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| ln Vitro |
In GL216 cells, ALK-IN-26 (0.5-2 μM, 24 h) can suppress ALK activity [1]. In GL216, U87MG, and Hela cells, ALK-IN-26 (0.5–10 μM, 24-72 h) can suppress GL216 and U87MG activity, but it has little effect on Hela cell activity [1]. In GL216 cells, mTOR protein expression can be decreased by ALK-IN-26 (0.5-2 μM, 24 h) [1]. In both GL261 and U87MG cells, ALK-IN-26 (0.5-2 μM, 24 h) markedly decreased the levels of p-ERK1/2 protein, increased those of p-JNK, and had no effect on p-AKT or p-STAT3 protein[1]. In GL261 cells, autophagy can be induced by ALK-IN-26 (0.5-2 μM, 24 h) [1]. In GL261 cells, cleaved-PARP (c-PARP) and cleaved-caspase-3 (c-caspase 3) protein levels are elevated by ALK-IN-26 (0.5 μM-2 μM, 24-72 h) [1]. GL261 cells undergo apoptosis in response to ALK-IN-26 (0.5 μM–2 μM, 24-72 h) [1].
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| ln Vivo |
Male C57BL6/J mice exhibit the pharmacokinetic characteristics of ALK-IN-26 (5 mg/kg, iv, single dose)[1]. In male C57BL6/J mice, ALK-IN-26 (20 mg/kg, ip, single dose) can cross the blood-brain barrier[1]. Male C57BL6/J mice were used for the pharmacokinetic analysis[1]; the pharmacokinetic properties were T1/2(h) Tmax(h) Cmax (ng/mL) AUC(0-8) (h*ng/mL) AUC(0 -∞) (h*ng/mL) MRT(0-8) (h) MRT(0-∞) (h) V∞ (L/kg) V2 (L/kg) bioavailability F (%) iv(5mg/kg) 1.13 0.08 1978.21 884.88 924.56 0.63 0.84 4.59 8.40 ip(5mg/kg) 3.55 0.58 117.57 339.79 420.50 2.25 4.60 / / / /
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: GL261 Tested Concentrations: 0.5 μM, 1.0 μM, 2.0 μM Incubation Duration: 24 h, 48 h, 72 h Experimental Results: Induced apoptosis of glioblastoma in a concentration- and time-dependent manner, and caused the cells (24.5%) entered the S phase but barely proceeded to the G2/M phase when treated with 1 μM for 72 h. Cell Viability Assay[1] Cell Types: GL216, U87MG, Hela Tested Concentrations: 0.5 μM, 1.0 μM, 2.0 μM , 5 μM, 10 μM for GL216 and U87MG cells 5 μM, 10 μM, 20 μM, 40 μM, 80 μM, 160 μM for Hela cells Incubation Duration: 24 h, 48h, 72h Experimental Results: Inhibited the activity of GL216 cells with the inhibition rate of cells at 80% when incubated with 2 μM for 72 h and inhibited U87MG cells viability with a dose- and time-dependent manner, while demonstrated limited inhibition on Hela cells, even at 160 μM, the inhibition rate is less than 50 %. Can inhibit the activity of ALK tyrosine kinase with a dose-dependent manner. Cell Autophagy Assay[1] Cell Types: GL261 Tested Concentrations: 0.5 μM, 1.0 μM, 2.0 μM Inc |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 J mice[1]
Doses: 5 mg/kg Route of Administration: intravenous (iv) injection ( iv), Single dose Experimental Results: Could be rapidly absorbed (Tmax = 0.58 h) with an acceptable half-life (T1/2 = 3.55 h) and bioavailability (F = 38.4%). Animal/Disease Models: Male C57BL/6J mice[1] Doses: 20mg/kg Route of Administration: intraperitoneal (ip) injection (ip), Single dose Experimental Results: Could enter the body at concentrations up to 2.7μmol/kg (after 2 h administration at 20 mg/kg) and penetrate the blood-brain barrier. |
| References |
[1]. Feng L, et al. Synthesis and Bioevaluation of 3-(Arylmethylene) indole Derivatives: Discovery of a Novel ALK Modulator with Antiglioblastoma Activities[J]. Journal of Medicinal Chemistry, 2023.
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| Molecular Formula |
C24H23NO3S
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|---|---|
| Molecular Weight |
405.51
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| CAS # |
2447607-85-2
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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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4660 mL | 12.3302 mL | 24.6603 mL | |
| 5 mM | 0.4932 mL | 2.4660 mL | 4.9321 mL | |
| 10 mM | 0.2466 mL | 1.2330 mL | 2.4660 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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