| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
LIB3S0280 (72-96 hours) showed significant inhibitory effects on pancreatic cancer cell lines that highly express TBK1, with GI50 values of 2.24 μM (MIA PaCa-2) and 4.71 μM (PANC-1), and IC50 values of 6.64 μM (MIA PaCa-2) and 10.98 μM (PANC-1) (96 hours), respectively [1]. LIB3S0280 (10-20 μM, 3 hours) effectively reduced the phosphorylation levels of AKT (Ser473) and IκBα, key targets of TBK1, in MIA PaCa-2 and PANC-1 cells, thereby inhibiting downstream signaling pathways of TBK1, including the PI3K/AKT and NF-κB pathways [1]. LIB3S0280 (10-20 μM, 48-96 hours) induces G₂/M phase arrest, apoptosis and cellular senescence in pancreatic cancer cells (MIA PaCa-2 and PANC-1) by regulating key regulatory factors such as p-cdc2, p-MPM2, cyclin B1 and p21 [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: MIA PaCa-2 and PANC-1 cells Tested Concentrations: 10 and 20 μM Incubation Duration: 3, 48, 72 and 96 hours Experimental Results: Dose-dependent reduction of IκBα phosphorylation. Reduced AKT phosphorylation at Ser473. p21 levels increased between 48 and 96 hours. Cell viability assay [1] Cell Types: MIA PaCa-2, PANC-1 and SW1990 cells Tested Concentrations: 10 μM Incubation Duration: 72 and 96 hours Experimental Results: Significantly inhibited cell proliferation and cell viability in a concentration-dependent manner, with efficacy comparable to BX-795. It showed stronger inhibitory effects on the MIA PaCa-2 cell line. It had no inhibitory effect on SW1990 cells. Cell cycle analysis [1] Cell Types: MIA PaCa-2 and PANC-1 cells Tested Concentrations: 10 and 20 μM Incubation Duration: 48, 72 and 96 hours Experimental Results: After 48 hours, the proportion of cells in the G2/M phase increased significantly, while the proportion of cells in the sub-G1 phase increased slightly. After 48 hours, the expression level of p-MPM2 was downregulated, while the expression levels of p-cdc2 (tyr15) and cyclin B1 were upregulated. Compared with 48 hours, after 72 hours, the proportion of cells in the G2/M phase decreased slightly, but the proportion of cells in the sub-G1 phase increased. After 96 hours, the proportion of cells in the sub-G1 phase increased significantly, while the proportion of cells in the G2/M phase decreased further.
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| References |
| Molecular Formula |
C22H25CLN4O5
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|---|---|
| Molecular Weight |
460.91
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| Appearance |
Off-white to gray solid
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| SMILES |
OC1=C(OC)C=C(CCNC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Cl)C=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) |
DMSO : ~50 mg/mL (~108.48 mM; with sonication)
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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 | 2.1696 mL | 10.8481 mL | 21.6962 mL | |
| 5 mM | 0.4339 mL | 2.1696 mL | 4.3392 mL | |
| 10 mM | 0.2170 mL | 1.0848 mL | 2.1696 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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