Venetoclax (ABT-199, GDC-0199)

Catalog No.S8048

Venetoclax (ABT-199, GDC-0199) Chemical Structure

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.

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In DMSO USD 680 In stock
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5 Customer Reviews

  • (b) MV4-11 cells were treated in vitro with ABT-199 (0.01, 0.1, 1 or 10 μM) with or without BL-8040 (20 μM) for 24 h in 1% FCS RPMI medium. The percentage of dead cells (PI+ cells) was evaluated by FACS. (c) miR-15a and miR-16-1 transfections were performed using Lipofectamine 2000 transfection reagent. At 72 h post-transfection, cells were stained with Annexin-V and PI. FACS plots and numerical data of % cells are shown. The results are expressed as the mean±s.d. and were analyzed using Student’s t-test (*P ⩽0.05 compared with control).

    Leukemia, 2017, 31(11):2336-2346. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

    MDA-MB-468 cells were treated with BETd-246 (50 nM), BM-1197 (250 nM), ABT-263 (250 nM), ABT-199 (250 nM) or A-1155463 (250 nM) as indicated for 24 h for Annexin V-PI apoptosis analysis. Data are the mean ± SEM (n=3).

    Cancer Res, 2017, 77(9):2476-2487. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

  • 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.

  • CLL cells were incubated with drugs immediately or co-cultured on CD154 stroma overnight and incubated with the indicated concentrations of ABT-199.

    J Biol Chem 2014 289(23), 16190-9. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

Purity & Quality Control

Choose Selective Bcl-2 Inhibitors

Biological Activity

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).
Targets
Bcl-2 [1]
(Cell-free assay)
<0.01 nM(Ki)
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CS-THL1 MknxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4C1dVIxKG6P NWPCe2FZPzJiaB?= NFjseIlFVVOR M2e0TGlvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 NEnwfFAzPTlzNk[5PC=>
CS-THL1 MYfBdI9xfG:2aXOgRZN{[Xl? M1WyOlI2KG6P NVj5TYE3TE2VTx?= NIixT5NKdmS3Y3XzJIFxd3C2b4Ppdy=> MXuyOVkyPjZ7OB?=
DoGKiT NGqyTndCeG:ydH;0bYMhSXO|YYm= M1Th[|UxKG6P NEfNTGdFVVOR MUjJcoR2[2W|IHHwc5B1d3Orcx?= NHHYb5IzPTlzNk[5PC=>
RS4-11 MlPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVK3NkBp MmLSTWM2OD1yLkC0NFIh|ryP MYSyOVY1QTd4OB?=
NALM-6 NGnsWZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjQW|FwPzJiaB?= NH7wfItKSzVyPkOg{txO MV[yOVY1QTd4OB?=
SU-DHL-6 NWPSfGJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzrV2piOC56IN88US=> MYrJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> NWLxeWlLOjV3OUC4NFM>
OCI-Ly19 NF;0SmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXv4[oI4OSEQvF2= MoTYTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NXfPPJZjOjV3OUC4NFM>
SU-DHL-6 MYHGeY5kfGmxbjDBd5NigQ>? NYnVNFZxOC55NTFOwG0> Ml63NVghcA>? MX3JcoNz\WG|ZYOgdJJwNXO3co\peoFtKHC{b4TlbY4hVUOOLUGg[ZhxemW|c3nvci=> Mk[yNlU2QTB6MEO=
KCL22 NH3MZ5VHfW6ldHnvckBCe3OjeR?= MoriNkDPxE1? MXS0PEBp MX3EUXNQ NWrDUJc3UW6lcnXhd4V{KESQQTDmdoFo[W2nboTheIlwdg>? NWft[Fc5OjV|M{OyOVI>
LOUCY NETmV|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWxNEDPxE1? MXm0PEBp MVnEUXNQ NH;mdZFKSzVyPUCuNFE{QSEQvF2= MmjONlU{ODF5MES=
ALL-SIL M1:3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoX4NVAh|ryP NIXzcYc1QCCq MorQSG1UVw>? M4DJ[GlEPTB;MD6xPFA{KM7:TR?= M3ewcVI2OzBzN{C0
CUTLL1 NVzNUYN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIW2fnQyOCEQvF2= Mn3nOFghcA>? M4K2O2ROW09? NIXnOmVKSzVyPUCuN|gzOyEQvF2= M{XlSFI2OzBzN{C0
KOPTK1 Mny2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3JWmMyOCEQvF2= MlTLOFghcA>? NXy5fIdXTE2VTx?= MYDJR|UxRTBwNkSzNkDPxE1? MlXpNlU{ODF5MES=
DND-41 NUCzN4ZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVGxNEDPxE1? NYf6UGt6PDhiaB?= NWfudo06TE2VTx?= NGS3do5KSzVyPUGuPVY6PSEQvF2= MkPMNlU{ODF5MES=
PF-382 M4LVWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLNNVAh|ryP NX;SZodkPDhiaB?= NXO2O5p6TE2VTx?= MlvuTWM2OD1{LkG4NlQh|ryP NWfndJhEOjV|MEG3NFQ>
KARPAS-45 NUPXUIRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPvNVAh|ryP M3LsS|Q5KGh? NY\SbFNyTE2VTx?= NVLRb4R2UUN3ME2zMlIzOjVizszN NFTuVnQzPTNyMUewOC=>
PEER MlTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3MR5UyOCEQvF2= NF7LV|c1QCCq M3L5cmROW09? NYTXU2lUUUN3ME20MlY1ODNizszN NGD2UokzPTNyMUewOC=>
CX-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzXTZgyODBizszN NF3ON2c4OiCq NHLGTVNKSzVyPU[uO{DPxE1? Mm\pNlUzODh6OEK=
LS147T NFW3bJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSxNFAh|ryP M{TNXlczKGh? M2X5TWlEPTB;MkmuOUDPxE1? MkLGNlUzODh6OEK=
HL-60 MlrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELrNHI1QCCq MUDJR|UxRDFizszN NXTod3h4OjR|NE[xNVY>
MOLM-13 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrtcVI1QCCq NX3JUHZ[UUN3MEyxJO69VQ>? NVXhUIxxOjR|NE[xNVY>
OCI-AML2 NGfudZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHNO4dxPDhiaB?= NUT5TIgzUUN3MEyxJO69VQ>? NVjrfZhGOjR|NE[xNVY>
Kasumi-1 MkHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYm0PEBp M2fUTmlEPTB:MTFOwG0> Mk\LNlQ{PDZzMU[=
KG-1 NEnR[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVi0PEBp MnHYTWM2ODxzIN88US=> NUPOZ3hVOjR|NE[xNVY>
THP-1 Mnz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXW0PEBp NYXhRW5kUUN3MEyxJO69VQ>? MkC0NlQ{PDZzMU[=
MOLM-14 NGTvWmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vUZVQ5KGh? MUTJR|UxRDFizszN NUW2XHNGOjR|NE[xNVY>
MOLM-13 M2\tbmFxd3C2b4TpZ{BCe3OjeR?= NH3Le2c2OCCwTR?= MnjsNlQhcA>? NEmySIdCeG:ydH;zbZMhcW6mdXP0bY9v M3rkd|I1OzR4MUG2
HSB M{\aZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnzNVAh|ryP NFP1So41QCCq MkfhSG1UVw>? MVHJR|UxRTRwNES4JO69VQ>? MUmyOFM1Ojl2OB?=
MOLT4 M1XjWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3foOVExKM7:TR?= NVfSbYJ1PDhiaB?= NXzFfGlTTE2VTx?= M3jydmlEPTB;ND6xOVQh|ryP NX3YXXR6OjR|NEK5OFg>
SKW-3/KE-37 M{XkT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XYb|ExKM7:TR?= MnvIOFghcA>? M4rQTWROW09? NGmxPY5KSzVyPUCuO|EzKM7:TR?= NFO5UVgzPDN2Mkm0PC=>
SUPT-11 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX6xNEDPxE1? MWW0PEBp MnK2SG1UVw>? NYXTdnJTUUN3ME20MlQ4OyEQvF2= MnPQNlQ{PDJ7NEi=
JURKAT NFjlV3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWixNEDPxE1? MljEOFghcA>? NHzYSWtFVVOR MY\JR|UxRTRwOEmzJO69VQ>? NYOxc5BGOjR|NEK5OFg>
CCRF-CEM M2fJbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe4T24yOCEQvF2= MkTYOFghcA>? NVW5eJlmTE2VTx?= NX;YOYxyUUN3ME2xMlM3OCEQvF2= Mnn4NlQ{PDJ7NEi=
LOUCY M2Hyc2Fxd3C2b4TpZ{BCe3OjeR?= MkTKNkDPxE1? NGri[|E1QCCq MluwSG1UVw>? MUnBdI9xfG:|aYOgbY5lfWO2aX;u MnzKNlQ{PDJ7NEi=

... Click to View More Cell Line Experimental Data

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. [1]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[1]
+ Expand
  • Cell lines: NHL, DLBCL, MCL, AML and ALL cell lines
  • Concentrations: ~1 μM
  • Incubation Time: 48 hours
  • Method: RS4;11 cells are seeded at 5 × 104 per well in 96-well plates and treated with ABT-199 diluted in half-log steps starting at 1 μM-0.05 nM. Leukemia and lymphoma cell lines are seeded at 1.5-2 × 104 cells per well in the appropriate medium and incubated with ABT-199 for 48 h. Effects on proliferation are determined using Cell TiterGlo reagent. EC50 values are determined by nonlinear regression analysis of the concentration-response data.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Female C.B-17 SCID mice (DoHH2 and Granta-519 xenografts) and female C.B-17 SCID-beige mice (RS4;11 and Toledo xenografts)
  • Formulation: 60% phosal 50 propylene glycol (PG), 30% polyethylene glycol (PEG) 400 and 10% ethanol
  • Dosages: ~100 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (115.14 mM)
Water Insoluble
Ethanol Insoluble
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.
5mg/mL

* 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.

Chemical Information

Molecular Weight 868.44
Formula

C45H50ClN7O7S

CAS No. 1257044-40-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03735875 Not yet recruiting Acute Myeloid Leukemia With FLT3/ITD Mutation|FLT3 Gene Mutation|FLT3 Internal Tandem Duplication|Recurrent Acute Myeloid Leukemia|Refractory Acute Leukemia M.D. Anderson Cancer Center|National Cancer Institute (NCI) March 31 2019 Phase 1|Phase 2
NCT03708003 Not yet recruiting Relapsed/Refractory Chronic Lymphocytic Leukemia|Chronic Lymphocytic Leukemia|Leukemia Swiss Group for Clinical Cancer Research March 2019 Phase 2
NCT03710772 Not yet recruiting CD20 Positive|Mantle Cell Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) January 31 2019 Phase 2
NCT03701321 Not yet recruiting Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) January 25 2019 Phase 1|Phase 2
NCT03639324 Not yet recruiting Chronic Lymphocytic Leukemia|CLL|Relapsed CLL|Refractory Chronic Lymphocytic Leukemia|Relapsed Chronic Lymphocytic Leukemia Virginia Commonwealth University January 31 2019 Phase 1
NCT03573024 Not yet recruiting Acute Myeloid Leukemia University of Colorado Denver January 2019 Phase 2

Tech Support

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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Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Could you please offer some advice on the half-life of the drug ?

  • Answer:

    According to the reference (https://www.ncbi.nlm.nih.gov/pubmed/24212376), the half-life of ABT-199 in dogs is 12.9 hr.

  • Question 2:

    how to prepare the working solution for mice including how to dissolve the powder?

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID