| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
AFP464 (1-50 μM; 5 d) showed dose-dependent cytotoxicity against LM05-E and LM05-Mix mouse breast cancer cells, with LM05-E cells being more sensitive [1].
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|---|---|
| ln Vivo |
AFP464 (12 mg/kg; intraperitoneal injection; once daily for 5 consecutive days) significantly inhibited the growth of M05 breast tumors, reduced breast globule formation capacity, and decreased the frequency of stem cell-like cells and α6 integrin-positive tumor cells in BALB/c mice [1]. AFP464 (35-50 mg/kg; intravenous injection; 14-day cycle, administered on days 1, 3, and 5; 4 cycles in total) inhibited the growth of MDA-MB-468 breast cancer xenografts by 54-57% [2]. AFP464 (35-70 mg/kg; intravenous injection; 14-day cycle, administered on days 1, 3, and 5; 2 cycles in total) did not inhibit the growth of MDA-MB-231 breast cancer xenografts, with 70 mg/kg being the maximum tolerated dose [2].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: LM05-E (epithelial cells), LM05-Mix (epithelial cells and fibroblasts) Tested Concentrations: 1-50 μM Incubation Duration: 5 days Experimental Results: The cell viability of both LM05-E and LM05-Mix cells was reduced, with LM05-E cells showing a higher response to treatment. |
| Animal Protocol |
Animal/Disease Models:BALB/c (2-4 month old females; M05 spontaneous hormone-dependent mammary tumor model, inoculated with M05 tumor cells) [1]
Doses: 1.2 mg/kg; 12 mg/kg Route of Administration: Intraperitoneal injection; once daily; for 5 consecutive days Experimental Results: Significantly inhibited M05 tumor growth, with a median tumor surface area much lower than the control group throughout the study. Effectively reduced the formation of mammary globules derived from M05 tumors. Reduced the number of Lin(-)/CD29hi/CD24+ stem cell-like cells. Significantly reduced the proportion of α6 integrin-positive cells in the tumor. No significant tumor growth inhibition was observed at the 1.2 mg/kg dose. Animal/Disease Models:Athymic BALB/c mice (female, 5-6 weeks old) [2] Doses: 35 mg/kg; 50 mg/kg Route of Administration: Intravenous injection; administered on days 1, 3, and 5 of a 14-day cycle; for a total of 4 cycles Experimental Results: After one cycle, the median inhibition rate of tumor growth was 57%. After two cycles, the median inhibition rate of tumor growth was 54%. It showed statistically significant equivalent antitumor activity compared with the solvent control group. The mice tolerated the treatment well. Animal/Disease Models:Athymic BALB/c mice (female, 5-6 weeks old) [2] Doses: 35 mg/kg; 70 mg/kg Route of Administration: Intravenous injection; administered on days 1, 3, and 5 of a 14-day cycle; for a total of 2 cycles Experimental Results: Neither the 35 mg/kg nor the 70 mg/kg dose inhibited tumor growth. The 35 mg/kg dose was well tolerated. The 70 mg/kg dose resulted in a weight loss of up to 15% in mice, and 1 out of 7 mice died; therefore, this dose was defined as the maximum tolerated dose (MTD). |
| References |
|
| Molecular Formula |
C24H31F3N4O9S2
|
|---|---|
| Molecular Weight |
640.65
|
| Exact Mass |
640.148
|
| CAS # |
468719-53-1
|
| Appearance |
Typically exists as solids at room temperature
|
| LogP |
6.964
|
| SMILES |
CS(=O)(O)=O.FC1=C2C(C(C=C(C3=CC(F)=C(C=C3)NC([C@@H](N)CCCCN)=O)O2)=O)=C(C(F)=C1C)N.CS(=O)(O)=O
|
| Synonyms |
NSC710464
|
| 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
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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 | 1.5609 mL | 7.8046 mL | 15.6091 mL | |
| 5 mM | 0.3122 mL | 1.5609 mL | 3.1218 mL | |
| 10 mM | 0.1561 mL | 0.7805 mL | 1.5609 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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