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	NGnMZ21HfW6ldHnvckBie3OjeR?=		MWrJcohq[mm2aX;uJI9nKGincnXneYxqdi2\|dHnteYxifGWmIFjFVlIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1ETjdiY3XscJMtKEmFNUC9N{BvVQ>?	NHPuZlIzPDlyMEe0NS=>
human KB cells	NUi3d3dsTnWwY4Tpc44h[XO\|YYm=		M3e3WmlvcGmkaYTpc44hd2ZiRVfGMZN1cW23bHH0[YQhTUeIUjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iS1KgZ4VtdHNuIFnDOVA:PCCwTR?=	MknqNlQ6ODB5NEG=
human MCF7 cells	MXXGeY5kfGmxbjDhd5NigQ>?		NWj1PW4yUW6qaXLpeIlwdiCxZjDo[ZJm\3WuaX6td5RqdXWuYYTl[EBJTVJ\|IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCPQ1[3JINmdGy\|LDDJR\|UxRTRibl2=	MX:yOFkxODd2MR?=
human MCF-7 cl.24 cells	M3jtV2Z2dmO2aX;uJIF{e2G7	NWiwcFFnPCCq	NVzkUmQ2UW6qaXLpeIlwdiCxZjDmeYxtNWynbnf0bEBJTVJ{IIDoc5NxcG:{eXzheIlwdiC2cnHud4Zm[3SnZDDpckBqdiCqdX3hckBOS0ZvNzDjcE4zPCClZXzsd{Bi\nSncjC0JIhzeyCkeTDsZZNmeiC\|Y3Hucolv\yCobIXvdoV{[2WwY3WgcYlkem:ybHH0[UBkgXSxbXX0dpktKEmFNUC9OlAhdk1?	M{XWeVI1QTByN{Sx

... 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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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

Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Phase 3.
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)

Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.
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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Gefitinib (ZD1839)

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Features:A potent EGFR tyrosine kinase inhibitor.

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Sapitinib (AZD8931)