Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: ~1 μM (DNA-PK)[3]
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ln Vitro |
Canfosfamide (TLK-28) has an IC50 value of less than 1 µM and inhibits the catalytic kinase activity of purified DNA-dependent protein kinase (DNA-PK), but it does not directly harm DNA very much[2]. In a dose-dependent manner, canfosfamide (TER286) inhibits MCF-7, NIH-3T3, and M7609[3].
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ln Vivo |
Canfosfamide (TER286) shows a more potent antitumor effect with increased dosing[3].
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Cell Assay |
Cell Proliferation Assay[3]
Cell Types: MCF-7, NIH-3T3 and M7609 Tested Concentrations: 0-100 μM Incubation Duration: Co-incubated for 2 h then removed and incubated for 5 days in MCF-7; co-incubated for 10 days in NIH-3T3; co-incubated for 48 h in M7609 Experimental Results: Inhibited these cancer cell lines in a dose-dependent manner. |
Animal Protocol |
Animal/Disease Models: BALB/c nude mice (sc with tumors of M7609, MX -1 human breast tumor, lung tumor[3]
Doses: 150 mg/kg for M7609 xenografts; 400 mg/kg or 200 mg/kg for other xenografts Route of Administration: iv, single dosage for M7609 xenograft; ip, single dosage for other xenografts ; ip, daily for 5 days Experimental Results: The best response to TER286 was for the MX-1 human breast tumor treated with an aggressive regimen (daily for 5 days), under which nearly all of the tumors were either severely growth inhibited or substantially regressed . |
References |
[1]. Dourado DF, et al. Mechanism of glutathione transferase P1-1-catalyzed activation of the prodrug canfosfamide (TLK286, TELCYTA). Biochemistry. 2013 Nov 12;52(45):8069-78.
[2]. Tew KD. TLK-286: a novel glutathione S-transferase-activated prodrug. Expert Opin Investig Drugs. 2005 Aug;14(8):1047-54. [3]. Morgan AS, et al. Tumor efficacy and bone marrow-sparing properties of TER286, a cytotoxin activated by glutathione S-transferase. Cancer Res. 1998 Jun 15;58(12):2568-75. |
Molecular Formula |
C26H40CL4N5O10PS
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Molecular Weight |
787.47
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CAS # |
158382-37-7
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Related CAS # |
439943-59-6 (HCl);158382-37-7;
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(O)[C@H](NC([C@@H](NC(CC[C@H](N)C(O)=O)=O)CS(=O)(CCOP(N(CCCl)CCCl)(N(CCCl)CCCl)=O)=O)=O)C1=CC=CC=C1
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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 | 1.2699 mL | 6.3494 mL | 12.6989 mL | |
5 mM | 0.2540 mL | 1.2699 mL | 2.5398 mL | |
10 mM | 0.1270 mL | 0.6349 mL | 1.2699 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.