| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Trabectedin (also known as ET743; Ecteinascidin-743; ET-743; trade name Yondelis) is a novel antitumor agent of marine origin with potent in vitro and in vivo antitumour activity. It has been authorized as an antitumor chemotherapy drug as of 2015 for the treatment of ovarian cancer and advanced soft-tissue sarcoma. In both types of breast cancer cells, trabectedin caused cytotoxicity and apoptosis in a time- and concentration-dependent manner.
| Targets |
MX-1 cells (IC50 = 0.1 nM); MCF7 cells (IC50 = 1.5 nM); MCF7/DXR cells (IC50 = 3.7 nM); Reactive oxygen species (ROS); Apoptosis
|
|---|---|
| ln Vitro |
Treatment with trabectedin (ET-743; 10 nM; 24-72 hours; MCF7 cells) causes cell accumulation in the late S to G2 phase[1].
Trabectedin has an IC50 of 0.1 nM, 1.5 nM, and 3.7 nM, respectively, which inhibits the growth of MX-1, MCF7, and MCF7/DXR cells[1]. Trabectedin causes cytotoxicity and apoptosis in both types of breast cancer cells in a manner that depends on both time and concentration. When Trabectedin is applied to MCF-7 cells, the expression levels of the death receptor pathway molecules TRAIL-R1/DR4, TRAIL-R2/DR5, FAS/TNFRSF6, TNF RI/TNFRSF1A, and FADD are significantly increased by 2.6, 3.1, 1.7, 11.2, and 4.0 fold, respectively. Pro-apoptotic proteins Bax, Bad, Cytochrome c, Smac/DIABLO, and cleaved Caspase-3 expression levels are increased by 4.2, 3.6, 4.8, 4.5, and 4.4 fold in MDA-MB-453 cells, whereas anti-apoptotic protein expression levels Bcl-2 and Bcl-XL are decreased by 4.8 and 5.2 fold[2]. Myxoid liposarcoma (MLS) primary tumor cultures and/or cell lines can produce CCL2, CXCL8, IL-6, VEGF, and PTX3 when treated in vitro with noncytotoxic concentrations of Trabectedin[3]. |
| ln Vivo |
Treatment with trabectin (ET-743; 30-50 μg/kg; intravenous injection; every three days; female athymic nude mice) increases the antitumor effects in nude mice bearing MX-1 mammary carcinoma xenografts without increasing toxicity[1].
Following Trabectedin treatment, CCL2, CXCL8, CD68+ infiltrating macrophages, CD31+ tumor vessels, and partial decreases in PTX3 are significantly reduced in a xenograft mouse model of human myxoid liposarcoma (MLS)[3]. |
| Cell Assay |
Before samples were collected for Western blot analysis, RNAiMax Lipofectamine (4.5 mL per well in a 6-well dish) was added to siRNA targeting the EWS-FLI1 breakpoint site II, complexed, combined with cells, and incubated for 36 to 48 hours.
|
| References |
|
| Molecular Formula |
C39H43N3O11S
|
|---|---|
| Molecular Weight |
761.843
|
| Exact Mass |
761.2618
|
| Elemental Analysis |
C, 61.49; H, 5.69; N, 5.52; O, 23.10; S, 4.21
|
| CAS # |
114899-77-3
|
| Related CAS # |
Trabectedin-d3
|
| Appearance |
Solid powder
|
| SMILES |
CC1=CC2=C([C@@H]3[C@@H]4[C@H]5C6=C(C(=C7C(=C6[C@@H](N4[C@H]([C@H](C2)N3C)O)COC(=O)[C@@]8(CS5)C9=CC(=C(C=C9CCN8)O)OC)OCO7)C)OC(=O)C)C(=C1OC)O
|
| InChi Key |
PKVRCIRHQMSYJX-RJZIEWFPSA-N
|
| InChi Code |
InChI=1S/C39H43N3O11S/c1-16-9-20-10-22-37(46)42-23-13-50-38(47)39(21-12-25(48-5)24(44)11-19(21)7-8-40-39)14-54-36(30(42)29(41(22)4)26(20)31(45)32(16)49-6)28-27(23)35-34(51-15-52-35)17(2)33(28)53-18(3)43/h9,11-12,22-23,29-30,36-37,40,44-46H,7-8,10,13-15H2,1-6H3/t22-,23-,29+,30+,36+,37-,39+/m0/s1
|
| Chemical Name |
[(1R,2R,3R,11S,12S,14R,26R)-5,6',12-trihydroxy-6,7'-dimethoxy-7,21,30-trimethyl-27-oxospiro[17,19,28-trioxa-24-thia-13,30-diazaheptacyclo[12.9.6.13,11.02,13.04,9.015,23.016,20]triaconta-4(9),5,7,15,20,22-hexaene-26,1'-3,4-dihydro-2H-isoquinoline]-22-yl] acetate
|
| Synonyms |
Trabectedin; ET-743; ET 743; ET743; Ecteinascidin 743
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (3). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 33.3~100 mg/mL (43.8~131.3 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.28 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3126 mL | 6.5631 mL | 13.1261 mL | |
| 5 mM | 0.2625 mL | 1.3126 mL | 2.6252 mL | |
| 10 mM | 0.1313 mL | 0.6563 mL | 1.3126 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04076579 | Active Recruiting |
Drug: Olaparib Drug: Trabectedin |
Sarcoma Sarcoma Metastatic |
University of Michigan Rogel Cancer Center |
March 17, 2020 | Phase 2 |
| NCT03985722 | Active Recruiting |
Drug: Olaratumab and Trabectedin |
Sarcoma, Soft Tissuec | Grupo Espanol de Investigacion en Sarcomas |
September 21, 2018 | Phase 1 |
| NCT04979442 | Active Recruiting |
Drug: RAIN-32 Drug: Trabectedin |
Dedifferentiated Liposarcoma | Rain Oncology Inc | July 14, 2021 | Phase 3 |
| NCT02359474 | Active Recruiting |
Genetic: DNA double-strand breaks Drug: Trabectedin |
Sarcoma | Ludwig-Maximilians - University of Munich |
December 19, 2014 | Phase 2 |
| NCT03127215 | Active Recruiting |
Drug: Olaparib Drug: Trabectedin |
Cancers With DNA Repair- Deficiency |
National Center for Tumor Diseases, Heidelberg |
October 25, 2018 | Phase 2 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA