129497-78-5
129497-78-5 structure
- Name: Verteporfin
- Chemical Name: Verteporfin
- CAS Number: 129497-78-5
- Molecular Formula: C41H42N4O8
- Molecular Weight: 718.79
- Catalog: API Special medicine Ophthalmic medication
- Create Date: 2018-09-20 07:46:41
- Modify Date: 2024-01-02 15:57:47
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Verteporfin is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions.
| Name | Verteporfin |
|---|---|
| Synonyms |
trans-3,4-Dicarboxy-4,4a-dihydro-4a,8,14,19-tetramethyl-18-vinyl-23H,25H-benzo(b)porphine-9,13-dipropionic acid 3,4,9-trimethyl ester
Visudyne ,3(28),4,6,8,10,12,14,16(26),17,19,21-dodécaén-9-yl]propanoïque - acide 3-[(1Z,6Z,12Z,17Z,23S,24R)-14-éthényl-22,23-bis(méthoxycarbonyl)-9-(3-méthoxy-3-oxopropyl)-4,10,15,24-tétraméthyl-25,26,27,28-té VERTEPORFIN (200 MG) trans-18-Ethenyl-4,4a-dihydro-3,4-bis(methoxycarbonyl)-4a,8,14,19-tetramethyl-23H,25H-benzo[b]porphine-9,13-dipropionic Acid Monomethyl Ester ,4,6,8,10,12,14,16(26),17,19,21-dodecaen-9-yl]propanoic acid - 3-[(1Z,6Z,12Z,17Z,23S,24R)-14-ethenyl-22,23-bis(methoxycarbonyl)-9-(3-methoxy-3-oxopropyl)-4,10,15,24-tetramethyl-25,26,27,28-tetraazahex ,4,6,8,10,12,14,16(26),17,19,21-dodecaen-9-yl]propansäure--3-[(1Z,6Z,12Z,17Z,23S,24R)-14-ethenyl-22,23-bis(methoxycarbonyl)-9-(3-methoxy-3-oxopropyl)-4,10,15,24-tetramethyl-25,26,27,28-tetraazahexacyc Verteporphin 3-[(1Z,6Z,12Z,17Z,23S,24R)-22,23-Bis(methoxycarbonyl)-5-(3-methoxy-3-oxopropyl)-4,10,15,24-tetramethyl-14-vinyl-25,26,27,28-tetraazahexacyclo[16.6.1.1.1.1.0]octacosa-1,3(28),4 ,6,8,10,12,14,16(26),17,19,21-dodecaen-9-yl]propanoic acid - 3-[(1Z,6Z,12Z,17Z,23S,24R)-22,23-bis(methoxycarbonyl)-9-(3-methoxy-3-oxopropyl)-4,10,15,24-tetramethyl-14-vinyl-25,26,27,28-tetraazahexacyc lo[16.6.1.1.1.1.0]o Verteprofin |
| Description | Verteporfin is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. |
|---|---|
| Related Catalog | |
| In Vitro | Verteporfin is specifically selected by PDX-cell screening. The concentrations to cause 50% growth inhibition (GI50) for PhLO, PhLH, and PhLK are 228 nM, 395 nM, and 538 nM, respectively, whereas GI50 for ALL-1, TCC-Y/sr, and NPhA1 are 3.93 µM, 2.11 µM, and 5.61 µM, respectively. GSH significantly reduces the sensitivity of 2 out of 3 PDX cells to verteporfin. Verteporfin reduces the mitochondrial membrane potential in PDX cells[1]. Verteporfin reduces the PTX-resistance on HCT-8/T cells by inhibiting YAP expression and combination therapy with verteporfin and paclitaxel (PTX) shows synergism on inhibition of YAP and cytotoxicity to HCT-8/T[2]. |
| In Vivo | Verteporfin (10 mg/kg, c.s.c.) and dasatinib significantly reduces the leukemia cell ratio, and combined therapy further reduced the number of leukemia cells in the spleen[1]. |
| Cell Assay | PDX cells co-cultured with S17 cells are treated with 16 combinations of verteporfin (60 nM, 120 nM, 180 nM, and 240 nM) and dasatinib (12 nM, 24 nM, 36 nM, and 48 nM). The viabilities of cells treated with each combination are measured after 48 h using FACS Aria flow cytometer. In order to estimate drug interaction between verteporfin and dasatinib, a normalized isobologram and fraction affectedcombination index (CI) plot are made using CompuSyn software. CI values greater than 1.0 indicated antagonistic effects, equal to 1.0 additive effects, and below 1.0 synergistic effects. |
| Animal Admin | Mice: PhLO cells (1.0×107/mouse) are injected intravenously into 6-week-old male NOG mice, which are then treated with vehicle, verteporfin (140 mg/kg/day), dasatinib (20 mg/kg/day), and a combination of these drugs from days 22 to 28. Verteporfin is administered by continuous subcutaneous infusion (c.s.c.) using Alzet osmotic pumps. An intraperitoneal injection (i.p.) is performed for dasatinib. All mice are sacrificed on day 28 and the chimerism of leukemia cells is investigated by flow cytometer using an anti-human CD19 antibody and antimouse CD45 antibody. Blood concentrations of verteporfin are calculated by LCMS-2020. |
| References |
| Molecular Formula | C41H42N4O8 |
|---|---|
| Molecular Weight | 718.79 |
| PSA | 337.48000 |
| LogP | 10.24600 |
| Storage condition | ?20°C |
| Water Solubility | DMSO: soluble2mg/mL, clear (warmed) |
| RIDADR | NONH for all modes of transport |
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