Free shipping on all orders over $ 500

Rigosertib

Cat. No. M2211
Rigosertib Structure
Synonym:

ON-01910

Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 550 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Rigosertib (ON-01910 sodium salt) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM. Rigosertib (ON-01910) inhibited polo-like kinase1 (Plk1), induced apoptosis in CLL B cells without significant toxicity against T cells or normal B cells. Rigosertib also inhibits several multidrug resistant tumor cell lines, including MES-SA, MES-SA/DX5a, CEM, and CEM/C2a, with IC50 of 50-100 nM. Rigosertib also abrogates the pro-survival effect of follicular dendritic cells on CLL cells and reduces SDF-1-induced migration of leukemic cells. Rigosertib (200 mg/kg) shows inhibition on tumor growth in a mouse xengraft model of BT20 cells in vivo.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 473.47
Formula C21H24NNaO8S
CAS Number 1225497-78-8
Purity >99%
Solubility DMSO 80 mg/mL
Water 80 mg/mL
Storage at -20°C
References

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.
Chapman CM, et al. Clin Cancer Res. 2012 Apr 1;18(7):1979-91. PMID: 22351695.

Phase I study of Rigosertib, an inhibitor of the phosphatidylinositol 3-kinase and Polo-like kinase 1 pathways, combined with gemcitabine in patients with solid tumors and pancreatic cancer.
Ma WW, et al. Clin Cancer Res. 2012 Apr 1;18(7):2048-55. PMID: 22338014.

Related PLK Products
HMN-214

HMN-214 is a procompound of HMN-176, which alters the cellular spatial orientation of Plk1.

TAK-960

TAK-960 is a novel, potent and selective Plk1 inhibitor with IC50 of 8 nM.

Ro3280

RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.

MLN0905

MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.

GW843682X

GW 843682X is a PLK inhibitor for PLK1 and PLK3 with IC50 of 2.2 nM and 9.1 nM, respectively.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Rigosertib, ON-01910 supplier, PLK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.