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

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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).
Bcl-2 [1]
(Cell-free assay)
Bcl-xL [1]
(Cell-free assay)
Bcl-w [1]
(Cell-free assay)
Mcl-1 [1]
(Cell-free assay)
<0.01 nM(Ki) 48 nM(Ki) 245 nM(Ki) >444 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 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkW5NlAhdk1? MlPSO|IhcA>? M2DobmROW09? MlvlTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NUOzV4Q2OjV7MU[2PVg>
CS-THL1 NULSV3Z7SXCxcITveIlkKEG|c3H5 Mmi0NlUhdk1? NH3KdIVFVVOR NVq3NJkxUW6mdXPld{BieG:ydH;zbZM> MWOyOVkyPjZ7OB?=
DoGKiT NFv5c5BCeG:ydH;0bYMhSXO|YYm= Mo\iOVAhdk1? NUjtbmV[TE2VTx?= NH7uRlNKdmS3Y3XzJIFxd3C2b4Ppdy=> MYGyOVkyPjZ7OB?=
RS4-11 M3K0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[0O|IhcA>? NXXUcpZxUUN3ME2wMlA1ODJizszN NE\0OpIzPTZ2OUe2PC=>
NALM-6 NX7LV5R7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LGR|czKGh? MlPFTWM2OD5|IN88US=> M3fFVlI2PjR7N{[4
SU-DHL-6 NYWwU|VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2wMlgh|ryP NVLZWpU1UW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? NILvPHEzPTV7MEiwNy=>
OCI-Ly19 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrKZooyKM7:TR?= MV;Jcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> MlrpNlU2QTB6MEO=
SU-DHL-6 NWjxVppWTnWwY4Tpc44hSXO|YYm= NYC1TpI1OC55NTFOwG0> NVjWZolxOThiaB?= MkfxTY5kemWjc3XzJJBzdy2|dYL2bZZidCCycn;0[YlvKE2FTD2xJIV5eHKnc4Ppc44> Ml6xNlU2QTB6MEO=
KCL22 M2ntXWZ2dmO2aX;uJGF{e2G7 MV6yJO69VQ>? MYS0PEBp MULEUXNQ MmjnTY5kemWjc3XzJGRPSSCocnHnZY1mdnSjdHnvci=> NI\0fY8zPTN|M{K1Ni=>
LOUCY MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrqZpA{OTBizszN NY\CNY9sPDhiaB?= MXTEUXNQ MoXITWM2OD1yLkCxN|kh|ryP M3;aV|I2OzBzN{C0
CUTLL1 NIT1PXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[5VFExKM7:TR?= M2PsfVQ5KGh? MoW5SG1UVw>? MnH5TWM2OD1yLkO4NlMh|ryP MYWyOVMxOTdyNB?=
DND-41 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XlUlExKM7:TR?= NUn0NZBMPDhiaB?= M1TyPGROW09? NVqxcnZrUUN3ME2xMlk3QTVizszN NED0ZYEzPTNyMUewOC=>
CX-1 NUG1TGlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXLOlIyODBizszN MlXCO|IhcA>? NY\IN29CUUN3ME22Mlch|ryP NID3So4zPTJyOEi4Ni=>
LS147T Mnr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\uNVAxKM7:TR?= MlTrO|IhcA>? M3zMfWlEPTB;MkmuOUDPxE1? NInoXGIzPTJyOEi4Ni=>
HL-60 M4qxOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLrOFghcA>? NWLHUFh6UUN3MEyxJO69VQ>? M2i4PVI1OzR4MUG2
OCI-AML2 NVOwT3hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWj0Um9nPDhiaB?= NH\TWIRKSzVyPEGg{txO NYe2O5A5OjR|NE[xNVY>
Kasumi-1 M3L4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j3SFQ5KGh? NEjXRmZKSzVyPEGg{txO MorBNlQ{PDZzMU[=
KG-1 NUS3Sm1RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvyOFghcA>? M2D3T2lEPTB:MTFOwG0> M2HCVlI1OzR4MUG2
THP-1 NF;GOHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV20PEBp MVrJR|UxRDFizszN NF;1fogzPDN2NkGxOi=>
MOLM-14 M1uyVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DrR|Q5KGh? M1nmUGlEPTB:MTFOwG0> MXyyOFM1PjFzNh?=
MOLM-13 MUTBdI9xfG:2aXOgRZN{[Xl? MUG1NEBvVQ>? NUH6XXZQOjRiaB?= MXvBdI9xfG:|aYOgbY5lfWO2aX;u NU\sRmpOOjR|NE[xNVY>
MOLT4 M4nmWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHUNVAh|ryP M3LB[VQ5KGh? MlzDSG1UVw>? NXPa[3B7UUN3ME20MlE2PCEQvF2= MYWyOFM1Ojl2OB?=
SKW-3/KE-37 MkjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LFflExKM7:TR?= MXm0PEBp NUfvSWk2TE2VTx?= NHfhTG1KSzVyPUCuO|EzKM7:TR?= NEPQVYYzPDN2Mkm0PC=>
SUPT-11 Mlr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn6[olOOTBizszN M1z2dlQ5KGh? MmDPSG1UVw>? M2exemlEPTB;ND60O|Mh|ryP MX2yOFM1Ojl2OB?=
JURKAT NHrJXWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF71TXEyOCEQvF2= MmTrOFghcA>? NUfpdoplTE2VTx?= M3vCOmlEPTB;ND64PVMh|ryP NEj2bJkzPDN2Mkm0PC=>
LOUCY M4jkVmFxd3C2b4TpZ{BCe3OjeR?= M3XXfVIh|ryP MXS0PEBp MlqySG1UVw>? MWfBdI9xfG:|aYOgbY5lfWO2aX;u NUW5RYxmOjR|NEK5OFg>

... 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
in solvent
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID