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    ASP3026
    ASP3026

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0612
    CAS #: 1097917-15-1Purity ≥98%

    Description: ASP3026 (ASP-3026; ASP 3026) is an orally bioavailable inhibitor of ALK (anaplastic lymphoma kinase) with potential antineoplastic activity. It inhibits ALK with an IC50 of 3.5 nM. ALK is a validated target for treating ALK positive non-small cell lung cancer (NSCLC). ASP3026 demonstrates high anti-proliferative activity in vitro against various cancer cells such as NCI-H2228and 3T3 cells which express EML4-ALK variant 1, 2 and 3. It also exhibied high in vivo antitumor efficacy in mice xenografted with NCI-H2228 cells expressing EML4-ALK.

    References: Mol Cancer Ther. 2014 Feb;13(2):329-40; Oncotarget. 2014 Jul 30;5(14):5750-63;  2018;66(3):251-262.

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    Molecular Weight (MW)580.74
    FormulaC29H40N8O3S
    CAS No.1097917-15-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 14 mg/mL (24.1 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILESO=S(C1=CC=CC=C1NC2=NC=NC(NC3=CC=C(N4CCC(N5CCN(C)CC5)CC4)C=C3OC)=N2)(C(C)C)=O
    SynonymsASP-3026; ASP 3026; ASP3026;  

    Chemical Name: N2-[2-Methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-1,3,5-triazine-2,4-diamine

    InChi Key: MGGBYMDAPCCKCT-UHFFFAOYSA-N

    InChi Code: InChI=1S/C29H40N8O3S/c1-21(2)41(38,39)27-8-6-5-7-25(27)33-29-31-20-30-28(34-29)32-24-10-9-23(19-26(24)40-4)36-13-11-22(12-14-36)37-17-15-35(3)16-18-37/h5-10,19-22H,11-18H2,1-4H3,(H2,30,31,32,33,34)

    SMILES Code: O=S(C1=CC=CC=C1NC2=NC=NC(NC3=CC=C(N4CCC(N5CCN(C)CC5)CC4)C=C3OC)=N2)(C(C)C)=O


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    In Vitro

    In vitro activity: ASP3026 shows more selective ALK inhibition in a Tyr-kinase panel than PF02341066. ASP3026 inhibits the growth of NCI-H2228, a human NSCLC tumor cell line endogenously expressing EML4-ALK variant 3, with an IC50 value of 64.8 nM.


    Kinase Assay: ASP3026 inhibited ALK activity in an ATP-competitive manner and had an inhibitory spectrum that differed from that of crizotinib, a dual ALK/MET inhibitor. 


    Cell Assay: In mice xenografted with NCI-H2228 cells expressing EML4-ALK, orally administered ASP3026 was well absorbed in tumor tissues, reaching concentrations >10-fold higher than those in plasma, and induced tumor regression with a wide therapeutic margin between efficacious and toxic doses. In the same mouse model, ASP3026 enhanced the antitumor activities of paclitaxel and pemetrexed without affecting body weight. ASP3026 also showed potent antitumor activities, including tumor shrinkage to a nondetectable level, in hEML4-ALK transgenic mice and prolonged survival in mice with intrapleural NCI-H2228 xenografts. In an intrahepatic xenograft model using NCI-H2228 cells, ASP3026 induced continuous tumor regression, whereas mice treated with crizotinib showed tumor relapse after an initial response. Finally, ASP3026 exhibited potent antitumor activity against cells expressing EML4-ALK with a mutation in the gatekeeper position (L1196M) that confers crizotinib resistance. Taken together, these findings indicate that ASP3026 has potential efficacy for NSCLC and is expected to improve the therapeutic outcomes of patients with cancer with ALK abnormality.

    In VivoASP3026, administered to mice bearing subcutaneous NCI-H2228 tumor xenografts as twice daily oral dosing for 14 days, induces dose dependent anti-tumor effects starting at 1 mg/kg with strong regression at 10, 30 and 100 mg/kg.
    Animal modelMice wtih NCI-H2228 tumor xenografts
    Formulation & Dosage10, 30 and 100 mg/kg; s.c.
    ReferencesMol Cancer Ther. 2014 Feb;13(2):329-40; Oncotarget. 2014 Jul 30;5(14):5750-63.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    ASP3026

    ASP3026 reduces the tyrosine kinase activity of NPM-ALK, downregulates the phosphorylation of NPM-ALK and target proteins, and induces biochemical effects consistent with apoptosis. Oncotarget. 2014 Jul; 5(14): 5750–5763.

    ASP3026

    ASP3026 overcomes the resistance to crizotinib in NPM-ALK+ ALCL.

    ASP3026

    ASP3026 suppresses NPM-ALK+ ALCL tumor cell growth in vivo. Oncotarget. 2014 Jul 30;5(14):5750-63.


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