Art. -Nr.: HY-16446

SAR125844

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SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC₅₀ is 4.2 nM and K_i is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer.

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Reinheit: 98.17%
CAS. Nr.: 1116743-46-4
Formel: C₂₅H₂₃FN₈O₂S₂
Molecular Weight:550.63

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

SAR125844 Chemical Structure

CAS. Nr.: 1116743-46-4

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

c-Met

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle MEK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MKN-45	IC₅₀	7 nM Compound: 12; SAR125844	Antiproliferative activity against human MKN45 cells assessed as reduction in [14C]-thymidine incorporation incubated for 96 hrs by beta counting method Antiproliferative activity against human MKN45 cells assessed as reduction in [14C]-thymidine incorporation incubated for 96 hrs by beta counting method	[PMID: 27355974]

In Vitro

SAR125844 (1-10000 nM, 96 h) inhibits proliferation in H-460 cells, HCT116 cells, H1993 cells, EBC-1 cells, SNU-5 cells, OE33 cells, Hs 746T cells and MKN-45 cells^[1].
SAR125844 (1-300 nM, 24 72 h) promotes apoptosis in SNU-5 cells^[1].
SAR125844 (3-1000 nM, 20 h) inhibits HGF-mediated tumor cell migration in PC-3 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

H-460 cells, HCT116 cells, H1993 cells, EBC-1 cells, SNU-5 cells, OE33 cells, Hs 746T cells and MKN-45 cells
Concentration:

1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM, 10000 nM
Incubation Time:

96 h
Result:

Inhibited cell proliferation in all cell lines with MET gene amplification, with IC₅₀ values in the nanomolar range (1-7 nM), with the exception of the lung cancer cell line NCI-H1573.

Apoptosis Analysis^[1]

Cell Line:

SNU-5 cells
Concentration:

1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
Incubation Time:

24 h, 48 h, 72 h
Result:

Induced massive apoptosis in SNU-5 cells at 48 and 72 hours, with a relative EC₅₀ value of 6 nM and a plateau of 60% at 72 hours.

Cell Migration Assay ^[1]

Cell Line:

H-460 cells, HCT116 cells, H1993 cells, EBC-1 cells, SNU-5 cells, OE33 cells, Hs 746T cells and MKN-45 cells
Concentration:

3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time:

20 h
Result:

Inhibited cell migration with an IC₅₀ value of 26 nM。

In Vivo

SAR125844 (45 mg/kg, Intravenous injection, single dose) results in tumor regression in SNU-5 and Hs 746T tumor-bearing mice^[1].
SAR125844 (20 mg/kg, Intravenous injection, o single dose) nanoformulation results in long duration pharmacodynamic impact and tumor regression in MET-amplified gastric tumor models^[1].
SAR125844 (20 mg/kg, Intravenous injection, single dose) shows MET kinase inhibition was complete at 4 h (96%), significant at 24 h (80%), and partial at 48 h (61%) in mice bearing xenograft tumor of the MET-amplified Hs 746T human gastric tumor cell line^[3].

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

Animal Model:

SNU-5 and Hs 746T tumor-bearing mice^[1]
Dosage:

45 mg/kg
Administration:

Intravenous injection (i.v.)
Result:

Resulted in complete and almost complete tumor regression in 3 of 8 mice and 5 of 8 mice, respectively.

Animal Model:

MET-amplified gastric tumor model mice^[1]
Dosage:

5 mg/kg, 11 mg/kg, 21 mg/kg, 53 mg/kg, 106 mg/kg, 213 mg/kg
Administration:

Intravenous injection (i.v.)
Result:

Resulted complete tumor regression in 7 of 8 of mice at 53, 106, and 213 mg/kg and partial regression at 11 and 21 mg/kg.
Showed more than 80% MET inhibition at all doses and maintained for 96 hours at 213 mg/kg, 72 hours at 106 mg/kg, and 48 hours at 53 mg/kg.
Showed complete or near-complete regression (92%–99%) and maintained for 7 days at 106 mg/kg, and 48 hours at 53 mg/kg.

Clinical Trial

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

Chemical Information

CAS. Nr. 1116743-46-4
Appearance Solid
Molecular Weight 550.63
Formel C₂₅H₂₃FN₈O₂S₂
Color Light yellow to yellow
SMILES

O=C(NCCN1CCOCC1)NC2=NC3=CC=C(SC4=NN=C5C=CC(C6=CC=C(F)C=C6)=NN54)C=C3S2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 45 mg/mL (81.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.8161 mL

9.0805 mL

18.1610 mL

5 mM

0.3632 mL

1.8161 mL

3.6322 mL

10 mM

0.1816 mL

0.9081 mL

1.8161 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 90% Corn Oil

Solubility: ≥ 2.25 mg/mL (4.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 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 (22.5 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 (276 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]. Egile C, et al. The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer [J]. Molecular cancer therapeutics, 2015, 14(2): 384-394. [Content Brief]

[2]. Angevin E, et al. A first-in-human phase I study of SAR125844, a selective MET tyrosine kinase inhibitor, in patients with advanced solid tumours with MET amplification [J]. European Journal of Cancer, 2017, 87: 131-139. [Content Brief]

[3]. Ugolini A, et al. Discovery and pharmacokinetic and pharmacological properties of the potent and selective MET kinase inhibitor 1-{6-[6-(4-fluorophenyl)-[1, 2, 4] triazolo [4, 3-b] pyridazin-3-ylsulfanyl] benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl) urea (SAR125844) [J]. 2016. [Content Brief]

[4]. Egile C, et al. The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer. Mol Cancer Ther. 2015 Feb;14(2):384-94. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8161 mL	9.0805 mL	18.1610 mL	45.4025 mL
	5 mM	0.3632 mL	1.8161 mL	3.6322 mL	9.0805 mL
	10 mM	0.1816 mL	0.9081 mL	1.8161 mL	4.5403 mL
	15 mM	0.1211 mL	0.6054 mL	1.2107 mL	3.0268 mL
	20 mM	0.0908 mL	0.4540 mL	0.9081 mL	2.2701 mL
	25 mM	0.0726 mL	0.3632 mL	0.7264 mL	1.8161 mL
	30 mM	0.0605 mL	0.3027 mL	0.6054 mL	1.5134 mL
	40 mM	0.0454 mL	0.2270 mL	0.4540 mL	1.1351 mL
	50 mM	0.0363 mL	0.1816 mL	0.3632 mL	0.9081 mL
	60 mM	0.0303 mL	0.1513 mL	0.3027 mL	0.7567 mL
	80 mM	0.0227 mL	0.1135 mL	0.2270 mL	0.5675 mL

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SAR125844

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Alle PI3K Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Alle MEK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SAR125844 Related Classifications

HY-16446 Related Classifications