AZD8931 (Sapitinib)

Catalog No.S2192

AZD8931 (Sapitinib) Chemical Structure

Molecular Weight(MW): 473.93

AZD8931 (Sapitinib) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.

Size Price Stock Quantity  
In DMSO USD 320 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock

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2 Customer Reviews

  • Western blot analysis confirm suppression of the biomarker p-EGFR upon treatment with EGFR TKIs in U-CH1 and UM-Chor1. Cells were serum-starved overnight before they were treated with a range of concentrations of the EGFR inhibitors for 4 h and then EGF-spiked (50 ng/ml) for 15 min. Endogenous controls (non-serum-starved, non-EGF-spiked), untreated controls (serum-starved, non-EGF-spiked) and vehicle controls (serum-starved, treated with 2.5% DMSO, EGF-spiked) were included. Phospho-EGFR was measured by western blot.

    J Pathol, 2016, 239(3):320-34.. AZD8931 (Sapitinib) purchased from Selleck.

    J Immunol 2014 192(2), 722-31. AZD8931 (Sapitinib) purchased from Selleck.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description AZD8931 (Sapitinib) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.
Targets
ErbB2 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
ErbB3 [1]
(Cell-free assay)
3 nM 4 nM 4 nM
In vitro

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. [1]

In vivo AZD8931 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. [1]

Protocol

Kinase Assay
+ Expand

Isolated kinase assays:

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 Research
+ Expand
  • Cell lines: 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,
  • Concentrations: 0.001-10 μM
  • Incubation Time: 96 hours
  • Method:

    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.


    (Only for Reference)
Animal Research
+ Expand
  • Animal Models: BT474c, Calu-3, LoVo, FaDu and PC-9 xenografts in Swiss nude or severe combined immunodeficient (Charles River) mice.
  • Formulation: Suspended in a 1% (v/v) solution of polyoxyethylenesorbitan monooleate (Tween 80) in deionized water
  • Dosages: 6.25-50 mg/kg
  • Administration: Gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL (84.4 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 5 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 473.93
Formula

C23H25ClFN5O3

CAS No. 848942-61-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01862003 Recruiting Metastatic Colorectal Cancer|Recurrent Colorectal Cancer University College, London|Cancer Research UK|AstraZeneca|National Institute for Health Research, United Kingdom May 2014 Phase 1
NCT02117167 Recruiting Non-small Cell Lung Cancer Metastatic UNICANCER|IFCT|Fondation ARC|AstraZeneca April 2014 Phase 2
NCT02299999 Recruiting Metastatic Breast Cancer UNICANCER|Fondation ARC|AstraZeneca April 2014 Phase 2
NCT01596530 Terminated Breast Neoplasm AstraZeneca June 2012 Phase 1
NCT01579578 Terminated Metastatic, Gastric or Gastro-oesophageal Junction, Cancer AstraZeneca April 2012 Phase 2
NCT01330758 Completed Healthy AstraZeneca April 2011 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID