1. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Epigenetics Cell Cycle/DNA Damage Apoptosis
  2. Anaplastic lymphoma kinase (ALK) mTOR PARP Caspase
  3. ALK-IN-26

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.

For research use only. We do not sell to patients.

ALK-IN-26 Chemical Structure

ALK-IN-26 Chemical Structure

CAS No. : 2447607-85-2

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5 mg USD 98 In-stock
10 mg USD 150 In-stock
25 mg USD 290 In-stock
50 mg USD 460 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

In Vitro

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.

Apoptosis Analysis[1]

Cell Line: GL261
Concentration: 0.5 μM, 1.0 μM, 2.0 μM
Incubation Time: 24 h, 48 h, 72 h
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.

Cell Viability Assay[1]

Cell Line: GL216, U87MG, Hela
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
Incubation Time: 24 h, 48h, 72h
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.

Cell Autophagy Assay[1]

Cell Line: GL261
Concentration: 0.5 μM, 1.0 μM, 2.0 μM
Incubation Time: 24 h
Result: Induced autophagy death in glioblastoma cells.
In Vivo

ALK-IN-26 (5 mg/kg, i.v., single dose) has pharmacokinetic properties in male C57BL6/J mice[1].
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.

Animal Model: Male C57BL/6J mice[1]
Dosage: 5 mg/kg
Administration: Intravenous injection (i.v.), Single dose
Result: Could be rapidly absorbed (Tmax = 0.58 h) with an acceptable half-life (T1/2 = 3.55 h) and bioavailability (F = 38.4%).
Animal Model: Male C57BL/6J mice[1]
Dosage: 20mg/kg
Administration: Intraperitoneal injection (i.p.), Single dose
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.
Molecular Weight

405.51

Formula

C24H23NO3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(C)C=C1)(N2C=C(CC3=CC(C)=C(O)C(C)=C3)C4=C2C=CC=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Purity & Documentation
References

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ALK-IN-26
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HY-156432
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