: Induced a pronounced accumulation of cells in the S phase and reduced the proportion of G0/G1-phase cells, indicating S-phase arrest.
Caused a reduction in Cyclin D1 protein levels via Western blot analysis.

Apoptosis Analysis[1]

Cell Line: SH-SY5Y, SK-N-SH (neuroblastoma cells)
Concentration: 10 nM
Incubation Time: 48 h
Result: Induced significant apoptosis in SH-SY5Y cells, with cleavage of Caspase-9 and PARP detected by Western blot.
Showed no proapoptotic activity in SK-N-SH cells, demonstrating GD2-dependent activity.
体内研究
(In Vivo)
Animal Model: BALB/c nude (male, 5-6 weeks old, 20±2 g, inoculated with 5×106 SH-SY5Y cells)[1]
Dosage: 6 mg/kg
Administration: i.v.; on day 0, 6, and 12
Result: Induced robust and sustained tumor growth inhibition, with tumor volumes remaining near baseline levels for the duration of the study.
Showed no significant changes in body weight compared with vehicle controls, indicating good tolerability.
分子量

1388.61

Formula

C64H89N15O16S2

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
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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.

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产品名称:
L2-FK866
目录号:
HY-181911
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