ChemicalBook > CAS DataBase List > SAR 131675

SAR 131675

Product Name
SAR 131675
CAS No.
1433953-83-3
Chemical Name
SAR 131675
Synonyms
CS-994;SAR 131675 USP/EP/BP;SAR131675(1433953-83-3);SAR131675, 10 mM in DMSO;(R)-2-amino-1-ethyl-7-(3-hydroxy-4-methoxy-3-methylbut-1-ynyl)-N-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide;(R)-2-Amino-1-ethyl-7-(3-hydroxy-4-methoxy-3-methylbut-1-yn-1-yl)-N-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide;1,8-Naphthyridine-3-carboxamide, 2-amino-1-ethyl-1,4-dihydro-7-[(3R)-3-hydroxy-4-methoxy-3-methyl-1-butyn-1-yl]-N-methyl-4-oxo-
CBNumber
CB92666683
Molecular Formula
C18H22N4O4
Formula Weight
358.39
MOL File
1433953-83-3.mol
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SAR 131675 Property

Boiling point:
592.2±50.0 °C(Predicted)
Density 
1.33±0.1 g/cm3(Predicted)
storage temp. 
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
solubility 
insoluble in DMSO; insoluble in EtOH; insoluble in H2O
form 
solid
pka
12.20±0.29(Predicted)
color 
White to yellow
InChI
InChI=1S/C18H22N4O4/c1-5-22-15(19)13(17(24)20-3)14(23)12-7-6-11(21-16(12)22)8-9-18(2,25)10-26-4/h6-7,25H,5,10,19H2,1-4H3,(H,20,24)/t18-/m1/s1
InChIKey
PFMPOBVAYMTUOX-GOSISDBHSA-N
SMILES
N1(CC)C2C(=CC=C(C#C[C@](O)(C)COC)N=2)C(=O)C(C(NC)=O)=C1N
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
28385
Product name
SAR131675
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
28385
Product name
SAR131675
Packaging
25mg
Price
$343
Updated
2024/03/01
Cayman Chemical
Product number
28385
Product name
SAR131675
Packaging
5mg
Price
$122
Updated
2024/03/01
Cayman Chemical
Product number
28385
Product name
SAR131675
Packaging
10mg
Price
$169
Updated
2024/03/01
ApexBio Technology
Product number
B2301
Product name
SAR131675
Packaging
10mg
Price
$50
Updated
2021/12/16
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SAR 131675 Chemical Properties,Usage,Production

Characteristics

SAR131675 is a potent and selective VEGFR-3 tyrosine kinase inhibitor

Biological Activity

sar131675 is a selective inhibitor of vegfr-3 with ic50 value of 20nm [1].sar131675 is an atp-competitive inhibitor. it inhibits recombinant human vegfr-3 with ic50 value of 23nm and inhibits the kinase activity of vegfr-3 with ki value of 12nm. sar131675 is found to be cell permeable and inhibits vegfr-3 autophosphorylation in hek cells with ic50 values ranging from 30nm to 50nm. sar131675 shows ic50 values of >3μm and 235nm against vegfr-1 and vegfr-2, respectively. it also havs no inhibitory effect on a panel of 65 kinases, 107 nonkinase enzymes and receptors and on 21 ion channels. moreover, sar131675 inhibits lymphatic cell survival induced by vegfc and vegfd with ic50 values of 14nm and 17nm. on another hand, sar131675 exerts inhibition of the migration induced by vegfa or vegfc with ic50 values of 100nm and <30nm in hlmvec cells, respectively [1]..

in vitro

SAR131675 inhibits the proliferation of primary human lymph node cells induced by VEGFR-3 ligands VEGFC and VEGFD in a dose-dependent manner with IC50 of approximately 20 nM, and also inhibits the activity of rh-VEGFR-3–TK in a dose-dependent manner characteristic, IC50 of 23 nM. SAR131675 inhibits VEGFR-1–TK activity with IC50 greater than 3 μM and inhibits VEGFR-2–TK activity with IC50 of 235 nM.

in vivo

sar131675 abrogates lymphangiogenesis and angiogenesis induced by fgf2. it also shows antitumor activity in the mice models. treatment with sar131675 significantly reduces the tumor volume of 4t1 mammary carcinoma tumors [1]

target

VEGFR3

References

[1] alam a, blanc i, gueguen-dorbes g, et al. sar131675, a potent and selective vegfr-3–tk inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities. molecular cancer therapeutics, 2012, 11(8): 1637-1649.

SAR 131675 Preparation Products And Raw materials

Raw materials

Preparation Products

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1433953-83-3, SAR 131675Related Search:


  • CS-994
  • (R)-2-amino-1-ethyl-7-(3-hydroxy-4-methoxy-3-methylbut-1-ynyl)-N-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide
  • 1,8-Naphthyridine-3-carboxamide, 2-amino-1-ethyl-1,4-dihydro-7-[(3R)-3-hydroxy-4-methoxy-3-methyl-1-butyn-1-yl]-N-methyl-4-oxo-
  • SAR 131675 USP/EP/BP
  • (R)-2-Amino-1-ethyl-7-(3-hydroxy-4-methoxy-3-methylbut-1-yn-1-yl)-N-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide
  • SAR131675, 10 mM in DMSO
  • SAR131675(1433953-83-3)
  • 1433953-83-3
  • Inhibitors
  • API