Sapitinib (AZD8931)

Catalog No.S2192

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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In DMSO USD 320 In stock
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USD 320 In stock
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Cited by 10 Publications

3 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.. Sapitinib (AZD8931) purchased from Selleck.

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

  • (A) Western blotting of FYN and E-cadherin expression in the MCF10A cells treated with EGF or FGF2 with or without their inhibitors AZD8931 or BGJ398. (B) Western blotting of FYN and N-cadherin expression in the MDAMB-231 cells treated with AZD8931 or BGJ398.

    Oncol Rep, 2016, 36(2):1000-6. Sapitinib (AZD8931) purchased from Selleck.

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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 MUXGeY5kfGmxbjDhd5NigQ>? M4i5RWlvcGmkaYTpc44hd2ZiaHXy[Yd2dGmwLYP0bY12dGG2ZXSgTGVTOiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hVUOINzDj[YxteyxiSVO1NF0{KG6P MofJNlQ6ODB5NEG=
human KB cells NEjtVo1HfW6ldHnvckBie3OjeR?= MV\Jcohq[mm2aX;uJI9nKEWJRj3zeIlufWyjdHXkJGVITlJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEuEIHPlcIx{NCCLQ{WwQVQhdk1? M32xSlI1QTByN{Sx
human MCF7 cells M17OfmZ2dmO2aX;uJIF{e2G7 NV3OUpM4UW6qaXLpeIlwdiCxZjDo[ZJm\3WuaX6td5RqdXWuYYTl[EBJTVJ|IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCPQ1[3JINmdGy|LDDJR|UxRTRibl2= NGPHXoQzPDlyMEe0NS=>
human MCF-7 cl.24 cells MVnGeY5kfGmxbjDhd5NigQ>? M3G5SFQhcA>? MmTPTY5pcWKrdHnvckBw\iCodXzsMYxmdme2aDDISXIzKHCqb4PwbI9zgWyjdHnvckB1emGwc3\lZ5Rm\CCrbjDpckBpfW2jbjDNR2YuPyClbD6yOEBk\WyuczDh[pRmeiB2IHjyd{BjgSCuYYPldkB{[2Gwbnnu[{BndHWxcnXzZ4Vv[2VibXnjdo9xdGG2ZTDjfZRwdWW2comsJGlEPTB;NkCgcm0> MXqyOFkxODd2MR?=

... Click to View More Cell Line Experimental Data
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]
+ 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:

[1]
+ 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:

[1]
+ 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 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01862003 Active not recruiting Metastatic Colorectal Cancer|Recurrent Colorectal Cancer University College London|Cancer Research UK|AstraZeneca|National Institute for Health Research United Kingdom May 2014 Phase 2
NCT01862003 Active not recruiting Metastatic Colorectal Cancer|Recurrent Colorectal Cancer University College London|Cancer Research UK|AstraZeneca|National Institute for Health Research United Kingdom May 2014 Phase 2
NCT02299999 Recruiting Metastatic Breast Cancer UNICANCER|Fondation ARC|AstraZeneca April 7 2014 Phase 2
NCT02117167 Active not recruiting Non-small Cell Lung Cancer Metastatic UNICANCER|IFCT|Fondation ARC|AstraZeneca April 23 2014 Phase 2
NCT02299999 Recruiting Metastatic Breast Cancer UNICANCER|Fondation ARC|AstraZeneca April 7 2014 Phase 2
NCT02117167 Active not recruiting Non-small Cell Lung Cancer Metastatic UNICANCER|IFCT|Fondation ARC|AstraZeneca April 23 2014 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID