| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In human lymphoblastoid cells, WI-L2 cells treated with trimethoxylate glucuronate (0.05–1 μM) for six hours show a decrease in adenylate and guanylate, but pyrimidine nucleotides, such as CTP and UTP, show a significant dose-dependent increase [1]. In L1210 mouse leukemia cells, trimethroxate glucuronate (1 μM, 2 h) can decrease dTTP levels by 29% while also decreasing dGTP and dATP. Additionally, it can broadly prevent deoxyuridine from being incorporated into DNA [1].
|
|---|---|
| ln Vivo |
Inbred DBA/2 mice with L1210 leukemia respond well to trimethoxyxate glucuronate (ip, 100-225 mg/kg daily, days 1, 5, and 9) in terms of antitumor activity [1].
|
| Animal Protocol |
Animal/Disease Models: Inbred DBA/2 mice with L1210 leukemia [1]
Doses: 100, 150, 225 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; results on days 1, 5, and 9: maximum lifespan shown T/C value is 171%. Animal/Disease Models: M5076 tumor C57BL/6 mice [1] Doses: 38, 62 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; 1-9 days Experimental Results: demonstrated toxicity at the high dose of 62 mg/kg (>10% early death) and demonstrated no activity at the low dose of 38 mg/kg (lifetime T/C <130%). |
| References | |
| Additional Infomation |
Trimetrexate Glucuronate can cause developmental toxicity according to state or federal government labeling requirements.
Trimetrexate Glucuronate is a lipid soluble methotrexate derivative with potential antineoplastic activity. Trimetrexate glucuronate inhibits the enzyme dihydrofolate reductase, thereby preventing the synthesis of purine nucleotides and thymidylate, with subsequent inhibition of DNA and RNA synthesis. Trimetrexate glucuronate also exhibits antiviral activity. (NCI04) |
| Molecular Formula |
C19H23N5O3.C6H10O7
|
|---|---|
| Molecular Weight |
563.55702
|
| Exact Mass |
563.223
|
| CAS # |
82952-64-5
|
| Related CAS # |
Trimetrexate;52128-35-5
|
| PubChem CID |
54949
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.305 g/cm3
|
| Boiling Point |
647ºC at 760 mmHg
|
| Flash Point |
345.1ºC
|
| LogP |
0.846
|
| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
40
|
| Complexity |
648
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
CC1=C(C=CC2=C1C(=NC(=N2)N)N)CNC3=CC(=C(C(=C3)OC)OC)OC.C(=O)[C@@H]([C@H]([C@@H]([C@@H](C(=O)O)O)O)O)O
|
| InChi Key |
ZCJXQWYMBJYJNB-LRDBBFHQSA-N
|
| InChi Code |
InChI=1S/C19H23N5O3.C6H10O7/c1-10-11(5-6-13-16(10)18(20)24-19(21)23-13)9-22-12-7-14(25-2)17(27-4)15(8-12)26-3;7-1-2(8)3(9)4(10)5(11)6(12)13/h5-8,22H,9H2,1-4H3,(H4,20,21,23,24);1-5,8-11H,(H,12,13)/t;2-,3+,4-,5-/m.0/s1
|
| Chemical Name |
5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline-2,4-diamine;(2S,3S,4S,5R)-2,3,4,5-tetrahydroxy-6-oxohexanoic acid
|
| 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 | 1.7744 mL | 8.8722 mL | 17.7443 mL | |
| 5 mM | 0.3549 mL | 1.7744 mL | 3.5489 mL | |
| 10 mM | 0.1774 mL | 0.8872 mL | 1.7744 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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