2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR MAPK/ERK Pathway Apoptosis
  3. c-Met/HGFR PI3K Akt MEK Apoptosis
  4. SAR125844

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

For research use only. We do not sell to patients.

SAR125844 Chemical Structure

SAR125844 Chemical Structure

CAS No. : 1116743-46-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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Description

SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer[1][2][3].

IC50 & Target

c-Met

 

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.

SAR125844 Related Antibodies

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
Molecular Weight

550.63

Formula

C25H23FN8O2S2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8161 mL 9.0805 mL 18.1610 mL
5 mM 0.3632 mL 1.8161 mL 3.6322 mL
View the 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, 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.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

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.

  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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, 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SAR1258441116743-46-4SAR 125844SAR-125844c-Met/HGFRPI3KAktMEKApoptosisPhosphoinositide 3-kinasePKBProtein kinase BMitogen-activated protein kinase kinaseMAPKKMAP2KcancerH-460HCT116H1993EBC-1SNU-5OE33Hs 746TMKN-45PC-3SNU-5 and Hs 746T tumor-bearing miceInhibitorinhibitorinhibit

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