2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. Anaplastic lymphoma kinase (ALK) mTOR PARP Caspase
  4. 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.

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ALK-IN-26 Chemical Structure

ALK-IN-26 Chemical Structure

CAS No. : 2447607-85-2

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ALK-IN-26 Related Antibodies

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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.

ALK-IN-26 Related Antibodies

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.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ALK-IN-26 Related Classifications

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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.

Keywords:

ALK-IN-262447607-85-2Anaplastic lymphoma kinase (ALK)mTORPARPCaspaseAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Mammalian target of Rapamycinpoly ADP ribose polymeraseGlioblastomaALK modulatorTarget drugU87MGGL261Inhibitorinhibitorinhibit

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