5.33575

Rigosertib

• 동의어(들): Rigosertib, Sodium ( E)-2-(2-methoxy-5-((2,4,6-trimethoxystyrylsulfonyl)methyl)phenylamino)acetate, ON01910, Na, Estybon
• 실험식(Hill 표기법): C₂₁H₂₄NNaO₈S
• CAS Number: 592542-60-4
• Molecular Weight: 473.47
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• Quality Level: 100
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: off-white
• solubility: DMSO: 50 mg/mL
• 저장 온도: 2-8°C
• InChI: 1S/C21H25NO8S.Na/c1-27-15-10-19(29-3)16(20(11-15)30-4)7-8-31(25,26)13-14-5-6-18(28-2)17(9-14)22-12-21(23)24;/h5-11,22H,12-13H2,1-4H3,(H,23,24);/q;+1/p-1/b8-7+;
• InChI key: VLQLUZFVFXYXQE-USRGLUTNSA-M

설명

일반 설명

A 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.

A 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.

Rigosertib, CAS 592542-60-4, is a cell-permeable, potent suppressor of PI 3-K/Akt/mTOR signaling. Allosterically inhibits several key protein kinases that are over active in many cancer cells.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
PI 3-K/Akt/mTOR signaling

Target IC₅₀: 32, 42, 182, 18 and 155 nM against Bcr-Abl, Flt1, Fyn, PDGFR, and Src, respectively

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

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 Cell7, 275.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable