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ABT-199

Cat. No. M2017
ABT-199 Structure
Synonym:

GDC-0199

Size Price Availability Quantity
10mg USD 200 In stock
50mg USD 500 In stock
100mg USD 720 In stock
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Quality Control
Biological Activity

ABT-199 (GDC-0199) is a new selective small molecule inhibitor of BCL-2 that appears to spare platelets while achieving potent antitumor activity. Proteins in the B cell CLL/lymphoma 2 (BCL-2) family are key regulators of the apoptotic process. As a single agent, ABT-199 was as effective as ABT-737 in prolonging survival of immunocompetent tumor-bearing mice without causing thrombocytopenia. ABT-199 (GDC-0199) is an engineered version of ABT-263 (Navitoclax) but with much better selectivity.

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 868.44
Formula C45H50ClN7O7S
CAS Number 1257044-40-8
Purity 100.00%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Oncotarget (2015). Figure 5. ABT 199 (Abmole BioScience)
Method Cell viability assay and Western blot
Cell Lines SNU668 and SNU638 cells
Concentrations 1 µM
Incubation Time 24 h
Results Combination 5-aza-dC and LPS treatment enhances binding activity of Sp1 and H3K4me3 in gastric cancer cells via activation of TLR4 signaling.
Rating
Product Citations
References

ABT-199, a new Bcl-2-specific BH3 mimetic, has in vivo efficacy against aggressive Myc-driven mouse lymphomas without provoking thrombocytopenia.
Vandenberg CJ, et al. Blood. 2013 Mar 21;121(12):2285-8. PMID: 23341542.

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.
Souers AJ, et al. Nat Med. 2013 Feb;19(2):202-8. PMID: 23291630.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ABT-199, GDC-0199 supplier, Bcl-2, inhibitors

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