Physicochemical Properties
| Molecular Formula | C47H77N3O11 |
| Molecular Weight | 860.13 |
| CAS # | 2055494-50-1 |
| Appearance | White to off-white solid powder |
| 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) |
Biological Activity
| Targets | Argininosuccinate synthetase (ASS1)[1] |
| ln Vitro | Colorectal cancer cell lines are strongly inhibited by LM2I (0µM~10µM, 48h) [1]. In colorectal cancer cells, LM2I (2µM, 15d) suppresses the EGFR pathway [1]. Through EGFR, LM2I suppresses colorectal cancer cells [1]. |
| ln Vivo | In a nude mouse xenograft tumor model, LM2I (2.5 mg/kg, intraperitoneally administered, every other day for 28 days) reduced tumor growth[1]. |
| Cell Assay |
Cell Viability Assay[1] Cell Types: CRC cell (HT29, SW480, SW620, HCT116, LoVo, RKO, and DLD1) Tested Concentrations: 0µM, 1.25µM, 2.5µM, 3.75µM, 5.00µM, 6.25µM, 7.5µM, 8.75 µM,10µM Incubation Duration: 48h Experimental Results: Inhibited the viability of HT29, SW480, SW620, HCT116, LoVo, RKO, and DLD1 cells. Cell Proliferation Assay[1] Cell Types: HT29 and SW480 cells Tested Concentrations: 0.75µM,1µM Incubation Duration: 14d Experimental Results: Had almost no effect on EGFR-KO cells. Western Blot Analysis[1] Cell Types: HT29, SW480, SW620, HCT116, LoVo, RKO, DLD1 cell Tested Concentrations: 2µM Incubation Duration: 0~15d Experimental Results: EGFR protein levels were higher than control group. Time-dependently inhibited the protein levels of EGFR and Dramatically diminished relative to phosphorylation. |
| Animal Protocol |
Animal/Disease Models: Female athymic BALB/c nude mice xenograft model(injected subcutaneously (sc) into the flank region with HT29 cell)[1]. Doses: 2.5 mg/kg/day Route of Administration: intraperitoneal (ip) injection, every other day for 28 days Experimental Results: The tumor weight was Dramatically lower than that of the control group, and the tumor cell density was lower. |
| References |
[1]. Spinosyn A and Its Derivative Inhibit Colorectal Cancer Cell Growth via the EGFR Pathway. J Nat Prod. 2023 Sep 8. |
Solubility Data
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1626 mL | 5.8131 mL | 11.6261 mL | |
| 5 mM | 0.2325 mL | 1.1626 mL | 2.3252 mL | |
| 10 mM | 0.1163 mL | 0.5813 mL | 1.1626 mL |