SAR125844
- Product Name
- SAR125844
- CAS No.
- 1116743-46-4
- Chemical Name
- SAR125844
- Synonyms
- SAR125884;SAR125844;SAR125844 /SAR-125844;SAR125844, 10 mM in DMSO;SAR125844; SAR 125844; SAR-125844;SAR125884 hydrochlorid (1116743-46-4(free base));Inhibitor,SAR125844,c-Met/HGFR,inhibit,SAR 125844,SAR-125844,Apoptosis;1-(6-((6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)thio)benzo[d]thiazol-2-yl)-3-(2-morpholinoethyl)urea;Urea, N-[6-[[6-(4-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]-2-benzothiazolyl]-N'-[2-(4-morpholinyl)ethyl]-;1-[6-[[6-(4-Fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl]-1,3-benzothiazol-2-yl]-3-[2-(morpholin-4-yl)ethyl]urea
- CBNumber
- CB22668390
- Molecular Formula
- C25H23FN8O2S2
- Formula Weight
- 550.63
- MOL File
- 1116743-46-4.mol
SAR125844 Property
- storage temp.
- Store at -20°C
- solubility
- DMSO : 45 mg/mL (81.72 mM)
- form
- Solid
- color
- Light yellow to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0006341
- Product name
- SAR125844
- Purity
- 99.03%
- Packaging
- 5mg
- Price
- $120
- Updated
- 2021/12/16
- Product number
- CS-0006341
- Product name
- SAR125844
- Purity
- 99.03%
- Packaging
- 10mg
- Price
- $190
- Updated
- 2021/12/16
- Product number
- CS-0006341
- Product name
- SAR125844
- Purity
- 99.03%
- Packaging
- 50mg
- Price
- $750
- Updated
- 2021/12/16
- Product number
- orb573075
- Product name
- SAR125844
- Purity
- >98%
- Packaging
- 100mg
- Price
- $1208.7
- Updated
- 2021/12/16
- Product number
- CS-0006341
- Product name
- SAR125844
- Purity
- 99.03%
- Packaging
- 100mg
- Price
- $1300
- Updated
- 2021/12/16
SAR125844 Chemical Properties,Usage,Production
Uses
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].
Biological Activity
SAR125844 is a potent and highly selective Met (c-Met) kinase inhibitor with nanomolar activity against wild-type Met (c-Met) kinase (IC50=4.2 nM), against H1094Y, Y1235D, M1250T, The IC50s of the L1195V and D1228H mutants were 0.22, 1.7, 6.5, 65 and 81 nM, respectively.
in vitro
SAR125844 is an ATP-competitive and reversible inhibitor. SAR125844 has moderate activity against RON, a homolog that is structurally similar to MET, and SAR125844 inhibits RON with an IC50 of approximately 740 nM. SAR125844 is more than 100-fold more selective for MET kinase than for RON.
in vivo
In a pharmacokinetic study in mice, the oral bioavailability of SAR125844 was low, approximately 2%. Its Caco-2 permeability is moderate. In female SCID mice bearing xenograft tumors (inoculated with the MET-expanded Hs 746T human gastric tumor cell line), a single intravenous injection of 20 mg/kg of SAR125844 resulted in a plasma exposure of 6190 h ng/kg mL, clearance CL = 3.1 L/h/kg, large volume of distribution (Vss = 4.2 L/kg).
IC 50
c-Met
References
[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. DOI:10.1158/1535-7163.MCT-14-0428
[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. DOI:10.1016/j.ejca.2017.10.016
[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. DOI:10.1021/acs.jmedchem.6b00280
[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. DOI:10.1158/1535-7163.MCT-14-0428
SAR125844 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from SAR125844 manufacturers
- Product
- SAR125844 1116743-46-4
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 95%~99%
- Supply Ability
- per week 100kg
- Release date
- 2019-09-05