| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 1g | |||
| Other Sizes |
| Targets |
Talotrexin targets dihydrofolate reductase (DHFR), a key enzyme in folate metabolism. It is a reduced folate carrier (RFC) specific inhibitor and selectively inhibits RFC transport.
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|---|---|
| ln Vitro |
In vitro, talotrexin ammonium inhibits tumor growth by targeting DHFR. It binds to and inhibits the function of DHFR, resulting in inhibition of folate metabolism, DNA synthesis, and cell division.
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| ln Vivo |
In vivo, talotrexin ammonium has demonstrated anti-tumor activity in a wide range of cancer models. It improves anti-tumor activity by targeting DHFR.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for talotrexin typically involve evaluating its inhibitory activity against purified DHFR using spectrophotometric assays. IC50 values are determined by measuring the inhibition of DHFR-mediated reduction of dihydrofolate.
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| Cell Assay |
For in vitro cell-based assays, talotrexin ammonium is dissolved in aqueous buffers and applied to cultured cancer cells at concentrations ranging from 1 nM to 10 µM. Effects on cell proliferation, DNA synthesis, and cell cycle progression are assessed after 24-72 hours of treatment.
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| Animal Protocol |
In vivo animal studies commonly use mouse xenograft models. Talotrexin ammonium is administered intravenously or intraperitoneally at doses ranging from 0.1-10 mg/kg. Anti-tumor efficacy is evaluated by measuring tumor volume, tumor weight, and histopathology.
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| ADME/Pharmacokinetics |
Talotrexin ammonium has a molecular formula of C27H30N10O6 and a molecular weight of 590.59 g/mol. It is hydrosoluble.
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| Toxicity/Toxicokinetics |
Talotrexin ammonium has a manageable toxicity profile. As an antifolate, it may cause myelosuppression and gastrointestinal toxicity.
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| References | |
| Additional Infomation |
Tarlotrexate ammonium salt is the ammonium salt of tarlotrexate, an analogue of aztreon, and possesses potential antitumor activity. As a folate antagonist, tarlotrexate binds to and inhibits dihydrofolate reductase, thereby suppressing folate metabolism, DNA synthesis, and cell division. Tarlotrexate is water-soluble and can be actively transported into cells via reduced folate carriers (RFCs), thus it is unlikely to be associated with P-glycoprotein-mediated multidrug resistance.
Talotrexin ammonium is a nonpolyglutamatable classic antifolate that has been developed as a potential antineoplastic agent. It is an analogue of aminopterin with improved properties. |
| Molecular Formula |
C27H30N10O6
|
|---|---|
| Molecular Weight |
590.5905
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| Exact Mass |
590.234
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| CAS # |
648420-92-2
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| Related CAS # |
648420-92-2 (ammonium);113857-87-7 (free);
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| PubChem CID |
9938420
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
43
|
| Complexity |
949
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| Defined Atom Stereocenter Count |
1
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| SMILES |
OC(C(CCCNC(C1C=CC=CC=1C(=O)O)=O)NC(C1C=CC(=CC=1)NCC1C=NC2=C(C(N)=NC(N)=N2)N=1)=O)=O.N
|
| InChi Key |
CURXCENNYPPKOS-FYZYNONXSA-N
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| InChi Code |
InChI=1S/C27H27N9O6.H3N/c28-21-20-22(36-27(29)35-21)32-13-16(33-20)12-31-15-9-7-14(8-10-15)23(37)34-19(26(41)42)6-3-11-30-24(38)17-4-1-2-5-18(17)25(39)40;/h1-2,4-5,7-10,13,19,31H,3,6,11-12H2,(H,30,38)(H,34,37)(H,39,40)(H,41,42)(H4,28,29,32,35,36);1H3/t19-;/m0./s1
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| Chemical Name |
azane;2-[[(4S)-4-carboxy-4-[[4-[(2,4-diaminopteridin-6-yl)methylamino]benzoyl]amino]butyl]carbamoyl]benzoic acid
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| HS Tariff Code |
2934.99.9001
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| 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)
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| 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
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|---|---|
| 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 | 1.6932 mL | 8.4661 mL | 16.9322 mL | |
| 5 mM | 0.3386 mL | 1.6932 mL | 3.3864 mL | |
| 10 mM | 0.1693 mL | 0.8466 mL | 1.6932 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.
Link: https://clinicaltrials.gov/ct2/show/NCT00098514
Conditions:Unspecified Adult Solid Tumor, Protocol SpecificLink: https://clinicaltrials.gov/ct2/show/NCT00088023
Conditions:NeoplasmsLink: https://clinicaltrials.gov/ct2/show/NCT00112060
Conditions:Non-Small-Cell Lung Carcinoma
Title:A Study to Evaluate PT-523 in Patients With Refractory Leukemia
Status:Withdrawn
updateDate:2013-12-04
Ctid:NCT00129558
Link: https://clinicaltrials.gov/ct2/show/NCT00129558
Conditions:LeukemiaProducts are for research use only; We do not sell to patients
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