| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Axl-IN-21 (compound 9im) (0.1–0.5 μM) in SNU668 and MKN1 gastric cancer cells, even when co-cultured with CAF, dose-dependently inhibited AXL phosphorylation and reversed epithelial-mesenchymal transition (restoring E-cadherin and reducing N-cadherin expression); and restored chemosensitivity by blocking CAF-induced AXL activation and downstream signaling, although co-culture with CAF usually reduces the levels of apoptosis markers (cleaved PARP and cleaved Caspase-3) after chemotherapy containing 5-Fluorouracil (5 FU) and cisplatin [1]. Axl-IN-21 (0.5–32 μM) showed lower cytotoxicity than BGB324 in non-cancer cells [1]. Axl-IN-21 (0.1–0.5 μM) inhibited the JAK1/STAT3, PI3K/AKT, and MEK/ERK signaling pathways and reduced CAF-induced enhanced cell migration in SNU668 cells co-cultured with cancer-associated fibroblasts (CAF), even in the presence of CAF conditioned medium or direct co-culture [1]. Axl-IN-21 (0.5–2 μM) inhibited CAF-induced AXL activation, downstream signaling, GC cell migration, and chemotherapeutic resistance in SNU668 cells co-cultured with CAF and/or treated with chemotherapeutic agents [1]. Axl-IN-21 (0.1–0.5 μM) simultaneously inhibited the upregulation of ABCG1 expression and phosphorylation of AXL, JAK1/STAT3, PI3K/AKT, and MEK/ERK in AXL-activated GC SNU668 cells treated with recombinant GAS6 [1]. When combined with CAF and 5-FU, Axl-IN-21 reduced ABCG1 expression and increased the number of cleaved Caspase-3 positive cells, indicating enhanced apoptosis [1]. Axl-IN-21 (0.03-3 μM, 6 h) exhibited strong Axl kinase inhibitory activity in MDA-MB-231 breast cancer cells [2]. Axl-IN-21 (0.04-5 μM, 96-144 h) dose-dependently inhibited TGF-β1-induced Axl activation in MDA-MB-231 breast cancer cells [2]. Axl-IN-21 (0.04-5 μM, 24 h) inhibited the migration and invasion of MDA-MB-231 cells [2].
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| ln Vivo |
Axl-IN-21 (compound 9im) (90 mg/kg, interface, once daily for 3 weeks) increased the expression of E-cadherin in CAF-mixed SNU668 xenografts, indicating that it could inhibit CAF-induced AXL activation and pivot signaling pathways [1]. Axl-IN-21 (30 or 90 mg/kg, interface, once daily for 21 days) was used in a xenograft model of highly metastatic 4T1 breast cancer cells [2].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: MDA-MB-231 Tested Concentrations: 0.03, 0.1, 0.3, 1 and 3 μM Incubation Duration: 6 h Experimental Results: Inhibited phosphorylation of Axl and downstream signaling (pAkt, pAxl). Immunofluorescence[2] Cell Types: MDA-MB-231 Tested Concentrations: 0.04, 0.2, 1 and 5μM Incubation Duration: 96 to 144 h Experimental Results: Dose-dependently restored the protein levels of E cadherin and N-cadherin back to the control levels. Reversed TGF β1-induced expression level changes of E-cadherin (an epithelial marker) and N-cadherin (a meschenchymal marker) EMT markers in MDA-MB-231 cells. Cell Migration Assay [2] Cell Types: MDA-MB-231 Tested Concentrations: 0.2, 1.0, 5.0 μM Incubation Duration: 24 h Experimental Results: Moderately inhibited the migrating process in MDA-MB-231 cells, suppressing the TGF β1 (10 ng/mL)-induced wound closure by ∼24.2%, ∼50.6%, and ∼58.4% at concentrations of 0.2, 1.0, and 5.0 μM. Cell Invasion Assay[2] Cell Types: MDA-MB-231 Tested Concentrations: 0.04, 0.2, 1.0, or 5.0 μM Incubation Duration: 24 h Experimental Results: Inhibited cancer cell invasion by 48.5%, 52.1%, 73.5%, and 78.1% at concentration of 0.04, 0.2, 1.0, and 5.0 μM, respectively. |
| Animal Protocol |
Animal/Disease Models: SNU668 cells (1×106) with or without induced CFAs (1×106, all cells in 100 μL PBS with 50% Matrigel)-BALB/c nude mice (5 weeks old)[1]
Doses: 90 mg/kg Route of Administration: p.o., daily for 3 weeks Experimental Results: Increased E-cadherin expression. Significantly reduced tumor volume and weight when combined with 5-FU whereas either agent alone had only limited effects. Animal/Disease Models: SNU668 cells (1×106) with or without induced CFAs (1×106, all cells in 100 μL PBS with 50% Matrigel)-BALB/c nude mice (5 weeks old)[1] Doses: 90 mg/kg Route of Administration: p.o., daily for 3 weeks Experimental Results: Increases E-cadherin expression. Significantly reduced tumor volume and weight when combined with 5-FU whereas either agent alone had only limited effects. Animal/Disease Models: 4T1 cells (0.5 × 106) induced-female BALB/c mice[2] Doses: 30 or 90 mg/kg Route of Administration: p.o., daily for 21 days Experimental Results: Did not show an obvious effect on growth of the primary tumor. Dose-dependently suppressed both size and number of liver metastases (21.3 and 13.0 in the 30 and 90 mg/kg dosing groups, respectively). |
| References |
| Molecular Formula |
C30H27FN4O5
|
|---|---|
| Molecular Weight |
542.56
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| CAS # |
1958081-87-2
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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 | 1.8431 mL | 9.2156 mL | 18.4311 mL | |
| 5 mM | 0.3686 mL | 1.8431 mL | 3.6862 mL | |
| 10 mM | 0.1843 mL | 0.9216 mL | 1.8431 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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