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Rigosertib sodium

Cat. No. M2211
Rigosertib sodium Structure
Synonym:

ON-01910 sodium; CAS# 592542-60-4

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 66  USD66 In stock
10mg USD 110  USD110 In stock
25mg USD 200  USD200 In stock
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Quality Control & Documentation
Biological Activity

Rigosertib sodium (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.

Chemical Information
Molecular Weight 473.47
Formula C21H24NNaO8S
CAS Number 1225497-78-8
Solubility (25°C) DMSO 90 mg/mL
Water 50 mg/mL
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Chapman CM, et al. Clin Cancer Res. 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.

[2] Ma WW, et al. Clin Cancer Res. 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.

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Keywords: Rigosertib sodium, ON-01910 sodium; CAS# 592542-60-4 supplier, PLK, inhibitors, activators


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