Savolitinib
Based on 7 publication(s) in Google Scholar
Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity.
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- Pureté: 99.99%
- CAS No.: 1313725-88-0
- Formule: C17H15N9
- Masse moléculaire:345.36
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Savolitinib
More- J Thorac Oncol. 2019 Oct;14(10):1753-1765. [Abstract]
- Adv Sci (Weinh). 2026 Feb 3:e16660. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- J Sep Sci. 2017 Oct;40(19):3782-3791. [Abstract]
- Separations. 2023 May 9, 10(5), 302.
- Transl Lung Cancer Res. 2020 Oct;9(5):1810-1821. [Abstract]
- bioRxiv. 2024 June 12.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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WB
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PK/PD Analysis
Activité biologique
IC50: 5 nM (c-Met) and 3 nM (p-Met)[1]
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Cell Line
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Type | Value | Description | References |
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| HepG2 | IC50 |
>20 μM
Compound: Savolitinib
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Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 38086189] |
| L02 | IC50 |
>20 μM
Compound: Savolitinib
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Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 38086189] |
| MHCC97H | IC50 |
2.46 nM
Compound: Savolitinib
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Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 38086189] |
| NCI-H441 | IC50 |
0.003 μM
Compound: 28
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Inhibition of c-Met autophosphorylation in human NCI-H441 cells for 1 hr by ELISA
Inhibition of c-Met autophosphorylation in human NCI-H441 cells for 1 hr by ELISA
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[PMID: 25148209] |
| NCI-H441 | IC50 |
0.006 μM
Compound: 28
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Antiproliferative activity against human NCI-H441 cells assessed as HGF-induced proliferation after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H441 cells assessed as HGF-induced proliferation after 72 hrs by MTT assay
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[PMID: 25148209] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:U87MG xenograft model in athymic nude mice[1]
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Dosage:1 mg/kg, 2.5 mg/kg and 10.0 mg/kg
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Administration:Oral administration; daily; for 21 days
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Result:Demonstrated dose-dependent tumor growth inhibition in a U87MG subcutaneous xenograft model.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1313725-88-0
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Appearance Solid
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Masse moléculaire 345.36
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Formule C17H15N9
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Color Off-white to yellow
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SMILES
CN1N=CC(C2=CN=C3C(N([C@H](C4=CN5C(C=C4)=NC=C5)C)N=N3)=N2)=C1
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Synonyms
Volitinib; HMPL-504; AZD-6094
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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 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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J Thorac Oncol
Sensitivity and Resistance of MET Exon 14 Mutations in Lung Cancer to Eight MET Tyrosine Kinase Inhibitors In Vitro. [Abstract]2019 Oct;14(10):1753-1765. PMID: 31279006
Savolitinib purchased from MedChemExpress. Usage Cited in: J Thorac Oncol. 2019 Oct;14(10):1753-1765. [Abstract]
Western blot analyses of transfected Ba/F3 cells in the presence of MET-TKIs at the indicated compounds (Savolitinib (1-100 nM), etc.) concentrations for 2 hours.
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Adv Sci (Weinh)
2026 Feb 3:e16660. PMID: 41632021
Savolitinib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Feb 3:e16660. [Abstract]
Compound testing in pancreatic cancer chip. Representative images 10 showing viability assessment by Hoechst33342 and EthD-2 staining after treatments with Savolitinib at indicated concentrations from 0.01 to 100 μM for 48 hours under 2D condition or after on-chip culture for 1 day or 7 days. Compound effects on BxPC-3 cell viability were analyzed using CellTiter-Glo ATP-assay or imaging detection (n=4).
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Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446
Savolitinib purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
Savolitinib (0.0097-10 μM; 96 h). Dose-effect curve of LCOs derived from the lymph node (LN) and pericardial effusion of P-60. IC50 of osimertinib combined with Savolitinib were 1.32, 0.71, 0.25, and 0.24 μM in these four LCOs, respectively. Compared with IC50 of Savolitinib (only performed in P-60-O3E and P-60-O4E, which were 11.59 and 17.61 μM).
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J Sep Sci
Simultaneous quantification of volitinib and gefitinib in rat plasma by HPLC-MS/MS for application to a pharmacokinetic study in rats. [Abstract]2017 Oct;40(19):3782-3791. PMID: 28749011
Savolitinib purchased from MedChemExpress. Usage Cited in: J Sep Sci. 2017 Oct;40(19):3782-3791. [Abstract]
Concentration-time profiles in rat plasma after intravenous administration of Volitinib (Savolitinib; 8 h) or oral administration of Volitinib, when simultaneously (○) at the dose of 2 mg/kg.
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Transl Lung Cancer Res
SRC and PIM1 as potential co-targets to overcome resistance in MET deregulated non-small cell lung cancer. [Abstract]2020 Oct;9(5):1810-1821. PMID: 33209603 -
Solvant et solubilité
DMSO : ≥ 20.83 mg/mL (60.31 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (6.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (6.02 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Jia H, et al. Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer. J Med Chem. 2014 Sep 25;57(18):7577-89. [Content Brief]
[2]. Gavine PR, et al. Volitinib, a potent and highly selective c-Met inhibitor, effectively blocks c-Met signaling and growth in c-MET amplified gastric cancer patient-derived tumor xenograft models. Mol Oncol. 2015 Jan;9(1):323-33. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8955 mL | 14.4776 mL | 28.9553 mL | 72.3882 mL |
| 5 mM | 0.5791 mL | 2.8955 mL | 5.7911 mL | 14.4776 mL | |
| 10 mM | 0.2896 mL | 1.4478 mL | 2.8955 mL | 7.2388 mL | |
| 15 mM | 0.1930 mL | 0.9652 mL | 1.9304 mL | 4.8259 mL | |
| 20 mM | 0.1448 mL | 0.7239 mL | 1.4478 mL | 3.6194 mL | |
| 25 mM | 0.1158 mL | 0.5791 mL | 1.1582 mL | 2.8955 mL | |
| 30 mM | 0.0965 mL | 0.4826 mL | 0.9652 mL | 2.4129 mL | |
| 40 mM | 0.0724 mL | 0.3619 mL | 0.7239 mL | 1.8097 mL | |
| 50 mM | 0.0579 mL | 0.2896 mL | 0.5791 mL | 1.4478 mL | |
| 60 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2065 mL |
Savolitinib Related Classifications
HY-15959 Related Classifications
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