(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:

Rigosertib sodium

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