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Sapitinib (AZD8931)
Catalog No.S2192
For research use only.
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.
CAS No. 848942-61-0
Selleck's Sapitinib (AZD8931) has been cited by 41 publications
Purity & Quality Control
Choose Selective HER2 Inhibitors
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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. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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| 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 (from reference)
| Kinase Assay: |
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|---|---|
| Cell Research: |
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| Animal Research: |
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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 |
5 mg/mL |
Chemical Information
| Molecular Weight | 473.93 | ||
|---|---|---|---|
| Formula | C23H25ClFN5O3 |
||
| CAS No. | 848942-61-0 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CNC(=O)CN1CCC(CC1)OC2=C(C=C3C(=C2)C(=NC=N3)NC4=C(C(=CC=C4)Cl)F)OC | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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%
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% ddH2O
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT01596530 | Terminated | Drug: Drug-AZD8931|Drug: Drug-Placebo | Breast Neoplasm | AstraZeneca | June 2012 | Phase 1 |
| NCT01579578 | Terminated | Drug: AZD8931|Drug: Placebo|Drug: Paclitaxel | Metastatic Gastric or Gastro-oesophageal Junction Cancer | AstraZeneca | April 2012 | Phase 2 |
| NCT01330758 | Completed | Drug: AZD8931 | Healthy | AstraZeneca | April 2011 | Phase 1 |
| NCT01284595 | Completed | Drug: [14C] AZD8931 | Healthy | AstraZeneca | March 2011 | Phase 1 |
| NCT01151215 | Terminated | Drug: AZD8931|Drug: anastrozole|Drug: Placebo | Neoplasms|Breast Neoplasms|Breast Cancer | AstraZeneca | June 2010 | Phase 2 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
Tech Support
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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