Venetoclax (ABT-199, GDC-0199)
Molecular Weight(MW): 868.44
Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.
Cited by 18 Publications
3 Customer Reviews
THP-1 cells were treated with cytarabine alone and in combination with ABT-199 for 8 h. Whole cell lysates were extracted and subjected to Western blotting, and probed with anti-γH2AX or -β-actin antibody. Densitometry for γH2AX expression was measured, normalized to β-actin, and graphed as fold change compared to the no drug control. The data are presented as mean ± standard error from at least 3 independent Western blots. * indicates p < 0.05.
Mol Oncol 2014 10.1016/j.molonc.2014.09.008. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.
C33A cells were treated with ABC294640 (5 μmol/L), together with/out ABT-737 (200 nM) or GDC-0199 (200 nM), cells were further cultured for indicated time, cell growth (MTT assay, (A) and apoptosis (Histone DNA ELISA assay, (B) were tested.
Oncotarget, 2017, 9(2):2384-2394. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.
Purity & Quality Control
Choose Selective Bcl-2 Inhibitors
|Description||Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.|
|Features||Re-engineered version of ABT-263 (Navitoclax).|
ABT-199 shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with Ki of 48 nM, > 444 nM and 245 nM, respectively. ABT-199 potently inhibits FL5.12-Bcl-2 cells, RS4;11 cells with EC50 of 4 nM and 8 nM, while shows low activity against FL5.12-Bcl-xL cells with EC50 of 261 nM. ABT-199 induces a rapid apoptosis in RS4;11 cells with cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA. Quantitative immunoblotting reveals that sensitivity to ABT-199 correlated strongly with the expression of Bcl-2, including NHL, DLBCL, MCL, AML and ALL cell lines. ABT-199 also induces apoptosis in CLL with an average EC50 of 3.0 nM. 
|In vivo||ABT-199 (100 mg/kg) causes a maximal tumor growth inhibition of 95% and tumor growth delay of 152% in RS4;11 xenografts. ABT-199 also inhibits xenograft growth (DoHH2, Granta-519) as a single agent or in combination with SDX-105 and other agents. |
Binding affinity assays:Binding affinities (Ki or IC50) of ABT-199 against different isoforms of Bcl-2 family are determined with competitive fluorescence polarization assays. The following peptide probe/protein pairs are used: f-bad (1 nM) and Bcl-xL (6 nM), f-Bax (1 nM) and Bcl-2 (10 nM), f-Bax (1 nM) and Bcl-w (40 nM), f-Noxa (2 nM) and Mcl-1 (40 nM), and f-Bax (1 nM) and Bcl-2-A1 (15 nM). Binding affinities for Bcl-xL are also determined using a time-resolved fluorescence resonance energy transfer assay. Bcl-xL (1 nM, His tagged) is mixed with 200 nM f-Bak, 1 nM Tb-labeled anti-His antibody, and ABT-199 at room temperature for 30 min. Fluorescence is measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-His antibody) emission filters.
|In vitro||DMSO||100 mg/mL warmed (115.14 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+50% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03583424||Recruiting||Hematopoietic Cell Transplantation Recipient|Recurrent Diffuse Large B-Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Non-Hodgkin Lymphoma|Refractory Diffuse Large B-Cell Lymphoma|Refractory Follicular Lymphoma|Refractory Marginal Zone Lymphoma|Refractory Non-Hodgkin Lymphoma|Refractory Transformed Indolent Non-Hodgkin Lymphoma||Ohio State University Comprehensive Cancer Center|National Cancer Institute (NCI)||July 9 2018||Phase 1|Phase 2|
|NCT03379051||Recruiting||Chronic Lymphocytic Leukemia||TG Therapeutics Inc.|James P. Wilmot Cancer Center||April 9 2018||Phase 1|Phase 2|
|NCT03415035||Recruiting||Chronic Lymphocytic Leukemia (CLL)||AbbVie||March 9 2018||--|
|NCT03223610||Recruiting||Lymphoma|Non-Hodgkin Lymphoma|Diffuse Large B-Cell Lymphoma|Burkitt Lymphoma||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||February 9 2018||Phase 1|
|NCT03236857||Recruiting||Malignancies|Acute Lymphoblastic Leukemia (ALL)|Acute Myeloid Leukemia (AML)|Non-Hodgkin''s Lymphoma|Neuroblastoma||AbbVie|Roche-Genentech||November 9 2017||Phase 1|
|NCT02611323||Recruiting||Non-Hodgkin''s Lymphoma||Hoffmann-La Roche||March 9 2016||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Could you please offer some advice on the half-life of the drug ?
According to the reference (https://www.ncbi.nlm.nih.gov/pubmed/24212376), the half-life of ABT-199 in dogs is 12.9 hr.
how to prepare the working solution for mice including how to dissolve the powder?
We recommend the following vehicle for ABT 199, 30% PEG400/0.5% Tween80/5% Propylene glycol (64.5% water, V/V), at a concentration up to 20mg/ml. Its a homogeneous suspension and can be used for oral gavage.