| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Axl 3.23 nM (IC50) Mer Tyro3
|
|---|---|
| ln Vitro |
Axl-IN-17 can inhibit multiple kinases such as TYRO3, MER, MET, and RON at a concentration of 1 μM [1]. Axl-IN-17 exhibits anti-proliferative activity in BaF3/TEL-AXL cells with an IC50 value of <1 nM[1]. Axl-IN-17 (1 nM, 2 h) inhibits AXL phosphorylation and its downstream signaling pathways [1].
|
| ln Vivo |
Axl-IN-17 (oral, 3 mg/kg, once daily) has good pharmacokinetic properties, with a half-life of 10.09 hours and an AUC value of 59815 ng·h/mL[1]. Axl-IN-17 (po, 25, 50, 100 mg/kg, once daily for seven days) showed anti-tumor effects in AXL-driven tumor xenograft mice[1]. Pharmacokinetic analysis of AXL-IN-17 in male Sprague-Dawley mice[1] Route Dose (mg/kg) AUC0→∞ (ng·h/mL) T1/2 (h) Tmax (h) Cmax (ng/mL) MRT0→∞(h) po 3 mg/kg 59815 10.09 2 2906 16.5
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: BaF3/TEL-AXL Tested Concentrations: 1 nM Incubation Duration: 72 h Experimental Results: Inhibited proliferation activity in BaF3/TEL-AXL cells. Western Blot Analysis[1] Cell Types: BaF3/TEL-AXL Tested Concentrations: 1 nM Incubation Duration: 2 h Experimental Results: Inhibited phosphorylation of AXL and its downstream signaling |
| Animal Protocol |
Animal/Disease Models: Male Sprague-Dawley rats /pharmacokinetic[1]
Doses: 3 mg/kg (p.o.), once daily Route of Administration: Oral gavage Experimental Results: Revealed a T1/2 value of 10.09 h and an AUC value of 59815 ng•h/mL. Animal/Disease Models: BaF3/TEL-AXL xenograft mice[1] Doses: 25, 50 or 100 mg/kg, once daily for 7 days Route of Administration: Oral gavage Experimental Results: Induced tumor regression. |
| References |
| Molecular Formula |
C32H27F2N7O
|
|---|---|
| Molecular Weight |
563.60
|
| 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) |
Typically soluble in DMSO (e.g. 10 mM)
|
|---|---|
| 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 | 1.7743 mL | 8.8715 mL | 17.7431 mL | |
| 5 mM | 0.3549 mL | 1.7743 mL | 3.5486 mL | |
| 10 mM | 0.1774 mL | 0.8872 mL | 1.7743 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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