| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Troxacitabine, formerly known as BCH-4556; SGX-145; SPD-758; beta-L-OddC, is a potent DNA polymerase inhibitor with the potential for the treatment of acute myeloid leukemia (AML) and solid. In comparison with gemcitabine, troxacitabine was more efficacious against Panc-01 and was equally active against MiaPaCa. Troxacitabine has a unique metabolic and pharmacokinetic profile and significant antileukemic activity. Troxacitabine merits further study in hematologic malignancies.
| ln Vitro |
Hepatocellular carcinoma (HepG2), prostate (PC3, DUI45), non-small cell lung cancer (NCI-H460, NCr-322M), colon (HT29), and renal cancer (CAK-1, A498, RXF-) cell lines have demonstrated cytotoxicity when treated with trisatabine. With an IC50 range of 15-35 μM, they are of pancreatic origin (Pnac-Ol, MiaPa Ca) and 393 SNI2-C.
|
|---|---|
| ln Vivo |
In the Panc-01 model, troxacitabine had substantial activity, as seen by TGI levels of 88.5% and 84.3% at doses of 10 mg/kg and 25 mg/kg, respectively. When comparing the mean final tumor weight of mice treated with troxacitabine to vehicle controls, this difference was statistically significant. Trisatabine's efficacy against the MiaPaCa model is minimal [3]. In human RCC tumor xenograft models, such as CAM-i, A498, RXF-393, and SN12C carcinomas, tresatabine exhibits remarkable efficacy. Animals with CAM-i, A498 and RXF-393 RCC tumors showed excellent responses when doses of 10, 25, and 50 mg/kg were administered intraperitoneally twice a day for five days [2].
|
| References |
|
| Additional Infomation |
Troxacitabine is a nucleobase-containing molecular entity and a carbohydrate derivative.
Troxacitabine is a nucleoside analog with antineoplastic activity. There has been growing interest in its development for the treatment of patients with refractory lymphoproliferative conditions. Troxacitabine is a dioxolane derivative and a novel L-configuration deoxycytidine analogue with potent antineoplastic activity. When incorporated into growing chain during DNA replication, troxacitabine stops DNA polymerization due to its unnatural L-configuration, in contrast to the normal nucleotides with D-configuration. As a result, this agent terminates DNA synthesis upon incorporated into DNA molecules, and consequently interrupts tumor cell proliferation. Drug Indication Investigated for use/treatment in leukemia (myeloid). Mechanism of Action Troxacitabine is activated by cellular kinases and incorporated into DNA, inhibiting its replication. In contrast to other cytosine nucleoside analogs, troxacitabine is resistant to inactivation by cytidine deaminase (CD). Pharmacodynamics Troxacitabine is a beta-L-nucleoside analog, which has shown preclinical antitumor activity in human xenograft tumor models and antileukemic response in patients with relapsed myeloid leukemia. |
| Molecular Formula |
C8H11N3O4
|
|---|---|
| Molecular Weight |
213.19064
|
| Exact Mass |
213.075
|
| CAS # |
145918-75-8
|
| PubChem CID |
454194
|
| Appearance |
White to off-white solid powder
|
| Density |
1.71g/cm3
|
| Boiling Point |
422.5ºC at 760mmHg
|
| Flash Point |
209.3ºC
|
| Vapour Pressure |
6.59E-09mmHg at 25°C
|
| Index of Refraction |
1.694
|
| LogP |
-1.7
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
15
|
| Complexity |
328
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C1[C@H](O[C@H](O1)CO)N2C=CC(=NC2=O)N
|
| InChi Key |
RXRGZNYSEHTMHC-MLWJPKLSSA-N
|
| InChi Code |
InChI=1S/C8H11N3O4/c9-5-1-2-11(8(13)10-5)6-4-14-7(3-12)15-6/h1-2,6-7,12H,3-4H2,(H2,9,10,13)/t6?,7-/m0/s1
|
| Chemical Name |
4-amino-1-[(2S)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]pyrimidin-2-one.
|
| Synonyms |
BCH-4556; SGX-145; SPD-758; beta-L-OddC; BCH4556; SGX145; SPD758; brand name Troxatyl.
|
| 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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 | 4.6907 mL | 23.4533 mL | 46.9065 mL | |
| 5 mM | 0.9381 mL | 4.6907 mL | 9.3813 mL | |
| 10 mM | 0.4691 mL | 2.3453 mL | 4.6907 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA