Rigosertib

TargetMol
Product Code: TAR-T16750
Supplier: TargetMol
CodeSizePrice
TAR-T16750-50mg50mgEnquire
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TAR-T16750-2mg2mg£98.00
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TAR-T16750-5mg5mg£115.00
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TAR-T16750-1mL1 mL * 10 mM (in DMSO)£128.00
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TAR-T16750-10mg10mg£148.00
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition of the PI3 kinase/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in the cell cycle.
CAS:
592542-59-1
Formula:
C21H25NO8S
Molecular Weight:
451.49
Pathway:
Angiogenesis; Cell Cycle/Checkpoint; Apoptosis; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors; Cytoskeletal Signaling
Purity:
0.9733
SMILES:
COc1cc(OC)c(C=CS(=O)(=O)Cc2ccc(OC)c(NCC(O)=O)c2)c(OC)c1
Target:
Apoptosis; FLT; PLK; PI3K; Bcr-Abl; CDK; PDGFR; Src

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. 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. 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. 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. 2011 Sep 22;54(18):6254-76. 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