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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Cited by 289 Publications

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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 NYHONFB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTGeohlOjBibl2= NED1cnA4OiCq NW\kR5VbTE2VTx?= MoPVTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NEDEfJEzPTlzNk[5PC=>
CS-THL1 NXy0UJZbSXCxcITveIlkKEG|c3H5 NGrvTXkzPSCwTR?= NFjzb41FVVOR NYe2NWlnUW6mdXPld{BieG:ydH;zbZM> M3HyT|I2QTF4Nkm4
DoGKiT M1SyOWFxd3C2b4TpZ{BCe3OjeR?= NUHBVJVnPTBibl2= NIHydJBFVVOR NW\HeoZZUW6mdXPld{BieG:ydH;zbZM> NVPn[Zg3OjV7MU[2PVg>
RS4-11 NHqzVoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vjc|czKGh? MWnJR|UxRTBwMESwNkDPxE1? Mn7oNlU3PDl5Nki=
NALM-6 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XL[VczKGh? NUL0b3ZbUUN3ME6zJO69VQ>? NHj5bY8zPTZ2OUe2PC=>
SU-DHL-6 NWm4NVZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fTeVAvQCEQvF2= NV7JZ29pUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? M3XCcFI2PTlyOECz
OCI-Ly19 NWrlSINNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1f6b|Eh|ryP Mlz6TY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NX7kdXB[OjV3OUC4NFM>
SU-DHL-6 NEXQRW9HfW6ldHnvckBCe3OjeR?= M13WdlAvPzVizszN NVX1V3N3OThiaB?= MmXXTY5kemWjc3XzJJBzdy2|dYL2bZZidCCycn;0[YlvKE2FTD2xJIV5eHKnc4Ppc44> MnXRNlU2QTB6MEO=
KCL22 MWHGeY5kfGmxbjDBd5NigQ>? MVeyJO69VQ>? NF\r[IQ1QCCq MYDEUXNQ MXvJcoNz\WG|ZYOgSG5CKG[{YXfhcYVvfGG2aX;u MUWyOVM{OzJ3Mh?=
LOUCY M2ToXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVexNEDPxE1? MYm0PEBp M37oRWROW09? NVvPN4hrUUN3ME2wMlAyOzlizszN NHvsZVEzPTNyMUewOC=>
ALL-SIL MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXKxNEDPxE1? MUK0PEBp M1HNe2ROW09? MY\JR|UxRTBwMUiwN{DPxE1? MWeyOVMxOTdyNB?=
CUTLL1 NH3veWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYG0OGRROTBizszN NIXYN4g1QCCq NH7TZpdFVVOR MXTJR|UxRTBwM{iyN{DPxE1? MUWyOVMxOTdyNB?=
KOPTK1 NXP5ZnpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jjbFExKM7:TR?= M3jMTlQ5KGh? MkXDSG1UVw>? M3Tk[GlEPTB;MD62OFMzKM7:TR?= NVvFdo93OjV|MEG3NFQ>
DND-41 MmnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;1[|QyOCEQvF2= MnLFOFghcA>? Mln5SG1UVw>? MWnJR|UxRTFwOU[5OUDPxE1? M4C2TlI2OzBzN{C0
PF-382 MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;5NVAh|ryP MWi0PEBp MXvEUXNQ NVf3VWVHUUN3ME2yMlE5OjRizszN NF;HZ3gzPTNyMUewOC=>
KARPAS-45 NGDDUndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrkZ28yOCEQvF2= MoC2OFghcA>? MnToSG1UVw>? NHztS2xKSzVyPUOuNlIzPSEQvF2= MlPJNlU{ODF5MES=
PEER MoTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvKbpVqOTBizszN NWKyRodtPDhiaB?= NH61TnhFVVOR M{LmWGlEPTB;ND62OFA{KM7:TR?= M1PLSFI2OzBzN{C0
CX-1 NEjUXYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjiNVAxKM7:TR?= NVXhR2tZPzJiaB?= NH3PNWNKSzVyPU[uO{DPxE1? MXuyOVIxQDh6Mh?=
LS147T MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXPSJlVOTByIN88US=> NVWwc|N5PzJiaB?= NGq3W|hKSzVyPUK5MlUh|ryP M2D4OFI2OjB6OEiy
HL-60 M{nuU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:zOWY1QCCq NY\1WXVKUUN3MEyxJO69VQ>? NG\YcFkzPDN2NkGxOi=>
MOLM-13 MnzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknnOFghcA>? MXrJR|UxRDFizszN Mn;3NlQ{PDZzMU[=
OCI-AML2 MmLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjtepVzPDhiaB?= MX7JR|UxRDFizszN NWH2V3BTOjR|NE[xNVY>
Kasumi-1 NVHoXIlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DabVQ5KGh? NWjJfFNmUUN3MEyxJO69VQ>? M1jpSlI1OzR4MUG2
KG-1 NXHDRWRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTFVYQ5PDhiaB?= MoDETWM2ODxzIN88US=> NVHYOnZ4OjR|NE[xNVY>
THP-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:xR5A1QCCq NV3oVnhwUUN3MEyxJO69VQ>? M3zpRVI1OzR4MUG2
MOLM-14 NV[yd4w2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33rUlQ5KGh? NWrFTII2UUN3MEyxJO69VQ>? NVroNnlzOjR|NE[xNVY>
MOLM-13 M1TWV2Fxd3C2b4TpZ{BCe3OjeR?= MlfEOVAhdk1? MnfqNlQhcA>? NWP4NXJLSXCxcITvd4l{KGmwZIXjeIlwdg>? Mn3ZNlQ{PDZzMU[=
HSB NXfaUFhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nqZlExKM7:TR?= NXP5bohuPDhiaB?= MX7EUXNQ Mne5TWM2OD12LkS0PEDPxE1? NICxVGQzPDN2Mkm0PC=>
MOLT4 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mln2NVAh|ryP M3fmc|Q5KGh? MXTEUXNQ MlrPTWM2OD12LkG1OEDPxE1? NY\vbWpQOjR|NEK5OFg>
SKW-3/KE-37 NEn0SJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn34NVAh|ryP NEfBU5E1QCCq MnfvSG1UVw>? MoryTWM2OD1yLkexNkDPxE1? NEjOUmEzPDN2Mkm0PC=>
SUPT-11 MlHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVqxZXNDOTBizszN NH;6OoQ1QCCq NFr5Sm5FVVOR MUfJR|UxRTRwNEezJO69VQ>? M3[5ZVI1OzR{OUS4
JURKAT NGrR[XdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33lNlExKM7:TR?= MnryOFghcA>? NFTZWnVFVVOR NUDvPFdTUUN3ME20Mlg6OyEQvF2= NUK5VWJXOjR|NEK5OFg>
CCRF-CEM NVzZTFg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fqVlExKM7:TR?= MWS0PEBp MX7EUXNQ M2TKSGlEPTB;MT6zOlAh|ryP M1fYW|I1OzR{OUS4
LOUCY NF62OZlCeG:ydH;0bYMhSXO|YYm= M{Hvd|Ih|ryP MVi0PEBp M2HCemROW09? MmPVRZBweHSxc3nzJIlv\HWldHnvci=> NUjHcHM4OjR|NEK5OFg>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Mcl-1 / Bcl-xl / Bcl-2 / Bak / NOXA / Bim; 

PubMed: 30663221     


A549 cells were treated with Ibr-7, ABT-199 or a combination for 2 or 4 h. Total RNA was extracted from A549 cells to undergo RT-qPCR assay.

PARP / Cleaved PARP / Caspase 3 / Cleaved caspase3 / p-S6(Ser236/236); 

PubMed: 30663221     


A549 cells were treated with Ibr-7, ABT-199 or a combination for 24 h before western blotting assay. 

30663221
Growth inhibition assay
Cell death; 

PubMed: 28714472     


The indicated cell lines, treated with 2 μM doxorubicin±1 or 2 μM ABT-199, were quantified by annexin-V staining at 24 h for H2171 and H446 or at 48 h for H196 and SW1271 (mean±s.d., n=3). 

Cell viability; 

PubMed: 29876007     


TNBC cells were cultured with the indicated doses of ABT-199 (μM) for 48 h. 

28714472 29876007
Immunofluorescence
Bcl-2 / Mcl-1; 

PubMed: 28767232     


HEK293T cells cotransfected with the plasmids. Upon transfection, DMSO carrier control, 0.5 μM ABT-199, 10 μM A1210477, or a combination of both 0.5 μM ABT-199 and 10 μM A1210447 were added to the cells. After 30 h, the cells were analyzed for GFP and RFP expression by fluorescence microscopy.

28767232
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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04073147 Not yet recruiting Drug: Venetoclax|Drug: Obinutuzumab Primary CNS Lymphoma Klinikum Stuttgart|University Hospital Freiburg November 2019 Phase 1
NCT04070768 Not yet recruiting Drug: Gemtuzumab Ozogamicin|Drug: Venetoclax Acute Myeloid Leukemia Big Ten Cancer Research Consortium|Pfizer|AbbVie October 2019 Phase 1
NCT03943342 Not yet recruiting Drug: Ibrutinib|Drug: Venetoclax Chronic Lymphocytic Leukemia|Loss of Chromosome 17p Kerry Rogers|National Cancer Institute (NCI)|Janssen Research & Development LLC|Ohio State University Comprehensive Cancer Center September 1 2019 Phase 2
NCT03900884 Not yet recruiting Drug: Venetoclax|Drug: Palbociclib|Drug: Letrozole Breast Neoplasm Female Peter MacCallum Cancer Centre Australia September 2019 Phase 1

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.

Handling Instructions

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