| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Axl
|
|---|---|
| ln Vitro |
Anticancer agent 109 (10 μM, 48 hours) induces G1 phase arrest and promotes late apoptosis, but does not alter DNA synthesis. It inhibits Gas6 and Axl in A549 cells and inhibits proteins related to the Gas6-Axl axis in PANC-1 cells [1].
|
| ln Vivo |
Anticancer agent 109 (3 mg/kg, i.p., 1 day for A549 tumor model 3, 6 times a week for 85 days for PANC-1 tumor model) significantly reduced tumor size and weight in nude mouse xenograft models[1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: MCF-7; PANC-1; MDA-MB-231; HT-29; DU145; U937; A549; PANC-1 Tested Concentrations: 30 μM Incubation Duration: 48 h Experimental Results: Inhibited the growth of cancer cells, and was up to 20-fold safer against normal cells and up to 5.4-fold more active than Sunitinib against the cancer cells. Inhibited growth with IC50s of 2.0 μM (MCF-7); 2.8 μM (MDA-MB- 231); 4.6 μM (HT-29); 1.1 μM (DU145); 6.7 μM (U937); 4.2 μM (A549); 4.0 μM (PANC-1). Apoptosis Analysis[1] Cell Types: PANC-1 Tested Concentrations: 1 μM , 5 μM , 10 μM Incubation Duration: 48 h Experimental Results: Increased the sub-G1 fraction and induced late apoptosis. Western Blot Analysis[1] Cell Types: A549; PANC-1 Tested Concentrations: 10 μM Incubation Duration: 48 h Experimental Results: Inhibited Gas6 and Axl in A549 and PANC-1 cell, increased the expression ratio of Bax/Bcl-2 and inhibited p-PI3K and p-AKT in PANC-1 cell. RT-PCR[1] Cell Types: PANC-1 Tested Concentrations: 3 μM; 5 μM 10 μM Incubation Duration: 48 h Experimental Results: Inhibited Gas6 and Axl. |
| Animal Protocol |
Animal/Disease Models: A549 or PANC-1 xenografted in BALB/c-nu (nude) mice [1].
Doses: 1 mg/kg; 3 mg/kg Route of Administration: intraperitoneal (ip) injection 6 times a week Experimental Results: Promoted tumor regression to around a quarter with 1 mg/kg, smaller but not eliminated with 3 mg/kg in A549 models. Promoted tumor regression to around a quarter with 3 mg/kg in PANC-1 models. |
| References |
| Molecular Formula |
C19H15N3O2
|
|---|---|
| Molecular Weight |
317.34
|
| CAS # |
2097497-16-8
|
| Appearance |
Typically exists as solid at room temperature
|
| 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)
|
| 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
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 | 3.1512 mL | 15.7560 mL | 31.5119 mL | |
| 5 mM | 0.6302 mL | 3.1512 mL | 6.3024 mL | |
| 10 mM | 0.3151 mL | 1.5756 mL | 3.1512 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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