| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In A549 cells, motexafin gadolinium (50 µM; 22 h) causes dichlorofluorescein ether salt (DCFA) to oxidize [1]. When coupled with Zn (100 μM) and ascorbic acid (100 μM), motezafin gadolinium (100 μM; 4, 12 hours) promotes intracellular ROS generation and cell disinfection (24 hours) in Ramos cells [2]. Combining motezafin gadolinium (0.01-100 μM) with zinc (100 μM) and ascorbic acid (100 μM) in HF-1 cells lowers p53 protein expression in a cautious manner [2].
|
|---|---|
| Cell Assay |
Western Blot Analysis[2]
Cell Types: HF-1 Cell Tested Concentrations: 0.01-100 μM, with Zn (100 μM) and ascorbic acid (100 μM) Incubation Duration: 5 hrs (hours) Experimental Results: Caused a dose-dependent decrease in p53 in HF-1 cells, but not p53 information in Ramos cells. |
| References |
[1]. Magda D, et al. Motexafin gadolinium: a novel redox active drug for cancer therapy. Semin Cancer Biol. 2006 Dec;16(6):466-76.
[2]. Singh AT, et al. Motexafin gadolinium enhances p53-Mdm2 interactions, reducing p53 and downstream targets in lymphoma cell lines. Anticancer Res. 2010 Apr;30(4):1131-6. [3]. Evens AM, et al. The novel expanded porphyrin, motexafin gadolinium, combined with [90Y]ibritumomab tiuxetan for relapsed/refractory non-Hodgkin's lymphoma: preclinical findings and results of a phase I trial. Clin Cancer Res. 2009 Oct 15;15(20):6462-71. |
| Additional Infomation |
Motexafin gadolinium is studied in the treatment of cancer by Pharmacyclics. It may make tumor cells more sensitive to radiation therapy, improve tumor images using magnetic resonance imaging (MRI), and kill cancer cells. It belongs to the family of drugs called metalloporphyrin complexes. Also called gadolinium texaphyrin.
Motexafin Gadolinium is a synthetic metallotexaphyrin with radiosensitizing and chemosensitizing properties. Motexafin gadolinium accumulates in tumor cells preferentially due to their increased rates of metabolism, generating reactive oxygen species (ROS) intracellularly and lowering the tumor cell apoptotic threshold to ionizing radiation and chemotherapy. (NCI04) Drug Indication Investigated for use/treatment in brain cancer, cancer/tumors (unspecified), lung cancer, and lymphoma (non-hodgkin's). Mechanism of Action Motexafin gadolinium (Xcytrin) is Pharmacyclics' most advanced anti-cancer product candidate, a small-molecule drug with a novel mechanism of action. Xcytrin accumulates selectively in cancer cells due to their increased rates of metabolism. Once inside the cell, Xcytrin induces apoptosis (programmed cell death) by disrupting redox-dependent pathways. Xcytrin inhibits the enzyme thioredoxin reductase, which is a tumor growth promoter. This mechanism provides the opportunity to use Xcytrin in a wide range of cancers. Xcytrin is paramagnetic, and therefore is detectable by magnetic resonance imaging (MRI), allowing the visualization of the drug in tumors. |
| Molecular Formula |
C52H72GDN5O14
|
|---|---|
| Molecular Weight |
1148.419
|
| Exact Mass |
1148.43
|
| CAS # |
246252-06-2
|
| Related CAS # |
156436-90-7 (lutetium hydrate);246252-06-2 (gadolinium);189752-49-6 (free);
|
| PubChem CID |
158385
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
1059.6ºC at 760mmHg
|
| Flash Point |
594.6ºC
|
| Vapour Pressure |
0mmHg at 25°C
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
28
|
| Heavy Atom Count |
72
|
| Complexity |
1900
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCC1=C(CC)C2=CC3=NC(=CN=C4C=C(C(=CC4=NC=C5C(=C(CCCO)C(=N5)C=C1[N-]2)C)OCCOCCOCCOC)OCCOCCOCCOC)C(=C3CCCO)C.CC(=O)[O-].CC(=O)[O-].[Gd+3]
|
| InChi Key |
VAZLWPAHMORDGR-UHFFFAOYSA-L
|
| InChi Code |
InChI=1S/C48H66N5O10.2C2H4O2.Gd/c1-7-35-36(8-2)40-28-42-38(12-10-14-55)34(4)46(53-42)32-50-44-30-48(63-26-24-61-22-20-59-18-16-57-6)47(62-25-23-60-21-19-58-17-15-56-5)29-43(44)49-31-45-33(3)37(11-9-13-54)41(52-45)27-39(35)51-40;2*1-2(3)4;/h27-32,54-55H,7-26H2,1-6H3;2*1H3,(H,3,4);/q-1;;;+3/p-2
|
| Chemical Name |
3-[4,5-diethyl-24-(3-hydroxypropyl)-16,17-bis[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]-10,23-dimethyl-13,20,25,26-tetraza-27-azanidapentacyclo[20.2.1.13,6.18,11.014,19]heptacosa-1(25),2,4,6,8(26),9,11,13,15,17,19,21,23-tridecaen-9-yl]propan-1-ol;gadolinium(3+);diacetate
|
| Synonyms |
PCI0120; PCI-0120; PCI 0120
|
| 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8708 mL | 4.3538 mL | 8.7076 mL | |
| 5 mM | 0.1742 mL | 0.8708 mL | 1.7415 mL | |
| 10 mM | 0.0871 mL | 0.4354 mL | 0.8708 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.
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