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Rigosertib sodium

HY-12037

(ON-01910 sodium; ON01910 sodium; ON01910 sodium)

Rigosertib sodium

Rigosertib sodium Chemical Structure

Rigosertib sodium (ON-01910 sodium) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM. It shows 30-fold greater selectivity against PLK2 and no activity to PLK3.

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10 mM * 1 mL in DMSO $77 In-stock
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Free sample   Apply now  
10 mM * 1 mL in DMSO €75 In-stock
5 mg €69 In-stock
10 mg €118 In-stock
50 mg €441 In-stock
100 mg €735 In-stock
200 mg Get quote
500 mg Get quote

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Product name: Rigosertib sodium
Cat. No.: HY-12037

Rigosertib sodium Data Sheet

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    Purity: 99.49%

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Biological Activity of Rigosertib sodium

Rigosertib sodium (ON-01910 sodium) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM. It shows 30-fold greater selectivity against PLK2 and no activity to PLK3.
IC50 Value: 9 nM [1]
Target: PLK1
in vitro: ON 01910.Na induced apoptosis in CLL B cells without significant toxicity against T cells or normal B cells. ON 01910.Na was equally active against leukemic cells associated with a more aggressive disease course [immunoglobulin heavy-chain variable region unmutated, adverse cytogenetics] than against cells without these features. Gene expression profiling revealed two main mechanisms of action: PI3K/AKT inhibition and induction of ROS that resulted in an oxidative stress response through activating protein 1 (AP-1), c-jun-NH(2)-terminal kinase, and ATF3 culminating in the upregulation of NOXA. ROS scavengers and shRNA mediated knockdown of ATF3- and NOXA-protected cells from drug-induced apoptosis [2]. ON 01910.Na caused hyperphosphorylation of RanGAP1·SUMO1 within 4 hours that was sustained for more than 24 hours. ON 01910.Na neither induces DNA damage directly nor acts as a tubulin toxin [3].
in vivo: ON 01910.Na were assessed after administration (10-150 mg/kg, IP or IV) to several species (mouse, rat, and dog). Plasma protein binding was assessed using ultrafiltration. Patients had solid tumors refractory to standard therapy [4]. ON 01910.Na was administered as a 2-hour infusion on days 1, 4, 8, 11, 15, and 18 in 28-day cycles. The starting dose was 80 mg, and an accelerated titration schedule (single-patient cohorts) was used for escalation. Pharmacokinetics was studied on days 1 and 15 of cycle 1 [5].
Toxicity: Mean absolute oral bioavailability ranged from 13·9% (fed) to 34·8% (fasting) in 12 patients treated at the 560 mg b.i.d. dose level. Dose-limiting toxicity (grade 3 dysuria and shortness of breath) occurred at the 700 mg b.i.d. dose. Five patients experienced grade 3 non-haematological toxicity, including symptoms of urothelial inflammation, hypotension and syncope, fatigue and abdominal pain [6].
 

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 473.47 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C21H24NNaO8S
CAS No 592542-60-4
Solvent & Solubility

DMSO ≥92mg/mL Water ≥92mg/mL Ethanol <1.2mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.1121 mL 10.5603 mL 21.1207 mL
5 mM 0.4224 mL 2.1121 mL 4.2241 mL
10 mM 0.2112 mL 1.0560 mL 2.1121 mL

Clinical Information of Rigosertib sodium

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
Rigosertib sodium Onconova Therapeutics Inc Myelodysplastic syndrome 31-AUG-13 31-DEC-15 Safety; Efficacy; Pharmacokinetics
Onconova Therapeutics Inc Metastatic pancreas cancer 31-MAY-11 31-DEC-14 Safety; Efficacy; Pharmacokinetics; Pharmacodynamics
Onconova Therapeutics Inc Myelodysplastic syndrome 30-NOV-10 31-DEC-13 Safety; Efficacy
Stanford University Myelodysplastic syndrome 31-MAY-09 28-FEB-11 Safety; Efficacy
Onconova Therapeutics Inc Myelodysplastic syndrome 31-JUL-13 30-JUN-15 Safety; Efficacy

References on Rigosertib sodium

Other Forms

Inhibitor Kit

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