CAS 129497-78-5|Verteporfin
Introduction：Basic information about CAS 129497-78-5|Verteporfin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Verteporfin | ||
|---|---|---|---|
| CAS Number | 129497-78-5 | Molecular Weight | 718.79 |
| Density | / | Boiling Point | / |
| Molecular Formula | C41H42N4O8 | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | / |
Names
| Name | Verteporfin |
|---|---|
| Synonym | More Synonyms |
Verteporfin BiologicalActivity
| 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 | Signaling Pathways >>Autophagy >>AutophagySignaling Pathways >>Stem Cell/Wnt >>YAPResearch Areas >>Others |
| 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 | [1]. Morishita T, et al. The photosensitizer verteporfin has light-independent anti-leukemic activity for Ph-positive acute lymphoblastic leukemia and synergistically works with dasatinib. Oncotarget. 2016 Aug 2. [2]. Pan W, et al. Verteporfin can Reverse the Paclitaxel Resistance Induced by YAP Over-Expression in HCT-8/T Cells without Photoactivation through Inhibiting YAP Expression. Cell Physiol Biochem. 2016;39(2):481-90. |
Chemical & Physical Properties
| Molecular Formula | C41H42N4O8 |
|---|---|
| Molecular Weight | 718.79 |
| PSA | 337.48000 |
| LogP | 10.24600 |
| Storage condition | ?20°C |
| Water Solubility | DMSO: soluble2mg/mL, clear (warmed) |
Safety Information
| RIDADR | NONH for all modes of transport |
|---|
Articles81
More Articles| Verteporfin therapy and triamcinolone acetonide: convergent modes of action for treatment of neovascular age-related macular degeneration. Eur. J. Ophthalmol. 16(6) , 824-34, (2006) Choroidal neovascularization associated with age-related macular degeneration is the primary cause of blindness in the elderly in developed countries, due to a number of pathogenic effects, including ... | |
| NF2 Loss Promotes Oncogenic RAS-Induced Thyroid Cancers via YAP-Dependent Transactivation of RAS Proteins and Sensitizes Them to MEK Inhibition. Cancer Discov. 5 , 1178-93, (2015) Ch22q LOH is preferentially associated with RAS mutations in papillary and in poorly differentiated thyroid cancer (PDTC). The 22q tumor suppressor NF2, encoding merlin, is implicated in this interact... | |
| Aerobic glycolysis tunes YAP/TAZ transcriptional activity. EMBO J. 34 , 1349-70, (2015) Increased glucose metabolism and reprogramming toward aerobic glycolysis are a hallmark of cancer cells, meeting their metabolic needs for sustained cell proliferation. Metabolic reprogramming is usua... |
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 |
