| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In NanoBRET assays, SBP-5147 (compound 5) bound to ULK1 in HEK293T cells with an IC50 value of 47 nM[1]. In transfected HEK293T cells, SBP-5147 (10 μM; 1 h) inhibited the phosphorylation of downstream substrates Beclin-1 (Ser15) and Vps34 (Ser249) of ULK1 by approximately 80%[1]. Under nutrient-deprived conditions, SBP-5147 (10 μM; 18 h) inhibited autophagy flux in A549 cells and reduced the number of cells with high autophagy flux[1]. SBP-5147 (72 h) reduced the viability of A549, HCC827, H1373 and H1975 cells with IC50 values of 91, 49, 40 and 35 nM, respectively[1]. SBP-5147 (1 μM; 8–24 h) can induce caspase-dependent apoptosis in A549 cells[1]. SBP-5147 (15–30 nM; 72 h) can significantly upregulate the expression of total MHC-I protein in H1373, HCC827 and A549 cells[1]. In ADP-Glo biochemical assays, SBP-5147 can effectively inhibit ULK1 kinase activity (IC50 = 2 nM) and ULK2 kinase activity (IC50 = 53 nM)[2]. SBP-5147 (48 h) can induce the degradation of ATG13 in A549 non-small cell lung cancer (NSCLC) cells, with an IC50 of 4.5 μM[2].
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| ln Vivo |
SBP-5147 (10 mg/kg; oral; single dose) reduced the protein levels of ATG13 and ATG101 in the liver and lung tissues of C57BL/6J mice, indicating that it can persistently target and inhibit autophagy [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: HEK293T cells transfected with Myc-tagged WT ULK1 and Flag-tagged Beclin-1 or Vps34 Tested Concentrations: 10 μM Incubation Duration: 1 hour Experimental Results: Compared with DMSO-treated cells, phosphorylation of Beclin-1 at Ser15 was inhibited by approximately 80%. Compared with DMSO-treated cells, phosphorylation of Vps34 at Ser249 was inhibited by approximately 80%. Autophagy assay [1] Cell Types: A549 NSCLC cells expressing mCherry-GFP-LC3 reporter gene Tested Concentrations: 10 μM Incubation Duration: 18 hours Experimental Results: Compared with cells treated with EBSS alone, the percentage of cells exhibiting high autophagy flux was reduced, and the cell population was shifted to medium and low autophagy flux. Apoptosis Analysis [1] Cell Types: A549, H1975 non-small cell lung cancer cells Tested Concentrations: 1 μM Incubation Duration: 24 hours (imaging); 8 hours (Western blot) Experimental Results: Caspase-dependent apoptosis was induced in A549 cells. Emricasan eliminated cell death, and zVAD-fmk partially inhibited cell death. PARP and caspase-3 cleavage were induced, a process that could be blocked by apoptosis inhibitors.
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| Animal Protocol |
Animal/Disease Models:C57BL/6J (8-week-old female) [1]
Doses: 10 mg/kg Route of Administration: Oral; Single dose Experimental Results: The drug resulted in a progressive and significant decrease in ATG13 and ATG101 protein levels in liver and lung tissues. At 24 hours post-administration, ATG13 and ATG101 levels remained significantly reduced (SBP-5147 was almost completely cleared from plasma) compared to the solvent control group. At 4, 8, and 24 hours post-administration, both protein levels were significantly lower than in the solvent control group. |
| References |
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| Molecular Formula |
C17H18F3N5
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|---|---|
| Molecular Weight |
349.35
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| CAS # |
1884222-37-0
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
FC(F)(F)C1=C(NC2CC2)N=C(NC3=CC(CCNC4)=C4C=C3)N=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 | 2.8625 mL | 14.3123 mL | 28.6246 mL | |
| 5 mM | 0.5725 mL | 2.8625 mL | 5.7249 mL | |
| 10 mM | 0.2862 mL | 1.4312 mL | 2.8625 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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