Alectinib hydrochloride

For research use only.

Catalog No.S5232 Synonyms: AF802 hydrochloride

3 publications

Alectinib hydrochloride Chemical Structure

Molecular Weight(MW): 519.08

Alectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase.

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Biological Activity

Description Alectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase.
Targets
ALK [1]
(Cell-free)
1.9 nM
In vitro

Alectinib inhibits ALK with an IC50 value of 1.9 nmol/L and shows higher selectivity for ALK than for a number of other serine/tyrosine kinases. It also inhibits the ALK gatekeeper mutation L1196M with an IC50 of 1.56 nmol/L. Alectinib is effective with crizotinib-resistant ALK mutations L1196M, F1174L, R1275Q and C1156Y. In the KARPAS-299 (lymphoma), NB-1 (neuroblastoma) and NCI-H2228 (lung cancer) ALK-positive cell lines, alectinib inhibits cell proliferation with IC50 values of 3, 4.5 and 53 nmol/L, respectively[1].

In vivo Alectinib dose-dependently inhibits EML4-ALK positive NCI-H2228 xenograft model at doses ranging from 2 to 20 mg/kg p.o., q.d. Significant efficacy is also achieved in the EML4-ALK L1196M-driven tumors[1]. It has antitumor activity against cancers with ALK gene alterations[2].

Protocol

Cell Research:

[3]

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  • Cell lines: KB cells
  • Concentrations: 0.01-100 μM
  • Incubation Time: 72 h
  • Method:

    ---


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: SCID mice inocubated with subcutaneous tumors
  • Dosages: 60 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 2 mg/mL (3.85 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 519.08
Formula

C30H34N4O2.HCl

CAS No. 1256589-74-8
Storage powder
in solvent
Synonyms AF802 hydrochloride
Smiles Cl.CCC1=C(C=C2C(=C1)C(=O)C3=C([NH]C4=C3C=CC(=C4)C#N)C2(C)C)N5CCC(CC5)N6CCOCC6

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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ALK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID