Art. -Nr.: HY-15959

Savolitinib

(Synonyms: Volitinib; HMPL-504; AZD-6094)

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC₅₀s 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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Reinheit: 99.99%
CAS. Nr.: 1313725-88-0
Formel: C₁₇H₁₅N₉
Molecular Weight:345.36

Speicherung:

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

Savolitinib Chemical Structure

CAS. Nr.: 1313725-88-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 5 nM (c-Met) and 3 nM (p-Met)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	>20 μM Compound: Savolitinib	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	[PMID: 38086189]
L02	IC₅₀	>20 μM Compound: Savolitinib	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	[PMID: 38086189]
MHCC97H	IC₅₀	2.46 nM Compound: Savolitinib	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	[PMID: 38086189]
NCI-H441	IC₅₀	0.003 μM Compound: 28	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	[PMID: 25148209]
NCI-H441	IC₅₀	0.006 μM Compound: 28	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	[PMID: 25148209]

In Vivo

Savolitinib (Compound 28; 1-10.0 mg/kg; oral administration; daily; for 21 days; athymic nude mice) demonstrates dose-dependent tumor growth inhibition in a U87MG subcutaneous xenograft model. In addition, none of the mice in the dosing groups exhibits body weight loss during the experiment^[1].

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

Animal Model:

U87MG xenograft model in athymic nude mice^[1]
Dosage:

1 mg/kg, 2.5 mg/kg and 10.0 mg/kg
Administration:

Oral administration; daily; for 21 days
Result:

Demonstrated dose-dependent tumor growth inhibition in a U87MG subcutaneous xenograft model.

Clinical Trial

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

Chemical Information

CAS. Nr. 1313725-88-0
Appearance Solid
Molecular Weight 345.36
Formel C₁₇H₁₅N₉
Color Off-white to yellow
SMILES

CN1N=CC(C2=CN=C3C(N([C@H](C4=CN5C(C=C4)=NC=C5)C)N=N3)=N2)=C1
Synonyms

Volitinib; HMPL-504; AZD-6094
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (7)

All WBPK/PD AnalysisCell Proliferation/Viability Assay

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Journal Impact Factor

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.
Adv Sci (Weinh)

Deep Learning-Powered Scalable Cancer Organ Chip for Cancer Precision Medicine. [Abstract]

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).
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).
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.
Separations

2023 May 9, 10(5), 302.
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
bioRxiv

2024 June 12.

Lösungsmittel & Löslichkeit

In Vitro:

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.

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

2.8955 mL

14.4776 mL

28.9553 mL

5 mM

0.5791 mL

2.8955 mL

5.7911 mL

10 mM

0.2896 mL

1.4478 mL

2.8955 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, 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.

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: ≥ 2.08 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.

Protocol 2

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.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
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]. 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]

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, 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

Keywords

Savolitinib

7 Cited Publications

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Savolitinib

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Publications Citing Use of MedChemExpress (MCE) Savolitinib

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Savolitinib Related Classifications

HY-15959 Related Classifications