Sapitinib (AZD8931)

For research use only.

Catalog No.S2192

26 publications

Sapitinib (AZD8931) Chemical Structure

Molecular Weight(MW): 473.93

Sapitinib (AZD8931) 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.

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Selleck's Sapitinib (AZD8931) has been cited by 26 publications

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Biological Activity

Description Sapitinib (AZD8931) 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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7 cells NF;RT5BHfW6ldHnvckBie3OjeR?= MlX5TY5pcWKrdHnvckBw\iCqZYLl[5VtcW5vc4TpcZVt[XSnZDDISXIzKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOS0Z5IHPlcIx{NCCLQ{WwQVMhdk1? MUKyOFkxODd2MR?=
human KB cells NIm4TGtHfW6ldHnvckBie3OjeR?= NWnUbo9[UW6qaXLpeIlwdiCxZjDFS2Yue3SrbYXsZZRm\CCHR1\SJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDLRkBk\WyuczygTWM2OD12IH7N NFq1NIgzPDlyMEe0NS=>
human MCF7 cells M1m2VmZ2dmO2aX;uJIF{e2G7 MkPhTY5pcWKrdHnvckBw\iCqZYLl[5VtcW5vc4TpcZVt[XSnZDDISXI{KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOS0Z5IHPlcIx{NCCLQ{WwQVQhdk1? NIm0O5EzPDlyMEe0NS=>
human MCF-7 cl.24 cells MnjKSpVv[3Srb36gZZN{[Xl? MYC0JIg> Mn;OTY5pcWKrdHnvckBw\iCodXzsMYxmdme2aDDISXIzKHCqb4PwbI9zgWyjdHnvckB1emGwc3\lZ5Rm\CCrbjDpckBpfW2jbjDNR2YuPyClbD6yOEBk\WyuczDh[pRmeiB2IHjyd{BjgSCuYYPldkB{[2Gwbnnu[{BndHWxcnXzZ4Vv[2VibXnjdo9xdGG2ZTDjfZRwdWW2comsJGlEPTB;NkCgcm0> M2DzdVI1QTByN{Sx

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
pEGFR / EGFR / pAKT / AKT / pERK / ERK ; 

PubMed: 27102572     


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.

HER3 / p-HER3 / HER2 / p-HER2 / p-PRAS40 / p-S6 / p-4EBP1 / p-FOXO / PARP / cleaved PARP; 

PubMed: 26095475     


(A) BT474c or HCC1954 cells were treated for 24 h with increasing concentrations of AZD5363 ±0.3 μM or 1 μM AZD8931, respectively. Protein lysates were analysed by immunoblot with the indicated antibodies. Blots are representative of blots from 2–3 separate experiments.

27102572 26095475
Growth inhibition assay
Cell viability; 

PubMed: 28638122     


Growth control graphs showing effect of selected HER-family TKIs in doubling concentrations on growth of breast cancer cell lines. (a) EGFR reversible inhibitor erlotinib. (b) Dual EGFR/HER2 reversible inhibitor lapatinib. (c) Pan-HER reversible inhibitor sapitinib. (d) Pan-HER irreversible inhibitor canertinib. (e) Pan-HER irreversible inhibitor afatinib. Sulforhodamine B colorimetric assay was used to determine the effect of treatment of breast cancer cell lines with doubling dilutions of HER-family inhibiting TKIs. The irreversible pan-inhibitors (e.g. afatinib, canertinib, neratinib) were consistently more effective than the reversible dual and pan inhibitors (e.g. lapatinib, sapitinib), which were in turn more effective than the reversible EGFR inhibitors (e.g. erlotinib, gefitinib). Each point is a representative of the mean ± SD of triplicate samples.

28638122
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:

[1]
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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:

[1]
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  • 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:

[1]
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  • Animal Models: BT474c, Calu-3, LoVo, FaDu and PC-9 xenografts in Swiss nude or severe combined immunodeficient (Charles River) mice.
  • Dosages: 6.25-50 mg/kg
  • Administration: Gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL (84.4 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing. 		5 mg/mL

* 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
Smiles CNC(=O)CN1CCC(CC1)OC2=C(OC)C=C3N=CN=C(NC4=C(F)C(=CC=C4)Cl)C3=C2

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01596530 Terminated Drug: Drug-AZD8931|Drug: Drug-Placebo Breast Neoplasm AstraZeneca June 2012 Phase 1
NCT01579578 Terminated Drug: AZD8931|Drug: Placebo|Drug: Paclitaxel Metastatic Gastric or Gastro-oesophageal Junction Cancer AstraZeneca April 2012 Phase 2
NCT01330758 Completed Drug: AZD8931 Healthy AstraZeneca April 2011 Phase 1
NCT01284595 Completed Drug: [14C] AZD8931 Healthy AstraZeneca March 2011 Phase 1
NCT01151215 Terminated Drug: AZD8931|Drug: anastrozole|Drug: Placebo Neoplasms|Breast Neoplasms|Breast Cancer AstraZeneca June 2010 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID