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
USD 270 In stock
USD 970 In stock
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2 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.

    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).
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 M1e4Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV36VXVtOjBibl2= MnzFO|IhcA>? M1fwRWROW09? NX\Qb4RsUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? MUOyOVkyPjZ7OB?=
DoGKiT NYfQXYx2SXCxcITveIlkKEG|c3H5 NUfw[VI6PTBibl2= M1z0ZWROW09? NGHmbFNKdmS3Y3XzJIFxd3C2b4Ppdy=> M37RU|I2QTF4Nkm4
RS4-11 MmfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPVPWk4OiCq NWLIN3A6UUN3ME2wMlA1ODJizszN M4HWXFI2PjR7N{[4
NALM-6 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7Mb5g1PzJiaB?= MYTJR|UxRjNizszN NITtUnEzPTZ2OUe2PC=>
SU-DHL-6 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofuNE45KM7:TR?= MkLiTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> M3ixXVI2PTlyOECz
OCI-Ly19 NEmzempIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfDNXEyKM7:TR?= MVPJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> NVvVXnk6OjV3OUC4NFM>
SU-DHL-6 NW\qTVdKTnWwY4Tpc44hSXO|YYm= MXOwMlc2KM7:TR?= NXfrVJI{OThiaB?= NWCwbmloUW6lcnXhd4V{KHC{bz3zeZJ3cX[jbDDwdo91\WmwIF3DUE0yKGW6cILld5Nqd25? M{HhcVI2PTlyOECz
KCL22 NF;ZV4pHfW6ldHnvckBCe3OjeR?= M37OflIh|ryP MoPUOFghcA>? MnX3SG1UVw>? NF6yVnBKdmO{ZXHz[ZMhTE6DIH\yZYdidWWwdHH0bY9v MmLqNlU{OzN{NUK=
LOUCY Mm\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfveG4{OTBizszN M2jEV|Q5KGh? M4\nemROW09? NFj6WIpKSzVyPUCuNFE{QSEQvF2= MWiyOVMxOTdyNB?=
PEER NF;xOlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3mxblExKM7:TR?= NVzs[nNCPDhiaB?= Mke2SG1UVw>? M1[1cmlEPTB;ND62OFA{KM7:TR?= M13UO|I2OzBzN{C0
CX-1 MlHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrUc5kyODBizszN NXOzcZdHPzJiaB?= M{m3bmlEPTB;Nj63JO69VQ>? NXPaV2pwOjV{MEi4PFI>
LS147T MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWexNFAh|ryP M3TiRlczKGh? NWTVWZZnUUN3ME2yPU42KM7:TR?= M2rBNFI2OjB6OEiy
HL-60 NX7we5dGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;udFQ5KGh? NGDWN|RKSzVyPEGg{txO MVmyOFM1PjFzNh?=
MOLM-13 M3Tld2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDFT2x[PDhiaB?= NIrVUWhKSzVyPEGg{txO M{\QbFI1OzR4MUG2
OCI-AML2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHTOFghcA>? MWnJR|UxRDFizszN NITlWYUzPDN2NkGxOi=>
Kasumi-1 M{H4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWCwR5VsPDhiaB?= MYjJR|UxRDFizszN MlnRNlQ{PDZzMU[=
KG-1 M1TvUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH60VYQ1QCCq MVjJR|UxRDFizszN MnznNlQ{PDZzMU[=
THP-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfxOFghcA>? M1XXZ2lEPTB:MTFOwG0> M{\pTlI1OzR4MUG2
MOLM-14 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzxOFghcA>? NUGwWmc5UUN3MEyxJO69VQ>? NUDYTIhkOjR|NE[xNVY>
MOLM-13 Mk[4RZBweHSxdHnjJGF{e2G7 M1Tn[VUxKG6P NF;UTm4zPCCq Ml7mRZBweHSxc3nzJIlv\HWldHnvci=> MXKyOFM1PjFzNh?=
HSB M{HKVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rMT|ExKM7:TR?= MnSxOFghcA>? NYTCRYs{TE2VTx?= MV7JR|UxRTRwNES4JO69VQ>? Mo[wNlQ{PDJ7NEi=
MOLT4 MnL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3UclJ5OTBizszN NYH3N5NtPDhiaB?= MkDySG1UVw>? NGmzSXhKSzVyPUSuNVU1KM7:TR?= M{frNlI1OzR{OUS4
SUPT-11 MlzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rrcVExKM7:TR?= Mn3wOFghcA>? NXP6ZXBITE2VTx?= MUnJR|UxRTRwNEezJO69VQ>? NHGxPGYzPDN2Mkm0PC=>
JURKAT NIXvUHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M164flExKM7:TR?= MnjHOFghcA>? NYfkbpJTTE2VTx?= NUeyXmpuUUN3ME20Mlg6OyEQvF2= Mm\sNlQ{PDJ7NEi=
LOUCY NV\XZoRnSXCxcITveIlkKEG|c3H5 Mlu3NkDPxE1? NXzoVnpxPDhiaB?= NHyzfIZFVVOR M4C4[mFxd3C2b4Ppd{BqdmS3Y4Tpc44> Mk\aNlQ{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]


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 individually and in order:
5% DMSO+50% PEG 300+5% Tween 80+ddH2O

* 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


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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02756897 Recruiting Leukemia|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma M.D. Anderson Cancer Center|AbbVie July 7, 2016 Phase 2
NCT03036904 Not yet recruiting Diffuse Large B-Cell Lymphoma|High Grade B-Cell Lymphoma Weill Medical College of Cornell University|Genentech, Inc.|Massachusetts General Hospital|M.D. Anderson Cancer Center February 6, 2017 Phase 1
NCT02951117 Not yet recruiting Multiple Myeloma AbbVie May 2017 Phase 1
NCT02966756 Not yet recruiting Chronic Lymphocytic Leukemia (CLL) AbbVie|Genentech/Roche April 2017 Phase 2
NCT02966782 Not yet recruiting Myelodysplastic Syndromes (MDS) AbbVie|Genentech, Inc. March 2017 Phase 1
NCT03045328 Not yet recruiting Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma Steven E. Coutre|Stanford University March 2017 Phase 1|Phase 2

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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

  • Question 1:

    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