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

Alectinib Hydrochloride (Synonyms: CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride)

Cat. No.: HY-13011A Purity: 99.95%
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Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 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 Hydrochloride Chemical Structure

Alectinib Hydrochloride Chemical Structure

CAS No. : 1256589-74-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 82 In-stock
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50 mg USD 120 In-stock
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100 mg USD 192 In-stock
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200 mg USD 312 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Alectinib Hydrochloride:

Top Publications Citing Use of Products

    Alectinib Hydrochloride 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 Hydrochloride 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 Hydrochloride 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

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    Description

    Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 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

    519.08

    Formula

    C₃₀H₃₅ClN₄O₂

    CAS No.

    1256589-74-8

    SMILES

    [H]Cl.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 mg/mL (11.56 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9265 mL 9.6324 mL 19.2649 mL
    5 mM 0.3853 mL 1.9265 mL 3.8530 mL
    10 mM 0.1926 mL 0.9632 mL 1.9265 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References

    Purity: 99.95%

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    Keywords:

    AlectinibCH5424802RO5424802AF-802CH 5424802CH-5424802RO 5424802RO-5424802AF802AF 802ALKAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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    Product name:
    Alectinib Hydrochloride
    Cat. No.:
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