ChemicalBook > CAS DataBase List > (2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALT

(2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALT

Product Name
(2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALT
CAS No.
592542-59-1
Chemical Name
(2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALT
Synonyms
CS-1407;Rigosertib;Rigosertib(acid);rigosertib(PI3K/Plk1 inhibitor)ORPHAN DRUG;3: PN: WO2006074149 PAGE: 45 claiMed sequence;(E)-2-((2-Methoxy-5-(((2,4,6-triMethoxystyryl)sulfonyl)Methyl)phenyl)aMino)acetic acid;N-[2-Methoxy-5-[[[(1E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]glycine;Glycine, N-[2-Methoxy-5-[[[(1E)-2-(2,4,6-triMethoxyphenyl)ethenyl]sulfonyl]Methyl]phenyl]-;(2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALT;PI3K,Polo-like Kinase (PLK),Rigosertib,Phosphoinositide 3-kinase,Apoptosis,ON 01910,Inhibitor,inhibit,ON01910
CBNumber
CB92457038
Molecular Formula
C21H25NO8S
Formula Weight
451.49
MOL File
592542-59-1.mol
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(2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALT Property

Melting point:
172-174 °C(Solv: acetone (67-64-1))
Boiling point:
756.1±60.0 °C(Predicted)
Density 
1.332±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C,unstable in solution, ready to use.
solubility 
Soluble in DMSO
form 
Powder
pka
4.23±0.20(Predicted)
color 
White to light yellow
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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.

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N-Bromosuccinimide Price

TRC
Product number
R590713
Product name
Rigosertib
Packaging
50mg
Price
$685
Updated
2021/12/16
Biorbyt Ltd
Product number
orb181113
Product name
Rigosertib
Purity
>98%
Packaging
100mg
Price
$765
Updated
2021/12/16
ChemScene
Product number
CS-1710
Product name
Rigosertib
Purity
98.81%
Packaging
100mg
Price
$900
Updated
2021/12/16
ApexBio Technology
Product number
B1288
Product name
Rigosertib
Packaging
50mg
Price
$900
Updated
2021/12/16
Activate Scientific
Product number
AS59462
Product name
Rigosertib
Purity
95+%
Packaging
1g
Price
$903
Updated
2021/12/16
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(2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALT Chemical Properties,Usage,Production

Uses

Rigosertib is a microtubule destabilizing agent which may be employed in the treatment of high-?risk myelodysplastic syndrome.

Definition

ChEBI: Rigosertib is an N-[2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine in which the double bond has E-configuration. It is a non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM and exhibits anti-cancer properties. It has a role as a microtubule-destabilising agent, an EC 2.7.11.21 (polo kinase) inhibitor, an apoptosis inducer and an antineoplastic agent. It is a conjugate acid of a rigosertib(1-).

Biological Activity

rigosertib is a dual inhibitor of phosphoinositide 3-kinase (pi3k) and polo-like kinase 1 (plk1) [1].

in vitro

studies show that rigosertib inhibits the pi3k/akt pathway, down-regulates cyclin d1, induces noxa and bim and activates the jnk pathway in human leukemic cells. rigosertib induces apoptosis of a variety of human tumor cell lines including breast, prostate, ovarian, pancreatic, sclc, colorectal, melanoma and et al. for instant, it shows anti-tumor efficacy in bt20, mcf-7, bt474, ov-car-3, a549 and hct-116 with ic50 values of 80nm, 75nm, 50nm, 75nm, 90nm and 75nm, respectively. in addition, rigosertib is also effective against the drug resistant tumor cell lines. it potently inhibits tumor growth with ic50 values of 100nm and 50nm against mes-sa/dx5 and cem/c2, respectively. moreover, it is reported that rigosertib can affect the cell cycle of both normal cells and tumor cells. rigosertib leads to a blockade of cell cycle progression in the g1 and g2/m phases in normal diploid human fetal lung cells. when treated with du145 cells, rigosertib induces cell cycle arrest in g2/m phase [2].

References

[1] anderson r t, keysar s b, bowles d w, et al. the dual pathway inhibitor rigosertib is effective in direct patient tumor xenografts of head and neck squamous cell carcinomas. molecular cancer therapeutics, 2013, 12(10): 1994-2005.
[2] reddy m v r, venkatapuram p, mallireddigari m r, et al. discovery of a clinical stage multi-kinase inhibitor sodium (e)-2-{2-methoxy-5-[(2′, 4′, 6′-trimethoxystyrylsulfonyl) methyl] phenylamino} acetate (on 01910. na): synthesis, structure–activity relationship, and biological activity. journal of medicinal chemistry, 2011, 54(18): 6254-6276.

(2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALT Preparation Products And Raw materials

Raw materials

Preparation Products

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(2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALT Suppliers

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592542-59-1, (2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALTRelated Search:


  • CS-1407
  • Rigosertib(acid)
  • (2-METHOXY-5-[2-(2,4,6-TRIMETHOXY-PHENYL)-ETHENESULFONYLMETHYL]-PHENYLAMINO)-ACETIC ACID, SODIUM SALT
  • Glycine, N-[2-Methoxy-5-[[[(1E)-2-(2,4,6-triMethoxyphenyl)ethenyl]sulfonyl]Methyl]phenyl]-
  • (E)-2-((2-Methoxy-5-(((2,4,6-triMethoxystyryl)sulfonyl)Methyl)phenyl)aMino)acetic acid
  • 3: PN: WO2006074149 PAGE: 45 claiMed sequence
  • Rigosertib
  • N-[2-Methoxy-5-[[[(1E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]phenyl]glycine
  • rigosertib(PI3K/Plk1 inhibitor)ORPHAN DRUG
  • PI3K,Polo-like Kinase (PLK),Rigosertib,Phosphoinositide 3-kinase,Apoptosis,ON 01910,Inhibitor,inhibit,ON01910
  • 592542-59-1
  • C21H24NNaO8S
  • C21H25NO8S
  • Antineoplastic protein Kinase inhibitors
  • APIS