Sapitinib
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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- Pureté: 99.93%
- CAS No.: 848942-61-0
- Formule: C23H25ClFN5O3
- Masse moléculaire:473.93
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Activité biologique
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) Sapitinib
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Pharm Anal. 2025 Dec 10.
- EMBO J. 2025 Nov 3. [Abstract]
- J Transl Med. 2021 Jan 23;19(1):43. [Abstract]
- Cell Rep. 2023 May 29;42(6):112570. [Abstract]
- Bioorg Chem. 2024 Jun:147:107412. [Abstract]
- Mol Cancer Res. 2019 Jan;17(1):20-29. [Abstract]
- Molecules. 2023 Mar 2;28(5):2322. [Abstract]
- Mol Med Rep. 2025 Jun;31(6):165. [Abstract]
- Mol Pharmacol. 2019 Dec;96(6):862-870. [Abstract]
- Thorac Cancer. 2025 Jan;16(1):e15488. [Abstract]
- bioRxiv. 2026 Mar 13.
- World J Exp Med. 2025 Jun 20;15(2):100443. [Abstract]
- bioRxiv. 2025 Jun 7:2025.06.04.657911. [Abstract]
- Research Square Preprint. 2024 Nov 06.
- bioRxiv. October 28, 2021.
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Activité biologique
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EGFR 4 nM (IC50) |
ErbB2 3 nM (IC50) |
HER3 4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KB | IC50 |
4 nM
Compound: 2, AZD8931
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Inhibition of EGF-stimulated EGFR phosphorylation in human KB cells
Inhibition of EGF-stimulated EGFR phosphorylation in human KB cells
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[PMID: 24900741] |
| MCF7 | IC50 |
3 nM
Compound: 2, AZD8931
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Inhibition of heregulin-stimulated HER2 phosphorylation in human MCF7 cells
Inhibition of heregulin-stimulated HER2 phosphorylation in human MCF7 cells
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[PMID: 24900741] |
| MCF7 | IC50 |
4 nM
Compound: 2, AZD8931
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Inhibition of heregulin-stimulated HER3 phosphorylation in human MCF7 cells
Inhibition of heregulin-stimulated HER3 phosphorylation in human MCF7 cells
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[PMID: 24900741] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 848942-61-0
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Appearance Solid
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Masse moléculaire 473.93
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Formule C23H25ClFN5O3
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Color White to off-white
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SMILES
O=C(CN1CCC(OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC)CC1)NC
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Synonyms
AZD-8931
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (16)
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Journal Impact Factor
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Most Recent
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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 -
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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.
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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 -
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World J Exp Med
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 -
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Solvant et solubilité
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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.
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.
Pureté et documentation
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Fiche technique (279 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
Sapitinib Related Classifications
HY-13050 Related Classifications
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