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SAR125844

Catalog No. T5467 CAS 1116743-46-4

Synonyms: SAR125884

SAR125844, a potent and highly selective inhibitor of the MET receptor tyrosine kinase (RTK), for intravenous administration. (IC50 value of 4.2 nmol/L)

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SAR125844, CAS 1116743-46-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 118.00
25 mg	In stock	$ 239.00
50 mg	In stock	$ 383.00
100 mg	In stock	$ 622.00
1 mL * 10 mM (in DMSO)	In stock	$ 88.00

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Purity: 98.39%

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Description	SAR125844, a potent and highly selective inhibitor of the MET receptor tyrosine kinase (RTK), for intravenous administration. (IC50 value of 4.2 nmol/L)
Targets&IC50	MET RTK:4.2 nM
In vitro	SAR125844 inhibits MET autophosphorylation in cell-based assays in the nanomolar range, and promotes low nanomolar proapoptotic and antiproliferative activities selectively in cell lines with MET gene amplification or pathway addiction.
Kinase Assay	SAR125844 was preincubated at room temperature with each enzyme for 30 minutes in a buffer containing 10 mmol/L MOPS-NaOH pH 7.0, 0.01% Tween 20, and 1 mmol/L dithiothreitol. The enzymatic reactions were initiated by the addition of a mix of 1 ng/μL of a biotinylated poly(glutamate-alanine-tyrosine) peptide ATP and MgCl2. After 5-minute incubation at room temperature, the reactions were stopped by the addition of anti-phosphotyrosine monoclonal antibody (mAb) PT-66 -Europium cryptate and streptavidin 61SAXLB. After two hours at room temperature, the emission signals at 620 and 665 nm were recorded with a GENios reader, with an excitation wavelength of 320 nm. The percentage of inhibition versus nontreated sample was estimated using the emission ratios at 665/620 nm.
Cell Research	MKN-45, Hs 746T, and SNU-5 cells were seeded in poly d-lysine 96-well plates in complete medium.?Plates were incubated with increasing SAR125844 concentrations for 1 hour, cell lysates were generated using standard procedures and pMETY1230/1234/1235 level evaluated.?IC50 values were calculated using the Biost@t-SPEED internal software and a 4-parameter logistic model
Animal Research	Long duration of MET kinase inhibition up to 7 days was achieved with a nanosuspension formulation of SAR125844.?Daily or every-2-days intravenous treatment of SAR125844 promoted a dose-dependent tumor regression in MET-amplified human gastric cancer models at tolerated doses without treatment-related body weight loss.

Synonyms	SAR125884
Molecular Weight	550.63
Formula	C25H23FN8O2S2
CAS No.	1116743-46-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (81.72 mM)

References and Literature

1. 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.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library ReFRAME Related Library Anti-Colorectal Cancer Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SAR125844 1116743-46-4 Apoptosis Tyrosine Kinase/Adaptors c-Met/HGFR Inhibitor SAR-125844 SAR-125884 inhibit SAR125884 SAR 125884 SAR 125844 inhibitor

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