Temoporfin (m-THPC)是一种合成的chlorin化合物，具有光激活作用，可作为强效光敏剂。
Cas No.:122341-38-2
Sample solution is provided at 25 µL, 10mM.
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Temoporfin (m-THPC) is a synthetic chlorin compound with light-activated actions that acts as a potent photosensitizer [1]. Temoporfin is activated at 652nm with a light penetration depth of 1cm, and exhibits a high tumor selectivity with residual photosensitivity for two weeks[2]. Temoporfin has been widely used in photodynamic therapy (PDT) to inhibit different cancer cell growth[3]. Temoporfin-based PDT can repolarize macrophages to the M1 phenotype, which can induce a phenotypic shift of tumor-associated macrophages[4].
In vitro, Temoporfin treatment for 24h followed by irradiation with a 500W halogen lamp at 5.5×10-2mW/cm2/nm light intensity and 39.6mJ/cm2/nm light energy significantly inhibited HCT116 cell viability with an IC50 value 36.4nM[5]. When exposed to 620-660nm light at a dose of 13.3J/cm2, Temoporfin treatment for 24h significantly inhibited the proliferation of HL60 and 4T1 cells with an IC50 value of 42nM and 117nM, respectively[6].
References:
[1] Senge M O. mTHPC–A drug on its way from second to third generation photosensitizer?[J]. Photodiagnosis and Photodynamic Therapy, 2012, 9(2): 170-179.
[2] Dragicevic-Curic N, Scheglmann D, Albrecht V, et al. Development of different temoporfin-loaded invasomes—novel nanocarriers of temoporfin: Characterization, stability and in vitro skin penetration studies[J]. Colloids and Surfaces B: Biointerfaces, 2009, 70(2): 198-206.
[3] Senge M O, Brandt J C. Temoporfin (Foscan®, 5, 10, 15, 20‐tetra (m‐hydroxyphenyl) chlorin)—a second‐generation photosensitizer[J]. Photochemistry and photobiology, 2011, 87(6): 1240-1296.
[4] Zhu Z, Scalfi-Happ C, Ryabova A, et al. Photodynamic activity of Temoporfin nanoparticles induces a shift to the M1-like phenotype in M2-polarized macrophages[J]. Journal of Photochemistry and Photobiology B: Biology, 2018, 185: 215-222.
[5] Banfi S, Caruso E, Caprioli S, et al. Photodynamic effects of porphyrin and chlorin photosensitizers in human colon adenocarcinoma cells[J]. Bioorganic & medicinal chemistry, 2004, 12(18): 4853-4860.
[6] Králová J, Briza T, Moserová I, et al. Glycol porphyrin derivatives as potent photodynamic inducers of apoptosis in tumor cells[J]. Journal of medicinal chemistry, 2008, 51(19): 5964-5973.
Temoporfin (m-THPC)是一种合成的chlorin化合物，具有光激活作用，可作为强效光敏剂[1]。Temoporfin在652nm波长下被激活，光穿透深度为1厘米，并具有高肿瘤选择性，残留光敏性可持续两周[2]。Temoporfin已被广泛用于光动力疗法（PDT）中以抑制不同癌细胞的生长[3]。基于Temoporfin的PDT可使巨噬细胞复极化为M1表型，从而诱导肿瘤相关巨噬细胞的表型转变[4]。
在体外，Temoporfin处理24小时后，以5.5×10-2mW/cm2/nm的光强度和39.6mJ/cm2/nm的光能量用500W卤素灯照射，显著抑制了HCT116细胞的活力，IC50值为36.4nM[5]。当暴露于620-660nm波长、剂量为13.3J/cm2的光照时，Temoporfin处理24小时显著抑制了HL60细胞和4T1细胞的增殖，IC50值分别为42nM和117nM[6]。
| Cell experiment [1]: | |
Cell lines | HCT116 cells |
Preparation Method | HCT116 cells were cultured in Dulbecco's Modified Eagle's medium containing 10% fetal bovine serum at 37℃ in the presence of 5% CO2. HCT116 cells were seeded at a density of 5×104 cells/ml in 96-well flat-bottom plates and cultured for 48 hours. Cells were treated with different concentrations of Temoporfin (1, 10, 100, 1000, and 10000nM) for 24h, and cells were irradiated under visible light for 2h (average value between 400 and 700nm; light irradiance 5.5×10−2mW/cm2/nm and a light energy of 39.6mJ/cm2/nm). Cell viability was then analyzed after an additional 24h of incubation with drug-free medium. |
Reaction Conditions | 1, 10, 100, 1000, and 10000nM; 24h |
Applications | Temoporfin treatment reduced the cell viability of HCT116 cells in a concentration-dependent manner when exposed to light. |
References: | |
| Cas No. | 122341-38-2 | SDF | |
| 别名 | 替莫泊芬; m-THPC; KW2345 | ||
| Canonical SMILES | OC1=CC=CC(/C2=C3CCC(/C(C4=CC(O)=CC=C4)=C5C=C/C(N/5)=C(C6=CC(O)=CC=C6)/C(C=C/7)=NC7=C(C8=CC(O)=CC=C8)/C9=CC=C2N9)=N\3)=C1 | ||
| 分子式 | C44H32N4O4 | 分子量 | 680.75 |
| 溶解度 | DMSO : ≥ 30 mg/mL (44.07 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.469 mL | 7.3448 mL | 14.6897 mL |
| 5 mM | 293.8 μL | 1.469 mL | 2.9379 mL |
| 10 mM | 146.9 μL | 734.5 μL | 1.469 mL |
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