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Ridaifen-B

Catalog No. R5030 Name Sigma Aldrich
CAS Number 886465-70-9 Website http://www.sigmaaldrich.com
M. F. C34H42N2O2 Telephone 1-800-521-8956
M. W. 510.70948 Fax
Purity ≥98% (HPLC) Email
Storage desiccated Chembase ID: 154100

SYNONYMS

IUPAC name
1-{2-[4-(2-phenyl-1-{4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}but-1-en-1-yl)phenoxy]ethyl}pyrrolidine
IUPAC Traditional name
1-{2-[4-(2-phenyl-1-{4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}but-1-en-1-yl)phenoxy]ethyl}pyrrolidine
Synonyms
1,1′-[(2-Phenyl-1-buten-1-ylidene)bis(4,1-phenyleneoxy-2,1-ethanediyl)]bis-pyrrolidine

DATABASE IDS

MDL Number MFCD11114395
CAS Number 886465-70-9

PROPERTIES

Empirical Formula (Hill Notation) C34H42N2O2
Purity ≥98% (HPLC)
Apperance white solid
Solubility DMSO: ≥13 mg/mL
Solubility H2O: insoluble
GHS Pictograms GHS05
GHS Pictograms GHS07
GHS Signal Word Danger
GHS Hazard statements H315-H318-H335
European Hazard Symbols Irritant Irritant (Xi)
MSDS Link Download
Personal Protective Equipment dust mask type N95 (US), Eyeshields, Gloves
GHS Precautionary statements P261-P280-P305 + P351 + P338
Risk Statements 37/38-41
Safety Statements 26-39
Storage Condition desiccated
Storage Temperature 2-8°C
German water hazard class 3

DETAILS

Description (English)
Biochem/physiol Actions
Ridaifen-B (RID-B) is a novel tamoxifen (TAM) analog that significantly augments apoptosis-inducing effect of TAM in estrogen receptor (ER)-negatives cells. Ridaifen-B induces mitochondria-involved apoptosis in Jurkat cells, as evidenced by chromatin-condensed cells as well as downstream activation of caspases (caspase-3, -8 and -9) in a dose- and time-dependent manner. At 4 hours of incubation, IC50 for RID-B is 4 muM (30 muM for TAM). And at prolonged treatment of 48 hours, IC50 for RID-B is 0.1 muM.1 In a related report2 on the global anti-tumor activity, RID-B strongly inhibits 39 human cancer cells (JFCR 39), both ER-+ or ER-- at concentrations of equal or less than 1muM (e.g., at 0.38muM for SF-539 [central nervous system], at 0.58muM for HT-29 [colon], at 0.20muM for DMS114 [lung], at 0.21muM for LOX-IMVI [melanoma], and at 0.23muM for MKN74 [stomach]. The binding protein of RID-B that exerts the apoptosis events is currently under investigation.
Description (简体中文)
Biochem/physiol Actions
Ridaifen-B (RID-B) is a novel tamoxifen (TAM) analog that significantly augments apoptosis-inducing effect of TAM in estrogen receptor (ER)-negatives cells. Ridaifen-B induces mitochondria-involved apoptosis in Jurkat cells, as evidenced by chromatin-condensed cells as well as downstream activation of caspases (caspase-3, -8 and -9) in a dose- and time-dependent manner. At 4 hours of incubation, IC50 for RID-B is 4 muM (30 muM for TAM). And at prolonged treatment of 48 hours, IC50 for RID-B is 0.1 muM.1 In a related report2 on the global anti-tumor activity, RID-B strongly inhibits 39 human cancer cells (JFCR 39), both ER-+ or ER-- at concentrations of equal or less than 1muM (e.g., at 0.38muM for SF-539 [central nervous system], at 0.58muM for HT-29 [colon], at 0.20muM for DMS114 [lung], at 0.21muM for LOX-IMVI [melanoma], and at 0.23muM for MKN74 [stomach]. The binding protein of RID-B that exerts the apoptosis events is currently under investigation.

REFERENCES