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ABT-199 (Venetoclax)

Cat. No. M2017
ABT-199 (Venetoclax) Structure
Synonym:

GDC-0199, Venetoclax

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 70  USD70 In stock
2mg USD 30  USD30 In stock
5mg USD 55  USD55 In stock
10mg USD 75  USD75 In stock
50mg USD 95  USD95 In stock
100mg USD 125  USD125 In stock
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Quality Control & Documentation
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.

Product Citations
Customer Product Validations & Biological Datas
Source Cell Death & Disease (2018). Figure 2. ABT199 (Abmole Bioscience)
Method Cell viability analysis
Cell Lines MDA-MB-231, MDA-MB-157, and MDA-MB-468 cells
Concentrations 1 μM
Incubation Time 24 h
Results But treatment with Temsirolimus in combination with ABT263 or ABT199 only induced modest cell viability inhibition.
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.
Protocol (for reference only)
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
Chemical Information
Molecular Weight 868.44
Formula C45H50ClN7O7S
CAS Number 1257044-40-8
Solubility (25°C) DMSO 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Vandenberg CJ, et al. Blood. ABT-199, a new Bcl-2-specific BH3 mimetic, has in vivo efficacy against aggressive Myc-driven mouse lymphomas without provoking thrombocytopenia.

[2] Souers AJ, et al. Nat Med. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.

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Keywords: ABT-199 (Venetoclax), GDC-0199, Venetoclax supplier, Bcl-2, inhibitors, activators


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