Venetoclax (ABT-199)

For research use only.

Catalog No.S8048 Synonyms: GDC-0199

335 publications

Venetoclax (ABT-199) 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. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.

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Selleck's Venetoclax (ABT-199) has been cited by 335 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. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. 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 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvrTVczOCCwTR?= MUG3NkBp MWLEUXNQ MoLpTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> MYqyOVkyPjZ7OB?=
CS-THL1 MYHBdI9xfG:2aXOgRZN{[Xl? NUXvUmE{OjVibl2= MYrEUXNQ NUm5W2xRUW6mdXPld{BieG:ydH;zbZM> M2HydlI2QTF4Nkm4
DoGKiT MVXBdI9xfG:2aXOgRZN{[Xl? NGf4cVI2OCCwTR?= MWTEUXNQ MVvJcoR2[2W|IHHwc5B1d3Orcx?= NYfiR456OjV7MU[2PVg>
RS4-11 MkfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rPNVczKGh? NIjiXmxKSzVyPUCuNFQxOiEQvF2= Ml2zNlU3PDl5Nki=
NALM-6 M3HwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TFWVczKGh? MnK1TWM2OD5|IN88US=> NWXTRmxpOjV4NEm3Olg>
SU-DHL-6 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVuwMlgh|ryP MofjTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NWH6[2JkOjV3OUC4NFM>
OCI-Ly19 NFXyZpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\BelEh|ryP NY\aZnhTUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? M3rnT|I2PTlyOECz
SU-DHL-6 NWm1R293TnWwY4Tpc44hSXO|YYm= NXn6eFdzOC55NTFOwG0> MlXVNVghcA>? MlPCTY5kemWjc3XzJJBzdy2|dYL2bZZidCCycn;0[YlvKE2FTD2xJIV5eHKnc4Ppc44> MmXiNlU2QTB6MEO=
KCL22 MVvGeY5kfGmxbjDBd5NigQ>? NHrBNmUzKM7:TR?= M13LTlQ5KGh? MlzKSG1UVw>? MWTJcoNz\WG|ZYOgSG5CKG[{YXfhcYVvfGG2aX;u M1zCVlI2OzN|MkWy
LOUCY M1rJVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzLNo4yOCEQvF2= M3LYR|Q5KGh? NUjo[oRJTE2VTx?= NFnUVIVKSzVyPUCuNFE{QSEQvF2= NHnsbmczPTNyMUewOC=>
ALL-SIL NU\QXmtsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvPW3AyOCEQvF2= MoHmOFghcA>? NFvuXXRFVVOR MoHCTWM2OD1yLkG4NFMh|ryP M3fKU|I2OzBzN{C0
CUTLL1 NHu3cFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPvNVAh|ryP Mn3IOFghcA>? MXrEUXNQ MkjJTWM2OD1yLkO4NlMh|ryP M2ToR|I2OzBzN{C0
KOPTK1 M4LzVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnlNVAh|ryP NHPLcVQ1QCCq Mn7iSG1UVw>? M2\1[2lEPTB;MD62OFMzKM7:TR?= NIX2VWEzPTNyMUewOC=>
DND-41 NHfVT|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PXPVExKM7:TR?= MlX6OFghcA>? M4i0WmROW09? MWTJR|UxRTFwOU[5OUDPxE1? MUWyOVMxOTdyNB?=
PF-382 NX\mWpp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWW0eIYyOTBizszN NULUO3JWPDhiaB?= MmS5SG1UVw>? M3TVNmlEPTB;Mj6xPFI1KM7:TR?= MXSyOVMxOTdyNB?=
KARPAS-45 M3rLNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnScYoyOCEQvF2= NUf3Zm9NPDhiaB?= NEn6bHFFVVOR MlG4TWM2OD1|LkKyNlUh|ryP MXeyOVMxOTdyNB?=
PEER NWHPUGo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\0WpcyOCEQvF2= NEHFc|c1QCCq MlHUSG1UVw>? MWnJR|UxRTRwNkSwN{DPxE1? M{O4e|I2OzBzN{C0
CX-1 NIHKO4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWn0elBlOTByIN88US=> NEntfoM4OiCq NWfnbIV6UUN3ME22Mlch|ryP NF7helEzPTJyOEi4Ni=>
LS147T M1jQ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUixNFAh|ryP M3HVblczKGh? NXja[5JwUUN3ME2yPU42KM7:TR?= M2myPFI2OjB6OEiy
HL-60 NWTpc3dZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M164[lQ5KGh? MUHJR|UxRDFizszN M4P4NVI1OzR4MUG2
MOLM-13 MnvPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYq0PEBp MlPyTWM2ODxzIN88US=> M4TCe|I1OzR4MUG2
OCI-AML2 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXTUIg1PDhiaB?= M3fDUmlEPTB:MTFOwG0> M2n6[|I1OzR4MUG2
Kasumi-1 NV\MPVE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITFO|A1QCCq NGjsV4xKSzVyPEGg{txO MofENlQ{PDZzMU[=
KG-1 NFP4SYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUK0PEBp NXW5SGlGUUN3MEyxJO69VQ>? MUCyOFM1PjFzNh?=
THP-1 NY[1SXJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfjOFghcA>? MmSzTWM2ODxzIN88US=> NXjzSW1UOjR|NE[xNVY>
MOLM-14 M1LteWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHnTZc1QCCq M{XNW2lEPTB:MTFOwG0> MUOyOFM1PjFzNh?=
MOLM-13 M3\1fWFxd3C2b4TpZ{BCe3OjeR?= MXq1NEBvVQ>? MYqyOEBp NXn5S3FuSXCxcITvd4l{KGmwZIXjeIlwdg>? M1HBV|I1OzR4MUG2
HSB NIPtWYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXxUng2OTBizszN MmjROFghcA>? NFLi[pZFVVOR M3vjTWlEPTB;ND60OFgh|ryP NX73enFFOjR|NEK5OFg>
MOLT4 MojZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuxNEDPxE1? NFP5RnU1QCCq NXnUXmZ4TE2VTx?= NVnrTnhbUUN3ME20MlE2PCEQvF2= MUiyOFM1Ojl2OB?=
SKW-3/KE-37 NF3yNmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmxNEDPxE1? MUS0PEBp NHnV[2hFVVOR M{j4VGlEPTB;MD63NVIh|ryP M1myeVI1OzR{OUS4
SUPT-11 NH\WbYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP6Ro5XOTBizszN M2TTfFQ5KGh? NIDDRWRFVVOR M17LRmlEPTB;ND60O|Mh|ryP MnOyNlQ{PDJ7NEi=
JURKAT M1;XVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zRclExKM7:TR?= M1zwPVQ5KGh? NVy5XmxDTE2VTx?= MVrJR|UxRTRwOEmzJO69VQ>? MVuyOFM1Ojl2OB?=
CCRF-CEM M4LhSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHENll[OTBizszN M1zBS|Q5KGh? MlTiSG1UVw>? NVTGb|lVUUN3ME2xMlM3OCEQvF2= MVqyOFM1Ojl2OB?=
LOUCY MmOyRZBweHSxdHnjJGF{e2G7 MXOyJO69VQ>? MofoOFghcA>? MnrESG1UVw>? MUTBdI9xfG:|aYOgbY5lfWO2aX;u M2KxPFI1OzR{OUS4

... 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]
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  • 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)
  • 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 GDC-0199
Smiles CC1(C)CCC(=C(C1)C2=CC=C(Cl)C=C2)CN3CCN(CC3)C4=CC(=C(C=C4)C(=O)N[S](=O)(=O)C5=CC=C(NCC6CCOCC6)C(=C5)[N+]([O-])=O)OC7=CN=C8[NH]C=CC8=C7

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03557619 Recruiting Drug: Venetoclax|Drug: ethinyl estradiol/levonorgestrel Hematologic Malignancies AbbVie August 28 2020 Phase 1
NCT04284787 Not yet recruiting Drug: Azacitidine|Biological: Pembrolizumab|Drug: Venetoclax Acute Myeloid Leukemia|Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome|Secondary Acute Myeloid Leukemia National Cancer Institute (NCI) June 5 2020 Phase 2
NCT04298918 Not yet recruiting Drug: Placebo|Drug: Venetoclax|Drug: Trastuzumab emtansine Breast Cancer Hoffmann-La Roche May 28 2020 Phase 1|Phase 2
NCT04150029 Not yet recruiting Drug: MBG453|Drug: Venetoclax|Drug: Azacitidine Acute Myeloid Leukemia Novartis Pharmaceuticals|Novartis May 11 2020 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