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    Sapitinib (AZD-8931)
    Sapitinib (AZD-8931)

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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 #: V0567
    CAS #: 848942-61-0Purity ≥98%

    Description: Sapitinib (formerly AZD8931; AZD-8931) is an orally bioactive, reversible and ATP competitive inhibitor of multiple kinases including EGFR, ErbB2/3 with potential antitumor activity. It inhibits  EGFR, ErbB2/3 with IC50s of 4 nM, 3 nM and 4 nM in cell-free assays. It shows potent anti-proliferative activity in vitro against NSCLC cells.

    References: Clin Cancer Res. 2010 Feb 15;16(4):1159-69.

    Related CAS: 1196531-39-1 (difumarate)

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    Molecular Weight (MW)473.93
    FormulaC23H25ClFN5O3
    CAS No.848942-61-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 40 mg/mL (84.4 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo) 30% PEG400+0.5% Tween80+5% propylene glycol: 5 mg/mL
    SynonymsAZD 8931; Sapitinib; AZD 8931; AZD8931; 

    Chemical Name: 2-(4-((4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)-N-methylacetamide

    SMILES Code: O=C(NC)CN1CCC(OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC)CC1


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    In Vitro

    In vitro activity: AZD8931 shows different potency to NSCLC and SCCHN cell lines. AZD8931 has high sensitivity to PC-9 cells (EGFR activating mutation) with GI50 of 0.1 nM and low activity to NCI-1437 cells with GI50 above 10 μM. AZD8931 exhibits more potency against phospho-EGFR, phospho-erbB2 and phospho-erbB3 than either lapatinib or gefitinib in PE/CA-PJ41, PE/CA-PJ49, DOK and FaDu cells.


    Kinase Assay: The intracellular kinase domains of human EGFR and erbB2 are cloned and expressed in the baculovirus/Sf21 system. The inhibitory activity of AZD8931 is determined with ATP at Km concentrations (0.4 mM for erbB2 and 2 mM for EGFR) using the ELISA method. 


    Cell Assay: To determine the antiproliferative activity against cell lines grown in vitro, AZD8931 is tested in a panel of NSCLC and SCCHN cell lines. Cells are incubated for 96 hours with AZD8931 (0.001-10 μM). Viable cell number is determined by 4 hours of incubation with MTS Colorimetric Assay reagent and absorbance measured at 490 nm on a spectrophotometer. Head and neck tumor cell lines (KYSE-30, OE21, PE/CA-PJ15, PE/CA-PJ34 (clone C12), PE/CA-PJ41 (clone D2), PE/CA-PJ49, DOK, Detroit562, RPMI2650, SCC-4, SCC-9, SCC-25, CAL 27, SW579, FaDu, Hs 840.T, KB, KYSE-450, and HEp-2, HN5) and NSCLC cell lines (PC-9).

    In VivoAZD8931 reveals antitumor activity in BT474c, Calu-3, LoVo, FaDu and PC-9 xenografts. AZD8931 could reduce p-Akt, Ki67 expression and p-ERK in BT474c xenografts following acute treatment. AZD8931 also causes induction of the M30 apoptosis marker. Furthermore, AZD8931 shows greater proapoptotic effect compared with gefitinib and lapatinib in LoVo xenografts.
    Animal modelBT474c, Calu-3, LoVo, FaDu and PC-9 xenografts in Swiss nude or severe combined immunodeficient (Charles River) mice.
    Formulation & DosageSuspended in a 1% (v/v) solution of polyoxyethylenesorbitan monooleate (Tween 80) in deionized water; 6.25-50 mg/kg; oral gavage
    References

    Clin Cancer Res. 2010 Feb 15;16(4):1159-69.


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

    AZD8931 (Sapitinib)

    Cellular phospho-EGFR, phospho-erbB2, and phospho-erbB3 geometric IC50 means and 95% confidence intervals for AZD8931, gefitinib, and lapatinib in the (A) PE/CA-PJ41 cell line, (B) PE/CA-PJ49 cell line, (C) DOK cell line, and (D) FaDu cell line. Clin Cancer Res. 2010 Feb 15;16(4):1159-69.

    AZD8931 (Sapitinib)

    Antitumor studies of AZD8931, gefitinib, and lapatinib using (A) BT474c, (B) Calu-3, (C) LoVo, (D) FaDu, and (E) PC-9 xenograft mouse models.

    AZD8931 (Sapitinib)

    Pharmacodynamic effects of AZD8931, lapatinib, and gefitinib.


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