Sapitinib (AZD8931)

Catalog No.S2192

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.

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.

Purity & Quality Control

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Biological Activity

Description

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	Incubation Time	Activity Description	PMID
human MCF7 cells	NF7QZoNHfW6ldHnvckBie3OjeR?=		M2ribGlvcGmkaYTpc44hd2ZiaHXy[Yd2dGmwLYP0bY12dGG2ZXSgTGVTOiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hVUOINzDj[YxteyxiSVO1NF0{KG6P	NWj5RnNuOjR7MEC3OFE>
human KB cells	MoTqSpVv[3Srb36gZZN{[Xl?		MnPnTY5pcWKrdHnvckBw\iCHR1[td5RqdXWuYYTl[EBGT0[UIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCNQjDj[YxteyxiSVO1NF01KG6P	NEXt[3QzPDlyMEe0NS=>
human MCF7 cells	M{\uZWZ2dmO2aX;uJIF{e2G7		MYXJcohq[mm2aX;uJI9nKGincnXneYxqdi2\|dHnteYxifGWmIFjFVlMheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1ETjdiY3XscJMtKEmFNUC9OEBvVQ>?	MYKyOFkxODd2MR?=
human MCF-7 cl.24 cells	NVvXNpFWTnWwY4Tpc44h[XO\|YYm=	M4HsdlQhcA>?	Ml\NTY5pcWKrdHnvckBw\iCodXzsMYxmdme2aDDISXIzKHCqb4PwbI9zgWyjdHnvckB1emGwc3\lZ5Rm\CCrbjDpckBpfW2jbjDNR2YuPyClbD6yOEBk\WyuczDh[pRmeiB2IHjyd{BjgSCuYYPldkB{[2Gwbnnu[{BndHWxcnXzZ4Vv[2VibXnjdo9xdGG2ZTDjfZRwdWW2comsJGlEPTB;NkCgcm0>	NGTEdnQzPDlyMEe0NS=>

... 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)

References

[1] Hickinson DM, et al. Clin Cancer Res, 2010, 16(4), 1159-1169.

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 Download Sapitinib (AZD8931) SDF

Molecular Weight	473.93
Formula	C₂₃H₂₅ClFN₅O₃
CAS No.	848942-61-0
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-11-16)

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
NCT02117167	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
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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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HER2 Signaling Pathway Map

HER2 Inhibitors with Unique Features

Selective HER2 Inhibitors

CP-724714 : HER2/ErbB2-selective, IC50=10 nM.
Most Potent HER2 Inhibitor

Mubritinib (TAK 165) : HER2/ErbB2, IC50=6 nM.
FDA-approved HER2 Inhibitor

Lapatinib : Approved by FDA for breast cancer.
Classic HER2 Inhibitor

Lapatinib (GW-572016) Ditosylate : Dual EGFR/ErbB2 inhibitor, IC50=10.8/9.2 nM.

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Pexidartinib (PLX3397) ^New

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Lapatinib (GW-572016) Ditosylate

Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
AC480 (BMS-599626)

AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1.
CP-724714

CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.
Neratinib (HKI-272)

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Mubritinib (TAK 165)

Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line. Phase 1.
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Features:A potent EGFR tyrosine kinase inhibitor.

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Sapitinib (AZD8931)