ABT-737

• Catalog No.: S1002
• CAS Number: 852808-04-9
• M. F.: C42H45ClN6O5S2
• M. W.: 813.4269
• Storage: -20°C

SYNONYMS

• IUPAC name: 4-(4-{[2-(4-chlorophenyl)phenyl]methyl}piperazin-1-yl)-N-(4-{[(2R)-4-(dimethylamino)-1-(phenylsulfanyl)butan-2-yl]amino}-3-nitrobenzenesulfonyl)benzamide
• IUPAC Traditional name: 4-(4-{[2-(4-chlorophenyl)phenyl]methyl}piperazin-1-yl)-N-(4-{[(2R)-4-(dimethylamino)-1-(phenylsulfanyl)butan-2-yl]amino}-3-nitrobenzenesulfonyl)benzamide

DATABASE IDS

• CAS Number: 852808-04-9

PROPERTIES

• Target: Bcl-2
• Salt Data: Free Base
• Solubility: DMSO
• Storage Condition: -20°C

DETAILS

Description (English)

Research Area

• Description: Cancer

Protocol

• Protocol: Kinase Assay ^[1]
• Fluorescence polarization assays: Binding affinity of GST-Bcl-2 family proteins to the FITC-conjugated BH3 domain of Bim (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is determined. Briefly, 100 nM of GST-Bcl-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-Bim BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. Then IC50 are determined.
• Protocol: Cell Assay ^[4]
• Cell Lines: SCLC cell lines NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114
• Concentrations: 0.001-10 μM
• Incubation Time: 48 hours
• Methods:

  SCLC cells are treated for 48 hours in 96-well tissue culture plates in a total volume of 100 μL tissue culture medium supplemented with 10% human serum. Viable cells are determined using the MTS assay.

• Protocol: Animal Study ^[1]
• Animal Models: Scid mice injected with Luc-expressing FD/ΔRaf-1:ER cells
• Formulation: 1 g/mL stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4?5; final concentration of DMSO ≤ 1%)
• Doses: 20 and 30 mg/kg
• Administration: For intraperitoneal (i.p.) every day

References

• References: [1] Konopleva M, et al. Cancer Cell, 2006, 10(5), 375-388.
• References: [2] van Delft MF,et al. Cancer Cell, 2006, 10(5), 389-399.
• References: [3] Del Gaizo Moore V, et al. J Clin Invest, 2007, 117(1), 112-121.
• References: [4] Tahir SK, et al. Cancer Res, 2007, 67(3), 1176-1183.
• References: [5] Ishitsuka K, et al. Cancer Lett, 2012, 317(2), 218-225.
• References: [6] Hikita H, et al. Hepatology. 2010, 52(4), 1310-21.
• References: [7] Whitecross KF, et al, Blood, 2009, 113(9), 1982-1991.

REFERENCES

• Tahir SK, et al. Cancer Res, 2007, 67(3), 1176-1183.
• Ishitsuka K, et al. Cancer Lett, 2012, 317(2), 218-225.
• Hikita H, et al. Hepatology. 2010, 52(4), 1310-21.
• Whitecross KF, et al, Blood, 2009, 113(9), 1982-1991.
• Konopleva M, et al. Cancer Cell, 2006, 10(5), 375-388.
• van Delft MF,et al. Cancer Cell, 2006, 10(5), 389-399.
• Del Gaizo Moore V, et al. J Clin Invest, 2007, 117(1), 112-121.