Rigosertib sodium
- Product Name
- Rigosertib sodium
- CAS No.
- 592542-60-4
- Chemical Name
- Rigosertib sodium
- Synonyms
- Novonex;ON 01910 Na;ON 01910 sodium;RIGOSERTIB SODIUM;Rigosertib sodium(E);Rigosertib sodium, 10 mM in DMSO;RIGOSERTIB SODIUM (ON-01910 SODIUM);Rigosertib sodium - ON01910 sodium | Estybon;ON-01910 SODIUM;ON01910 SODIUM;ON01910 SODIUM;(E)-2,4,6-Trimethoxystyryl 3-[(carboxymethyl)amino]-4-methoxybenzyl sulfone sodium salt
- CBNumber
- CB62627915
- Molecular Formula
- C21H24NNaO8S
- Formula Weight
- 473.47193
- MOL File
- 592542-60-4.mol
Rigosertib sodium Property
- Melting point:
- 174-178℃
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
- color
- White to yellow
- InChI
- 1S/C21H25NO8S.Na/c1-27-15-10-19(29-3)16(20(11-15)30-4)7-8-31(25,26)13-14-5-6-18(28-2)17(9-14)22-12-21(23)24;/h5-11,22H,12-13H2,1-4H3,(H,23,24);/q;+1/p-1/b8-7+;
- InChIKey
- VLQLUZFVFXYXQE-USRGLUTNSA-M
- SMILES
- [Na+].[S](=O)(=O)(Cc2cc(c(cc2)OC)NCC(=O)[O-])\C=C\c1c(cc(cc1OC)OC)OC
Safety
- WGK Germany
- WGK 3
- Storage Class
- 11 - Combustible Solids
N-Bromosuccinimide Price
- Product number
- 5.33575
- Product name
- Rigosertib - CAS 592542-60-4 - Calbiochem
- Packaging
- 10MG
- Price
- $239
- Updated
- 2026/03/19
- Product number
- BR175409
- Product name
- Rigosertib sodium
- Packaging
- 50mg
- Price
- $290
- Updated
- 2021/12/16
- Product number
- CS-0189
- Product name
- Rigosertibsodium
- Purity
- 99.49%
- Packaging
- 50mg
- Price
- $290
- Updated
- 2021/12/16
- Product number
- orb611845
- Product name
- Rigosertib sodium
- Packaging
- 10mg
- Price
- $345.1
- Updated
- 2021/12/16
- Product number
- Axon2950
- Product name
- Rigosertibsodium-ON01910sodium|Estybon
- Purity
- 99%
- Packaging
- 25mg
- Price
- $357.5
- Updated
- 2021/12/16
Rigosertib sodium Chemical Properties,Usage,Production
Uses
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle[1][2]. Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM[3].
Definition
ChEBI: Rigosertib sodium is the sodium salt of rigosertib. It is an anti-cancer agent which has been granted Orphan Drug Designation by the FDA for use in patients with myelodysplastic syndromes (MDS). It has a role as a microtubule-destabilising agent, an antineoplastic agent, an EC 2.7.11.21 (polo kinase) inhibitor and an apoptosis inducer. It contains a rigosertib(1-).
Biological Activity
Cell permeable: yes', 'Primary Target
PI 3-K/Akt/mTOR signaling', 'Target IC50: 32, 42, 182, 18 and 155 nM against Bcr-Abl, Flt1, Fyn, PDGFR, and Src, respectively
in vivo
Rigosertib (250 mg/kg, i.p.) markedly inhibits tumor growth in mouse xenograft models of Bel-7402, MCF-7, and MIA-PaCa cells[3]. Rigosertib (200 mg/kg, i.p.) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells[4].
IC 50
PLK1: 9 nM (IC50); PLK2: 260 nM (IC50); PDGFR: 18 nM (IC50); Src: 155 nM (IC50); BCR-ABL: 32 nM (IC50); Cdk1: 260 nM (IC50); Flt1: 42 nM (IC50); Fyn: 182 nM (IC50)
References
[1] Xu F, et al. Rigosertib as a selective anti-tumor agent can ameliorate multiple dysregulated signalingtransduction pathways in high-grade myelodysplastic syndrome. Sci Rep. 2014 Dec 4;4:7310. DOI:10.1038/srep07310
[2] Hyoda T, et al. Rigosertib induces cell death of a myelodysplastic syndrome-derived cell line by DNA damage-induced G2/M arrest. Cancer Sci. 2015 Mar;106(3):287-93. DOI:10.1111/cas.12605
[3] Gumireddy K, et al. ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent. Cancer Cell. 2005 Mar;7(3):275-86. DOI:10.1016/j.ccr.2005.02.009
[4] Reddy MV, 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. J Med Chem. DOI:10.1021/jm200570p
[5] Chapman CM, et al. ON 01910.Na is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Clin Cancer Res. 2012 Apr 1;18(7):1979-91 DOI:10.1158/1078-0432.CCR-11-2113
Rigosertib sodium Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Rigosertib sodium manufacturers
- Product
- Glycine, N-[2-Methoxy-5-[[[(1E)-2-(2,4,6-triMethoxyphenyl)ethenyl]sulfonyl]Methyl]phenyl]-, sodiuM Slat 592542-60-4
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 85.0-99.8%
- Supply Ability
- 20 tons
- Release date
- 2020-11-09