1. Others Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  2. Fluorescent Dye Heme Oxygenase (HO) Reactive Oxygen Species (ROS) Apoptosis
  3. TiNIR

TiNIR 是一种近红外肿瘤起始细胞 (TIC) 探针。TiNIR 可检测并富集肺癌中具有功能活性的 TIC,还可通过光声特性对肺癌 TIC 进行可视化。TiNIR 可选择性结合纯化的重组人 HMOX2,其 Kd 值为 0.38 μM。TiNIR 可抑制 HMOX2 活性,诱导活性氧 (ROS) 积累,并触发表达 HMOX2 的肿瘤起始细胞发生细胞凋亡 (apoptosis)。TiNIR 可在肺癌小鼠模型中抑制肿瘤生长、减少肿瘤复发并提高存活率。

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TiNIR

TiNIR Chemical Structure

CAS No. : 1255954-46-1

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查看 Heme Oxygenase (HO) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TiNIR is a tumor initiating cell (TIC) probe with near infrared. TiNIR detects and enriches the functionally active TIC in lung tumors, and visualizes lung TIC through the photoacoustic property. TiNIR selectively binds to purified recombinant human HMOX2 with a Kd of 0.38 μM. TiNIR inhibits HMOX2 activity, induces ROS accumulation, and triggers apoptosis in HMOX2-expressing tumor initiating cells. TiNIR inhibits tumor growth, reduces tumor relapse, and prolongs survival rates in lung cancer mouse models[1].

IC50 & Target[1]

HMOX2

0.38 μM (Kd)

体外研究
(In Vitro)

TiNIR (10-100 nM; 30 min) 在敲低 HMOX2 的人肺癌起始细胞 (TS32 细胞) 中染色减弱,证实 HMOX2 是 TiNIR 的靶点[1]
TiNIR (100 nM; 30 min) 可选择性结合纯化的重组人源 HMOX2,Kd 值为 0.38 μM,但不结合 HMOX1[1]
TiNIR (0.1-1.0 μM; 30) 可抑制纯化的重组人源 HMOX2 的酶活性[1]
TiNIR (0.1-3.0 μM; 120 min) 可在人肺肿瘤起始细胞 (TS32 cells) 中诱导浓度依赖性的 ROS 积累[1]
TiNIR (0-3.0 μM; 24 h) 可呈浓度依赖性诱导人肺癌起始细胞 (TS32 细胞) 发生凋亡性细胞死亡,提高 G1 期细胞比例[1]
TiNIR (0-3.0 μM; 30 min) 对人肺癌起始细胞 (TS10、TS32 细胞) 具有选择性细胞毒性,而对对照细胞 (32A、hLuEpi 细胞) 无此作用[1]

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

Cell Cycle Analysis[1]

Cell Line: TS32 cells
Concentration: 0.1, 0.3, 1.0, 3.0 μM
Incubation Time: 24 h
Result: Increased the sub-G1 phase cell population (apoptotic marker) in a concentration-dependent manner.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 CL AUC0-t AUC0-∞ Vss
Mice[1] 0.5 mg/kg i.v. 15.9 h 0.43 L/h/kg 1.05 μg·h/mL 1.18 μg·h/mL 6.84 L/kg
体内研究
(In Vivo)

TiNIR (10-100 μM;静脉注射,每 2 天 1 次,持续 25 天) 可呈浓度依赖性抑制皮下肺癌的生长[1]
TiNIR (100 μM;静脉注射;每 2 天 1 次;共 27 天) 可降低肺癌术后的肿瘤复发率,仅 10% 的给药小鼠出现复发[1]
TiNIR (100 μM;静脉注射;每 2 天 1 次;120 天) 可显著延长转移性肺癌小鼠模型的生存期[1]

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

Animal Model: Lung cancer NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (4-6 weeks old)[1]
Dosage: 10 μM; 30 μM; 100 μM
Administration: i.v.; every other day; 25 days
Result: Inhibited tumor growth in a concentration-dependent manner.
Reduced tumor weights significantly across all tested doses compared to vehicle control, with the highest reduction observed at the 100 μM dose.
分子量

797.82

Formula

C45H53FIN3O

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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TiNIR
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HY-D3178
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