1. Protein Tyrosine Kinase/RTK
  2. ALK
  3. Alectinib

Alectinib (Synonyms: CH5424802; RO5424802; AF802)

Cat. No.: HY-13011 Purity: 99.84%
Handling Instructions

Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.

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

Alectinib Chemical Structure

Alectinib Chemical Structure

CAS No. : 1256580-46-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 120 In-stock
Estimated Time of Arrival: December 31
100 mg USD 192 In-stock
Estimated Time of Arrival: December 31
200 mg USD 312 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Alectinib:

Top Publications Citing Use of Products

    Alectinib purchased from MCE. Usage Cited in: Cancer Lett. 2017 Aug 1;400:61-68.

    Alectinib inhibits PI3K/Akt/mTOR signaling and induces apoptosis in NB cells. NB-19, Kelly, IMR-32, SH-SY5Y, SK-N-AS and LA-N-6 cells are treated with 10 mM alectinib for various time points as indicated. The anti-b-Actin antibody is used as a loading control for whole cell extracts.

    Alectinib purchased from MCE. Usage Cited in: Cancer Lett. 2017 Aug 1;400:61-68.

    In contrast to tumors treated with DMSO, tumors treated with Alectinib exhibits significantly decreased levels of p-Akt and p-S6. Furthermore, increased PARP and Caspase 3 cleavages are observed in tumors treated with Alectinib compared to controls.

    Alectinib purchased from MCE. Usage Cited in: Cell Death Discov. 2018 May 10;4:56.

    NB39-nu cells are treated with either 1000 nM Crizotinib (CR) or Alectinib (AL) for the indicated times and subjected to immunoblot analysis. CLTC is the loading control.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

    IC50 & Target

    IC50: 1.9 nM(ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)[1]
    Kd: 2.4 nM (ALK)[1]

    In Vitro

    Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT[1].
    Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner[1].

    Western Blot Analysis[1]

    Cell Line: NCI-H2228 cells
    Concentration: 0 nM,10 nM,100 nM, 1000 nM
    Incubation Time: 2 hours
    Result: Inhibition of ALK phosphorylation and signal transduction.

    Cell Viability Assay[1]

    Cell Line: HCC827, A549, or NCIH522 cells
    Concentration: 0-1000 nM
    Incubation Time: 5 days
    Result: Reduced cell activity in a dose-dependent manner.
    In Vivo

    Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed[1].

    Animal Model: SCID or nude mice bearing NCI-H2228 cells[1]
    Dosage: 0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg
    Administration: Oral administration; once daily; for 11 days
    Result: Resulted in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression.
    Clinical Trial
    Molecular Weight

    482.62

    Formula

    C₃₀H₃₄N₄O₂

    CAS No.

    1256580-46-7

    SMILES

    N#CC1=CC2=C(C3=C(N2)C(C)(C4=CC(N5CCC(CC5)N6CCOCC6)=C(C=C4C3=O)CC)C)C=C1

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 6.2 mg/mL (12.85 mM; Need warming)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0720 mL 10.3601 mL 20.7202 mL
    5 mM 0.4144 mL 2.0720 mL 4.1440 mL
    10 mM 0.2072 mL 1.0360 mL 2.0720 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.38 mg/mL (0.79 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 0.38 mg/mL (0.79 mM); Precipitated solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 0.38 mg/mL (0.79 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.84%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Alectinib
    Cat. No.:
    HY-13011
    Quantity: