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ABT-737

Cat. No. M1638
ABT-737 Structure
Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 300 In stock
100mg USD 420 In stock
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Quality Control
Biological Activity

ABT-737 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins. The ABT-737 single-agent LC90 values ranged from 100 nM for COG-LL-319 and RS4; 11 cells to low micromolar concentrations for the other five ALL cell lines. ABT-737 efficiently induces apoptosis and suppresses growth of hepatoma cells in combination with sorafenib. Moreover, we observed that the enhancement of ABT-737-mediated apoptosis by NCTD was associated with activation of mitochondrial apoptosis signaling pathway, which involved cytosolic release of cytochrome c, cleavage of caspase-9 and caspase-3. Finally, knockdown of Mcl-1 substantially potentiated ABT-737-mediated apoptotic cell death, confirming the potency of Mcl-1 repression by NCTD in enhancing ABT-737-induced apoptosis. These results therefore suggest that combination treatment with NCTD can overcome ABT-737 resistance and enhance ABT-737 therapeutic efficacy in treating human HCC.

Protocol
Cell Experiment
Cell lines CLL cells and platelets
Preparation method Apoptosis analysis Peripheral blood mononuclear cells were purified using Histopaque and cultured in RPMI 1640 medium supplemented with 10% fetal calf serum and 2 mmol/l L-glutamine at2*106 cells/ml. Cells were exposed to different concentrations of ABT-737, ABT-263, or ABT-199 for 4 h before analysis of apoptosis by externalisation of phosphatidylserine (PS) and binding of AnnexinV/fluorescein isothiocyanate (FITC). Platelets isolated from healthy volunteers were cultured in Hepes-buffered saline and exposed to different concentrations of ABT-737, ABT-263, or ABT-199 for 4 h before analysis of apoptosis in the CD41-positive population by externalisation of PS and binding of AnnexinV/FITC.
Concentrations 0~3µM
Incubation time 4 h
Animal Experiment
Animal models C57BL/6 mice were injected (i.v.) with 3x106 T1 lymphoma cells
Formulation formulated in 60% phosal 50PG (standardized phosphatidylcholine concentrate with at least 50% PC and propylene glycol
Dosages 100 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 813.43
Formula C42H45ClN6O5S2
CAS Number 852808-04-9
Purity 100.00%
Solubility DMSO ≥150 mg/mL
Storage at -20°C
References

Norcantharidin enhances ABT-737-induced apoptosis in hepatocellular carcinoma cells by transcriptional repression of Mcl-1.
Zhang et al. Cell Signal. 2012 Sep;24(9):1803-9. PMID: 22609455.

MEK inhibition enhances ABT-737-induced leukemia cell apoptosis via prevention of ERK-activated MCL-1 induction and modulation of MCL-1/BIM complex.
Konopleva et al. Leukemia. 2012 Apr;26(4):778-87. PMID: 22064351.

The Bcl-xL inhibitor, ABT-737, efficiently induces apoptosis and suppresses growth of hepatoma cells in combination with sorafenib.
Hikita et al. Hepatology. 2010 Oct;52(4):1310-21. PMID: 20799354.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ABT-737 supplier, Bcl-2, inhibitors

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