| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SMU-037 (compound 9y) showed significant activity against A549 (IC50 = 0.9 μM), HCC-78 (IC50 = 1.1 μM) and NCI-H3122 (IC50 = 1.1 μM) cells, and also showed significant inhibitory effects on Ba/F3 ROS1G2032R and Ba/F3 ROS1L2026R cells, with IC50 values of 8.9 nM and 32.0 nM, respectively [1]. SMU-037 (0.001-3 μM, 8 hours) could attenuate the phosphorylation of ROS1 and its downstream key signaling pathway MAPK-ERK in various Ba/F3 and A549 cells in a dose-dependent manner [1]. SMU-037 (0-100 nM, 48 hours) can cause cell cycle arrest (arrested at the G0/G1 phase in ROS1WT cells and at the G2/M phase in ROS1G2032R cells) and induce apoptosis in Ba/F3-ROS1WT and Ba/F3-ROS1G2032R cells [1].
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| ln Vivo |
SMU-037 (15, 30 and 60 mg/kg, by gavage, once daily for 14 days) showed strong tumor growth inhibition in xenograft and brain metastasis models [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Ba/F3-ROS1WT, Ba/F3-ROS1G2032R, Ba/F3-ROS1L2026M and A549-ROS1G2032R cells Tested Concentrations: 1, 10, 100, and 10000 nM, 0.1, 0.3, 1 and 3 μM Incubation Duration: 8 h Experimental Results: Exhibited remarkable inhibitory effects on ROS1G2032R phosphorylation at the concentration of 1000 nM. Slightly inhibited the downstream MAPK-ERK signaling pathway at the concentration of 1000 nM, with efficacy comparable to Cabozantinib. Led to attenuated phosphorylation of ROS1 and the key downstream MAPK-ERK signaling pathway in a dose-dependent manner in Ba/F3-ROS1WT and Ba/F3-ROS1L2026M cells, comparable to Crizotinib. Exhibited a marked suppression of ROS1 phosphorylation at a concentration of 1 μM in A549-ROS1G2032R cells. Cell Cycle Analysis[1] Cell Types: Ba/F3-ROS1WT and Ba/F3-ROS1G2032R cells Tested Concentrations: 0, 10, 30, and 100 nM Incubation Duration: 48 h Experimental Results: Significantly increased the percentage of ROS1WT cells in the G0/G1 phase. Caused a predominant G2/M phase accumulation in ROS1G2032R cells. The G0/G1 phase of ROS1G2032R cells increased from 57.10% (control) to 60.71%, 72.97%, and 85.28%, respectively. The G2/M phase of ROS1G2032R cells increased from 6.14% (control) to 6.98%, 14.42%, and 27.16%, respectively. Apoptosis Analysis[1] Cell Types: Ba/F3-ROS1WT and Ba/F3-ROS1G2032R cells Tested Concentrations: 0, 10, 30, and 100 nM Incubation Duration: 48 h Experimental Results: Induced a dose-dependent increase in apoptosis. Apoptotic rates in ROS1WT cells rose from 13.12% (control) to 16.95%, 31.50%, and 91.87%. Apoptotic rates in ROS1G2032R cells increased from 19.85% (control) to 20.46%, 28.03%, and 54.60%. |
| Animal Protocol |
Animal/Disease Models: Male Balb/c nude mice (16-20 g) injected with Ba/F3 CD74-ROS1G2032R cells[1]
Doses: 15, 30 and 60 mg/kg Route of Administration: i.g., q.d. for 14 days Experimental Results: Effectively suppressed Ba/F3 tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) values of 118, 140, and 156%, respectively. Showed no significant body weight reduction and no morphological changes or side effects in heart, liver and kidney. Significantly inhibited ROS1 phosphorylation in tumor tissue, demonstrating its on-target effect in vivo. Induced prominent alterations in the morphological characteristics of tumor cells, including cellular contraction, agglutination, and marginalization of nuclear chromatin. Significantly reduced expression level of the Ki-67 protein, indicating strong anti-proliferative activity. Animal/Disease Models: Male Balb/c nude mice (16-20 g) injected with A549-ROS1G2032R cells[1] Doses: 15, 30 and 60 mg/kg Route of Administration: i.g., q.d. for 14 days Experimental Results: Demonstrated significant tumor regression at doses of 30 mg/kg and 60 mg/kg, comparable to the positive control Lorlatinib (30 mg/kg). Animal/Disease Models: Male Balb/c nude mice (16-20 g) injected with luciferase-transduced A549-ROS1G2032R cells[1] Doses: 30 and 60 mg/kg Route of Administration: i.g., q.d. for 14 days Experimental Results: Prominently reduced tumor load (as measured using photon flux) in the brain without obvious body weight loss. Could penetrate blood-brain barrier. |
| References |
| Molecular Formula |
C29H29CLF2N4O
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|---|---|
| Molecular Weight |
523.02
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| Appearance |
Typically exists as solids at room temperature
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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 | 1.9120 mL | 9.5599 mL | 19.1197 mL | |
| 5 mM | 0.3824 mL | 1.9120 mL | 3.8239 mL | |
| 10 mM | 0.1912 mL | 0.9560 mL | 1.9120 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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