Art. -Nr.: HY-13050

Sapitinib

(Synonyms: AZD-8931)

16 Cited Publications

Kundenbewertung

Based on 16 publication(s) in Google Scholar

Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC₅₀s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

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Reinheit: 99.93%
CAS. Nr.: 848942-61-0
Formel: C₂₃H₂₅ClFN₅O₃
Molecular Weight:473.93

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Sapitinib Chemical Structure

CAS. Nr.: 848942-61-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC₅₀s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

IC₅₀ & Target^[1]

EGFR

4 nM (IC₅₀)

ErbB2

3 nM (IC₅₀)

HER3

4 nM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
KB	IC₅₀	4 nM Compound: 2, AZD8931	Inhibition of EGF-stimulated EGFR phosphorylation in human KB cells Inhibition of EGF-stimulated EGFR phosphorylation in human KB cells	[PMID: 24900741]
MCF7	IC₅₀	3 nM Compound: 2, AZD8931	Inhibition of heregulin-stimulated HER2 phosphorylation in human MCF7 cells Inhibition of heregulin-stimulated HER2 phosphorylation in human MCF7 cells	[PMID: 24900741]
MCF7	IC₅₀	4 nM Compound: 2, AZD8931	Inhibition of heregulin-stimulated HER3 phosphorylation in human MCF7 cells Inhibition of heregulin-stimulated HER3 phosphorylation in human MCF7 cells	[PMID: 24900741]

In Vitro

AZD8931 shows potent inhibitory effect on erbB2 in the ligand-independent MCF-7 cl24 cells, with IC₅₀ of 59 nM^[1]. AZD8931 (1 μM) has no significant effect on EGFR expression level, but significantly inhibits phosphorylation of Akt in a time- and dose-dependent manner in both SUM149 and FC-IBC-02 cells. AZD8931 (0.01, 0.1, 1, or 2 μM) inhibits proliferation and induces apoptosis in human IBC cells^[2]. At the cellular level, AZD8931 inhibits EGF-stimulated phosphorylation of EGFR in the KB cell line (IC₅₀: 4 nM) and heregulin-stimulated phosphorylation of HER2 (IC₅₀: 3 nM) and HER3 (IC₅₀: 4 nM) in the MCF-7 cell line. However, AZD8931 exhibits no CYP P450 inhibition (IC₅₀ > 10 μM against 1A2, 2C9, 2C19, 2D6, and 3A4)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AZD8931 (6.25-50 mg/kg, p.o.) significantly inhibits BT474c (breast), Calu-3 (NSCLC), LoVo (colorectal), FaDu (SCCHN), and PC-9 (NSCLC) tumor xenograft growth. AZD8931 is active in xenograft tumor models responsive to EGFR inhibition alone (LoVo and PC-9) or EGFR or erbB2 inhibition (BT474c, Calu-3, and FaDu). AZD8931 causes pharmacodynamic changes in proliferation and apoptosis markers in human tumor xenograft models^[1]. AZD8931 (25 mg/kg, p.o.) significantly inhibits the growth of SUM149 and FC-IBC-02 cells in vivo in SCID mice^[2]. AZD8931 displays favorable oral pharmacokinetics in rat and dog (low clearance and good bioavailability) and low human hepatocyte turnover (Clint < 4.5 μL/min/106 cells). In nude mouse after oral administration at 50 mg/kg, AZD8931 shows improved exposure, and at at 100 mg/kg oral dose once daily, it shows potent tumor growth inhibition activity in the LoVo mouse xenograft model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 848942-61-0
Appearance Solid
Molecular Weight 473.93
Formel C₂₃H₂₅ClFN₅O₃
Color White to off-white
SMILES

O=C(CN1CCC(OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC)CC1)NC
Synonyms

AZD-8931
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (16)

All WB

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Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Pharm Anal

2025 Dec 10.
EMBO J

Tyrosine kinase targeting uncovers oncogenic pathway plasticity in Tasmanian devil transmissible cancers. [Abstract]

2025 Nov 3. PMID: 41184587
J Transl Med

Role of epidermal growth factor receptor inhibitor-induced interferon pathway signaling in the head and neck squamous cell carcinoma therapeutic response. [Abstract]

2021 Jan 23;19(1):43. PMID: 33485341
Cell Rep

Kinetics of RTK activation determine ERK reactivation and resistance to dual BRAF/MEK inhibition in melanoma. [Abstract]

2023 May 29;42(6):112570. PMID: 37252843
Bioorg Chem

Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]

2024 Jun:147:107412. PMID: 38696845
Mol Cancer Res

Endothelial Cells Promote Colorectal Cancer Cell Survival by Activating the HER3-AKT Pathway in a Paracrine Fashion. [Abstract]

2019 Jan;17(1):20-29. PMID: 30131447

Sapitinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Res. 2019 Jan;17(1):20-29. [Abstract]

Western blotting showed that AZD8931 blocks LPEC-1 CM-induced HER3 and AKT phosphorylation. β-actin is used as the loading control.
Molecules

Development of an LC-MS/MS Method for Quantification of Sapitinib in Human Liver Microsomes: In Silico and In Vitro Metabolic Stability Evaluation. [Abstract]

2023 Mar 2;28(5):2322. PMID: 36903565
Mol Med Rep

Identification of the clinical value and biological effects of TTN mutation in liver cancer. [Abstract]

2025 Jun;31(6):165. PMID: 40242970
Mol Pharmacol

Functional RNAi Screens Define Distinct Protein Kinase Vulnerabilities in EGFR-Dependent HNSCC Cell Lines. [Abstract]

2019 Dec;96(6):862-870. PMID: 31554698
Thorac Cancer

Establishing a new human lung squamous cell carcinoma cell line, OMUL-1, expressing insulin-like growth factor 1 receptor and programmed cell death ligand 1. [Abstract]

2025 Jan;16(1):e15488. PMID: 39552203
bioRxiv

2026 Mar 13.
World J Exp Med

Establishment and characterization of a new human gallbladder cancer cell line, OCUG-2. [Abstract]

2025 Jun 20;15(2):100443. PMID: 40546672
bioRxiv

Modeling acquired TKI resistance and effective combination therapeutic strategies in murine RET+ lung adenocarcinoma. [Abstract]

2025 Jun 7:2025.06.04.657911. PMID: 40502048
Research Square Preprint

2024 Nov 06.
bioRxiv

October 28, 2021.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 33 mg/mL (69.63 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1100 mL

10.5501 mL

21.1002 mL

5 mM

0.4220 mL

2.1100 mL

4.2200 mL

10 mM

0.2110 mL

1.0550 mL

2.1100 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[1]

Cells are incubated for 96 h with a suitable range of concentrations of drug to ensure accurate estimation of the inhibitor concentration required to give 50% growth inhibition (GI₅₀; typically between 0.001-10 μM). Viable cell number is determined by 4 h of incubation with MTS Colorimetric Assay reagent and absorbance measured at 490 nm on a spectrophotometer. Each experiment is carried out in triplicate for each drug concentration and data are presented as geometric means. Sensitivity groupings of GI₅₀ data are <1 μM, 1 to 7 μM, and >7 μM.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Swiss nude (nu/nu genotype) and severe combined immunodeficient mice are used. AZD8931, GW572016, and ZD1839 are suspended in a 1% (v/v) solution of polyoxyethylenesorbitan monooleate (Tween 80) in deionized water. Animals are given AZD8931 (6.25-50 mg/kg), GW572016 (100 mg/kg), ZD1839 (100-150 mg/kg), or vehicle control once (qd) or twice daily (bid) by oral gavage. The duration of each study is determined by tumor growth characteristics, with studies ending once tumors reach ~1 cm³. Tumor volume and percentage tumor growth inhibition are calculated and statistical analysis of any change in tumor volume is carried out using a standard t test (P value of lower then 0.05 is considered to be statistically significant).

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hickinson DM, et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer. Clin Cancer Res. 2010 Feb 15;16(4):1159-69. [Content Brief]

[2]. Mu Z, et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor (EGFR), HER2, and HER3: preclinical activity in HER2 non-amplified inflammatory breast cancer models. J Exp Clin Cancer Res. 2014 May 30;33:47. [Content Brief]

[3]. Barlaam B, et al. Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors. ACS Med Chem Lett. 2013 May 31;4(8):742-6. [Content Brief]

[4]. Wang R, et al. Endothelial Cells Promote Colorectal Cancer Cell Survival by Activating the HER3-AKT Pathway in a Paracrine Fashion. Mol Cancer Res. 2018 Aug 21. pii: molcanres.0341.2018. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1100 mL	10.5501 mL	21.1002 mL	52.7504 mL
	5 mM	0.4220 mL	2.1100 mL	4.2200 mL	10.5501 mL
	10 mM	0.2110 mL	1.0550 mL	2.1100 mL	5.2750 mL
	15 mM	0.1407 mL	0.7033 mL	1.4067 mL	3.5167 mL
	20 mM	0.1055 mL	0.5275 mL	1.0550 mL	2.6375 mL
	25 mM	0.0844 mL	0.4220 mL	0.8440 mL	2.1100 mL
	30 mM	0.0703 mL	0.3517 mL	0.7033 mL	1.7583 mL
	40 mM	0.0528 mL	0.2638 mL	0.5275 mL	1.3188 mL
	50 mM	0.0422 mL	0.2110 mL	0.4220 mL	1.0550 mL
	60 mM	0.0352 mL	0.1758 mL	0.3517 mL	0.8792 mL

Keywords

Sapitinib

16 Cited Publications

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Sapitinib

Immunology/Inflammation Compound Library

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Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Sapitinib

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Sapitinib Related Classifications

HY-13050 Related Classifications