United States (Change Country)ABT-263 (Navitoclax) Chemical Structure
Overexpression of the prosurvival Bcl-2 family members (Bcl-2,Bcl-xL,and Mcl-1) is commonly associated with tumor maintenance, progression, and chemoresistance. Binding affinities were determined with competitive fluorescence polarization assays and a time-resolved fluorescence resonance energy transfer assay (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w). The oral bioavailability of ABT-263 in preclinical animal models is 20% to 50%, depending on formulation.[1]A wide range of SCLC cellular activity was observed with ABT-263 having a 50% growth inhibition (EC50) of 110 nmol/L against the most sensitive line (H146), whereas its activity in the least sensitive line (H82) resulted in an EC50 at 22 μmol/L. In all cell lines where the EC50 was <1 μmol/L, ABT-263 was more potent than its enantiomer by a factor of >20.[2]
| Molecular Weight (WM): | 974.61 |
|---|---|
| Formula: | C47H55ClF3N5O6S3 |
| Solubility(R.T.:25°C): | DMSO 195mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL |
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;Biochem Biophys Res Commun, 2011, 408(2), 344-9 ABT-263 (Navitoclax) purchased from Selleck
;PLoS One , 2011, 6, e21980 ABT-263 (Navitoclax) purchased from Selleck
;Clin Cancer Res, 2010, 16, 4217-4225 ABT-263 (Navitoclax) purchased from Selleck
;Clin Cancer Res, 2010, 16, 4217-4225 ABT-263 (Navitoclax) purchased from Selleck
;Clin Cancer Res, 2010, 16, 4217-4225 ABT-263 (Navitoclax) purchased from Selleck
;Cancer Res, 2011, 71, 4518-4526 ABT-263 (Navitoclax) purchased from Selleck
;PLoS One, 2011, 6, e21980 ABT-263 (Navitoclax) purchased from Selleck
;PLoS One, 2011, 6, e21980 ABT-263 (Navitoclax) purchased from Selleck
;Clin Cancer Res, 2010, 16, 4217-4225 ABT-263 (Navitoclax) purchased from Selleck
Data from [Clin Cancer Res 2010;16, 4217-4225] ABT-263 (Navitoclax) purchased from Selleck
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