2. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Sapitinib

Sapitinib  (Synonyms: AZD-8931)

Cat. No.: HY-13050 Purity: 99.93%
COA Handling Instructions

Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

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

Sapitinib Chemical Structure

Sapitinib Chemical Structure

CAS No. : 848942-61-0

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 73 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 99 In-stock
Estimated Time of Arrival: December 31
50 mg USD 209 In-stock
Estimated Time of Arrival: December 31
100 mg USD 319 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Sapitinib purchased from MCE. Usage Cited in: Mol Cancer Res. 2019 Jan;17(1):20-29.  [Abstract]

    Western blotting showed that AZD8931 blocks LPEC-1 CM-induced HER3 and AKT phosphorylation. β-actin is used as the loading control.

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    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

    IC50 & Target[1]

    EGFR

    4 nM (IC50)

    ErbB2

    3 nM (IC50)

    HER3

    4 nM (IC50)

    In Vitro

    AZD8931 shows potent inhibitory effect on erbB2 in the ligand-independent MCF-7 cl24 cells, with IC50 of 59 nM[1]. AZD8931 (1 μM) has no significant effect on EGFR expression level, but significantly inhibits phosphorylation of Akt in a time- and dose-dependent manner in both SUM149 and FC-IBC-02 cells. AZD8931 (0.01, 0.1, 1, or 2 μM) inhibits proliferation and induces apoptosis in human IBC cells[2]. At the cellular level, AZD8931 inhibits EGF-stimulated phosphorylation of EGFR in the KB cell line (IC50: 4 nM) and heregulin-stimulated phosphorylation of HER2 (IC50: 3 nM) and HER3 (IC50: 4 nM) in the MCF-7 cell line. However, AZD8931 exhibits no CYP P450 inhibition (IC50 > 10 μM against 1A2, 2C9, 2C19, 2D6, and 3A4)[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    AZD8931 (6.25-50 mg/kg, p.o.) significantly inhibits BT474c (breast), Calu-3 (NSCLC), LoVo (colorectal), FaDu (SCCHN), and PC-9 (NSCLC) tumor xenograft growth. AZD8931 is active in xenograft tumor models responsive to EGFR inhibition alone (LoVo and PC-9) or EGFR or erbB2 inhibition (BT474c, Calu-3, and FaDu). AZD8931 causes pharmacodynamic changes in proliferation and apoptosis markers in human tumor xenograft models[1]. AZD8931 (25 mg/kg, p.o.) significantly inhibits the growth of SUM149 and FC-IBC-02 cells in vivo in SCID mice[2]. AZD8931 displays favorable oral pharmacokinetics in rat and dog (low clearance and good bioavailability) and low human hepatocyte turnover (Clint < 4.5 μL/min/106 cells). In nude mouse after oral administration at 50 mg/kg, AZD8931 shows improved exposure, and at at 100 mg/kg oral dose once daily, it shows potent tumor growth inhibition activity in the LoVo mouse xenograft model[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    473.93

    Appearance

    Solid

    Formula

    C23H25ClFN5O3
    CAS No.
    SMILES

    O=C(CN1CCC(OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC)CC1)NC
    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 : ≥ 33 mg/mL (69.63 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1100 mL 10.5501 mL 21.1002 mL
    5 mM 0.4220 mL 2.1100 mL 4.2200 mL
    10 mM 0.2110 mL 1.0550 mL 2.1100 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: ≥ 2.5 mg/mL (5.28 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.93%

    COA (247 KB) LCMS (264 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cells are incubated for 96 h with a suitable range of concentrations of drug to ensure accurate estimation of the inhibitor concentration required to give 50% growth inhibition (GI50; typically between 0.001-10 μM). Viable cell number is determined by 4 h of incubation with MTS Colorimetric Assay reagent and absorbance measured at 490 nm on a spectrophotometer. Each experiment is carried out in triplicate for each drug concentration and data are presented as geometric means. Sensitivity groupings of GI50 data are <1 μM, 1 to 7 μM, and >7 μM.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Swiss nude (nu/nu genotype) and severe combined immunodeficient mice are used. AZD8931, GW572016, and ZD1839 are suspended in a 1% (v/v) solution of polyoxyethylenesorbitan monooleate (Tween 80) in deionized water. Animals are given AZD8931 (6.25-50 mg/kg), GW572016 (100 mg/kg), ZD1839 (100-150 mg/kg), or vehicle control once (qd) or twice daily (bid) by oral gavage. The duration of each study is determined by tumor growth characteristics, with studies ending once tumors reach ~1 cm3. Tumor volume and percentage tumor growth inhibition are calculated and statistical analysis of any change in tumor volume is carried out using a standard t test (P value of lower then 0.05 is considered to be statistically significant).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Sapitinib848942-61-0AZD-8931AZD8931AZD 8931EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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