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SAR125884 hydrochlorid (1116743-46-4(free base))

Catalog No. T5677 CAS T5677

SAR125844 is a potent and selective MET kinase inhibitor with a favorable preclinical toxicity profile,(IC50=4.2 nM).

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SAR125884 hydrochlorid (1116743-46-4(free base)) Chemical Structure

SAR125884 hydrochlorid (1116743-46-4(free base)), CAS T5677

Pack Size	Availability	Price/USD
1 mg	In stock	$ 53.00
5 mg	In stock	$ 92.00
10 mg	In stock	$ 153.00
25 mg	In stock	$ 331.00
50 mg	In stock	$ 488.00
100 mg	In stock	$ 693.00
200 mg	In stock	$ 995.00
1 mL * 10 mM (in DMSO)	In stock	$ 171.00

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Purity: 95%

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Description	SAR125844 is a potent and selective MET kinase inhibitor with a favorable preclinical toxicity profile,(IC50=4.2 nM).
Targets&IC50	MET RTK:4.2 nM
In vitro	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 software and a 4-parameter logistic model[1].
In vivo	SAR125844 inhibited autophosphorylation of AXL and cell proliferation of TPM–NTRK1-overexpressing KM12 cell line with IC50 values of 110 and 1,400 nmol/L, respectively, indicating a 30- and 500-fold selectivity index for AXL and NTRK1 in cell-based assays. The selectivity profile of SAR125844 was further confirmed in cell lines with a single-digit nanomolar antiproliferative activity in MET-addicted cell lines and a complete lack of impact in cells not addicted to the MET pathway. This is in contrast to ARQ197 that has equal antiproliferative activity on MET-addicted and MET-independent tumor cell lines[1].
Animal Research	The antitumor activity of SAR125844 was investigated after administration of SAR125844 solution daily in SNU-5 bearing mice at 10, 20, and 45 mg/kg and every 2 days in Hs 746T tumor–bearing mice (at 5, 10, 20, and 45 mg/kg for SAR125844 solution and at 5, 11, 21, 53, 106, and 213 mg/kg for SAR125844 nanosuspension). Tumor volumes (in mm^3, based on the following formula, volume = length (mm) × width2 (mm2)/2), were measured twice weekly and body weight recorded every day. Endpoints collected were complete regressions (CR, regression below the palpable limit), partial regressions (PR, regression of 50% of the initial tumor volume), and the percentage of tumor regression (% of volume decrease posttreatment compared with pretreatment). Statistical significance was determined by a Dunnett test versus vehicle after a two-way ANOVA with repeated measures performed separately on ranks of changes from baseline with P < 0.05 considered significant[1].

Molecular Weight	587
Formula	C25H23FN8O2S2.HCl
CAS No.	T5677

Storage

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

Solubility Information

DMSO: 55 mg/mL (93.7 mM)

References and Literature

1. 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. 2. Ugolini A , Kenigsberg M , Rak A , et al. Discovery, pharmacokinetic and pharmacological properties of the potent and selective MET kinase inhibitor, 1-{6-[6-(4-Fluoro-phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]-benzothiazol-2-yl-3-(2-morpholin-4-yl-ethyl)-urea (SAR125844)[J]. Journal of Medicinal Chemistry, 2016:acs.jmedchem.6b00280.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Inhibitor Library Bioactive Compounds Library Max Anti-Liver Cancer Compound Library Anti-Colorectal Cancer Compound Library Anti-Lung Cancer Compound Library NO PAINS Compound Library Cytokine Inhibitor Library Anti-Cancer Compound Library

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Keywords

SAR125884 hydrochlorid (1116743-46-4(free base)) T5677 Tyrosine Kinase/Adaptors c-Met/HGFR SAR-125884 hydrochlorid (1116743-46-4(free base)) SAR125884 hydrochlorid (1116743464(free base)) SAR125884 hydrochlorid (1116743 46 4(free base)) inhibitor inhibit

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