Alectinib (CH5424802) hydrochloride

Catalog No.S5232 Synonyms: AF802, RO5424802, RG-7853

For research use only.

Alectinib (AF802, CH5424802, RO5424802, RG-7853) is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase.

Alectinib (CH5424802) hydrochloride Chemical Structure

CAS No. 1256589-74-8

Selleck's Alectinib (CH5424802) hydrochloride has been cited by 19 publications

Purity & Quality Control

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Biological Activity

Description Alectinib (AF802, CH5424802, RO5424802, RG-7853) 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 (from reference)

Cell Research:

[3]

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

    ---

Animal Research:

[2]

  • Animal Models: SCID mice inocubated with subcutaneous tumors
  • Dosages: 60 mg/kg
  • Administration: Oral administration

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 519.08
Formula

C30H34N4O2.HCl

CAS No. 1256589-74-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=CC2=C(C=C1N3CCC(CC3)N4CCOCC4)C(C5=C(C2=O)C6=C(N5)C=C(C=C6)C#N)(C)C.Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

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