ALK-IN-26
Based on 1 Customer Validation
ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 has good pharmacokinetic properties and blood-brain barrier (BBB) permeability. ALK-IN-26 can induce apoptosis, autophagy and necrosis. ALK-IN-26 can be used in glioblastoma studies.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.87%
- CAS 番号: 2447607-85-2
- 分子式: C24H23NO3S
- 分子量:405.51
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| GL261 | IC50 |
1.35 μM
Compound: 4a
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Anti-proliferative activity against mouse GL261 cells assessed as cell viability incubated for 2 hrs by CCK8 assay
Anti-proliferative activity against mouse GL261 cells assessed as cell viability incubated for 2 hrs by CCK8 assay
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[PMID: 37861443] |
| U-87MG ATCC | IC50 |
7.25 μM
Compound: 4a
|
Anti-proliferative activity against human U-87 MG cells assessed as cell viability incubated for 2 hrs by CCK8 assay
Anti-proliferative activity against human U-87 MG cells assessed as cell viability incubated for 2 hrs by CCK8 assay
|
[PMID: 37861443] |
ALK-IN-26 (0.5-2 μM, 24 h) can inhibit the activity of ALK in GL216 cells[1].
ALK-IN-26 (0.5-2 μM, 24 h) can reduce the expression of mTOR protein in GL216 cells [1].
[1].
ALK-IN-26 (0.5-2 μM, 24 h) significantly decreases p-ERK1/2 protein level and enhances p-JNK protein level in GL261 and U87MG cells, while has little effect on p-AKT and p-STAT3 protein levels[1].
ALK-IN-26 (0.5μM-2.0 μM, 24h) can induce autophagy in GL261 cells[1].
ALK-IN-26 (0.5 μM-0.5 μM, 24-72 h) increases the protein levels of cleaved-PARP (c-PARP) and cleaved-caspase-3 (c-caspase 3) in GL261 cells[1].
ALK-IN-26 (0.5 μM-2μM, 24-72 h) induces apoptosis in GL261 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GL261
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Concentration:0.5 μM, 1.0 μM, 2.0 μM
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Incubation Time:24 h, 48 h, 72 h
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Result: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.
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Cell Line:GL216, U87MG, Hela
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Concentration: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
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Incubation Time:24 h, 48h, 72h
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Result: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 showed 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.
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Cell Line:GL261
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Concentration:0.5 μM, 1.0 μM, 2.0 μM
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Incubation Time:24 h
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Result:Induced autophagy death in glioblastoma cells.
ALK-IN-26 is (20 mg/kg, i.p., single dose) able to penetrate the blood-brain barrier in male C57BL6/J mice[1].
Pharmacokinetic parameters of C57BL6/J in male rats (n = 3) [1]
| Pharmacokinetic property | 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) | bioavailablity F (%) |
| i.v.(5mg/kg) | 1.13 | 0.08 | 1978.21 | 884.88 | 924.56 | 0.63 | 0.84 | 4.59 | 8.89 | 38.40 |
| i.p.(5mg/kg) | 3.55 | 0.58 | 117.57 | 339.79 | 420.50 | 2.25 | 4.60 | / | / | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice[1]
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Dosage:5 mg/kg
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Administration:Intravenous injection (i.v.), Single dose
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Result:Could be rapidly absorbed (Tmax = 0.58 h) with an acceptable half-life (T1/2 = 3.55 h) and bioavailability (F = 38.4%).
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Animal Model:Male C57BL/6J mice[1]
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Dosage:20mg/kg
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Administration:Intraperitoneal injection (i.p.), Single dose
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Result: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.
化学情報
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CAS 番号 2447607-85-2
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性状 Solid
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分子量 405.51
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分子式 C24H23NO3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(C)C=C1)(N2C=C(CC3=CC(C)=C(O)C(C)=C3)C4=C2C=CC=C4)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 125 mg/mL (308.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (283 KB)
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SDS (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4660 mL | 12.3302 mL | 24.6603 mL | 61.6508 mL |
| 5 mM | 0.4932 mL | 2.4660 mL | 4.9321 mL | 12.3302 mL | |
| 10 mM | 0.2466 mL | 1.2330 mL | 2.4660 mL | 6.1651 mL | |
| 15 mM | 0.1644 mL | 0.8220 mL | 1.6440 mL | 4.1101 mL | |
| 20 mM | 0.1233 mL | 0.6165 mL | 1.2330 mL | 3.0825 mL | |
| 25 mM | 0.0986 mL | 0.4932 mL | 0.9864 mL | 2.4660 mL | |
| 30 mM | 0.0822 mL | 0.4110 mL | 0.8220 mL | 2.0550 mL | |
| 40 mM | 0.0617 mL | 0.3083 mL | 0.6165 mL | 1.5413 mL | |
| 50 mM | 0.0493 mL | 0.2466 mL | 0.4932 mL | 1.2330 mL | |
| 60 mM | 0.0411 mL | 0.2055 mL | 0.4110 mL | 1.0275 mL | |
| 80 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.7706 mL | |
| 100 mM | 0.0247 mL | 0.1233 mL | 0.2466 mL | 0.6165 mL |