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533575 Rigosertib - CAS 592542-60-4 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
592542-60-4C₂₁H₂₄NNaO₈S

Products

Catalog NumberPackaging Qty/Pack
5.33575.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable, nontoxic benzylstyrylsulfone based compound with anti-tumor and radiosensitizing properties. Potently suppresses PI 3-K/Akt/mTOR signaling pathway and activates Cdc25C phosphatases. Acts as an allosteric, substrate-competitive, and reversible inhibitor of multiple protein kinases (IC50 = 32, 42, 182, 18 and 155 nM against Bcr-Abl, Flt1, Fyn, PDGFR, and Src, respectively). Induces DNA damage and blocks microtubule formation. Also shown to cause mitotic arrest and apoptosis in multiple types of cancer cells (GI50 = 30-200 nM) and blocks cell cycle at G2/M phase. Effective against several multi-drug resistance tumor cells (IC50 = 50-100 nM). Suppresses the growth of BT20 tumor xenografts in mice and improves their survival rate (200 mg/kg, i.v. Q2D X 20 schedule). However, it displays limited oral bioavailability.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number533575
Brand Family Calbiochem®
SynonymsSodium (E)-2-(2-methoxy-5-((2,4,6-trimethoxystyrylsulfonyl)methyl)phenylamino)acetate, ON01910, Na, Estybon
References
ReferencesLu, T., et al. 2015. Mol. Pharmacol. 87, 18.
Ramana Reddy, M.V., et al. 2011. J. Med. Chem. 54, 6254.
Gumireddy, K., et al. 2005. Cancer Cell 7, 275.
Product Information
CAS number592542-60-4
FormOff-white solid
Hill FormulaC₂₁H₂₄NNaO₈S
Chemical formulaC₂₁H₂₄NNaO₈S
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetPI 3-K/Akt/mTOR signaling
Primary Target IC<sub>50</sub>32, 42, 182, 18 and 155 nM against Bcr-Abl, Flt1, Fyn, PDGFR, and Src, respectively
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.33575.0001 04055977287028

Documentation

Rigosertib - CAS 592542-60-4 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Lu, T., et al. 2015. Mol. Pharmacol. 87, 18.
Ramana Reddy, M.V., et al. 2011. J. Med. Chem. 54, 6254.
Gumireddy, K., et al. 2005. Cancer Cell 7, 275.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision20-November-2015 JSW
SynonymsSodium (E)-2-(2-methoxy-5-((2,4,6-trimethoxystyrylsulfonyl)methyl)phenylamino)acetate, ON01910, Na, Estybon
DescriptionA cell-permeable, nontoxic benzylstyrylsulfone based compound with anti-tumor and radiosensitizing properties. Potently suppresses PI 3-K/Akt/mTOR signaling pathway and activates Cdc25C phosphatases. Acts as an allosteric, substrate-competitive, and reversible inhibitor of multiple protein kinases (IC50 = 32, 42, 182, 18 and 155 nM against Bcr-Abl, Flt1, Fyn, PDGFR, and Src, respectively). Induces DNA damage and blocks microtubule formation. Also shown to cause mitotic arrest and apoptosis in multiple types of cancer cells (GI50 = 30 - 200 nM) and blocks cell cycle at G2/M phase. Effective against several multi-drug resistance tumor cells (IC50 = 50-100 nM). Suppresses the growth of BT20 tumor xenografts in mice and improves their survival rate (200 mg/kg, i.v. Q2D X 20 schedule). However, it displays limited oral bioavailability.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number592542-60-4
Chemical formulaC₂₁H₂₄NNaO₈S
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesLu, T., et al. 2015. Mol. Pharmacol. 87, 18.
Ramana Reddy, M.V., et al. 2011. J. Med. Chem. 54, 6254.
Gumireddy, K., et al. 2005. Cancer Cell 7, 275.