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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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).
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 NXqzXm55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVuyNEBvVQ>? NIrIW3o4OiCq MYDEUXNQ MWHJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> NUTRUmhIOjV7MU[2PVg>
CS-THL1 MVfBdI9xfG:2aXOgRZN{[Xl? NXKxT4VDOjVibl2= NGjjdGRFVVOR M2\UNGlv\HWlZYOgZZBweHSxc3nz MYeyOVkyPjZ7OB?=
DoGKiT M125dWFxd3C2b4TpZ{BCe3OjeR?= MVK1NEBvVQ>? MmDrSG1UVw>? NUTOPHRLUW6mdXPld{BieG:ydH;zbZM> NIHsN4QzPTlzNk[5PC=>
RS4-11 MlPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWq3NkBp NXPjdXY{UUN3ME2wMlA1ODJizszN MX[yOVY1QTd4OB?=
NALM-6 NH71fllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGG3fHA4OiCq MlTwTWM2OD5|IN88US=> Mom5NlU3PDl5Nki=
SU-DHL-6 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTnV2t2OC56IN88US=> NIrpZYNKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MmDpNlU2QTB6MEO=
OCI-Ly19 NVfqPGM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTKXGRyOSEQvF2= NEDm[WZKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? M3LVfFI2PTlyOECz
SU-DHL-6 Mlq3SpVv[3Srb36gRZN{[Xl? MnyxNE44PSEQvF2= MVyxPEBp NX\nbpFWUW6lcnXhd4V{KHC{bz3zeZJ3cX[jbDDwdo91\WmwIF3DUE0yKGW6cILld5Nqd25? Mn3vNlU2QTB6MEO=
KCL22 NUfIR3VzTnWwY4Tpc44hSXO|YYm= NInWRXMzKM7:TR?= NXnNTndGPDhiaB?= NXvIdlBDTE2VTx?= M3j2Rmlv[3KnYYPld{BFVkFiZoLh[4Fu\W62YYTpc44> M3nqXVI2OzN|MkWy
LOUCY MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnXNVAh|ryP NGX0fFE1QCCq MmPXSG1UVw>? Mmr6TWM2OD1yLkCxN|kh|ryP NWrxb|BnOjV|MEG3NFQ>
ALL-SIL NGX0[5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUH4S2VlOTBizszN MWS0PEBp NXXBfZNLTE2VTx?= MlzZTWM2OD1yLkG4NFMh|ryP MlTLNlU{ODF5MES=
CUTLL1 NFzqS4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXWxNEDPxE1? M4TpVFQ5KGh? NXjtd4FbTE2VTx?= MVXJR|UxRTBwM{iyN{DPxE1? NWTFS2wyOjV|MEG3NFQ>
KOPTK1 M4nxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TnSlExKM7:TR?= MoS1OFghcA>? M{SyUmROW09? NEK1O49KSzVyPUCuOlQ{OiEQvF2= MXWyOVMxOTdyNB?=
DND-41 NWXKeoNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYj1XIRJOTBizszN MUi0PEBp NH3vcVRFVVOR M1z0XGlEPTB;MT65Olk2KM7:TR?= M1;G[|I2OzBzN{C0
PF-382 M4Gyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\Sc|ExKM7:TR?= MUi0PEBp MYTEUXNQ MWXJR|UxRTJwMUiyOEDPxE1? MYqyOVMxOTdyNB?=
KARPAS-45 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:w[VBoOTBizszN Mn\aOFghcA>? M1HsV2ROW09? NFn1c|lKSzVyPUOuNlIzPSEQvF2= MmjMNlU{ODF5MES=
PEER MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\kcVExKM7:TR?= MofuOFghcA>? MVHEUXNQ M3fxUGlEPTB;ND62OFA{KM7:TR?= M{XFbVI2OzBzN{C0
CX-1 NFPlWVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUCxNFAh|ryP NFnVSFE4OiCq MmnETWM2OD14Lkeg{txO MWKyOVIxQDh6Mh?=
LS147T NFi3d|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3zNVAxKM7:TR?= M3:5e|czKGh? MWrJR|UxRTJ7LkWg{txO MkDKNlUzODh6OEK=
HL-60 Ml;LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXr1TWNvPDhiaB?= NWPLXm8zUUN3MEyxJO69VQ>? MWqyOFM1PjFzNh?=
MOLM-13 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlu2OFghcA>? NHjCTXBKSzVyPEGg{txO MX6yOFM1PjFzNh?=
OCI-AML2 MmLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\RZlQ5KGh? MWfJR|UxRDFizszN M13hSlI1OzR4MUG2
Kasumi-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3H6bVQ5KGh? NEnHZm5KSzVyPEGg{txO M{n4WVI1OzR4MUG2
KG-1 M3PYZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1i0UVQ5KGh? NV63XItYUUN3MEyxJO69VQ>? NXfUcGRFOjR|NE[xNVY>
THP-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnX2OFghcA>? NIHxS4FKSzVyPEGg{txO MmTENlQ{PDZzMU[=
MOLM-14 NYfYR41qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzKOFghcA>? M4KycWlEPTB:MTFOwG0> NVPQ[WttOjR|NE[xNVY>
MOLM-13 NFTCWJVCeG:ydH;0bYMhSXO|YYm= MUS1NEBvVQ>? M3TQblI1KGh? MnjCRZBweHSxc3nzJIlv\HWldHnvci=> NXm3PVhSOjR|NE[xNVY>
HSB M1HhXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnsfWoyOCEQvF2= M12ye|Q5KGh? M1:0cGROW09? MlnqTWM2OD12LkS0PEDPxE1? M3\HUVI1OzR{OUS4
MOLT4 MoDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqxNEDPxE1? NWP3bJpCPDhiaB?= NFrv[mdFVVOR NVfQVmxmUUN3ME20MlE2PCEQvF2= M1TIdFI1OzR{OUS4
SKW-3/KE-37 NHTEfWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jDUVExKM7:TR?= NF\qfnc1QCCq M3zhNmROW09? MWnJR|UxRTBwN{GyJO69VQ>? M3TFSVI1OzR{OUS4
SUPT-11 NFrV[YpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKxNEDPxE1? NE\hNGU1QCCq MnHPSG1UVw>? NGTG[21KSzVyPUSuOFc{KM7:TR?= MWqyOFM1Ojl2OB?=
JURKAT MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;YfJA{OTBizszN M4XNPFQ5KGh? NU\HN2hmTE2VTx?= M3qxWmlEPTB;ND64PVMh|ryP NH\SUpYzPDN2Mkm0PC=>
CCRF-CEM NH;PZmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPINVAh|ryP MoPZOFghcA>? M3rCOWROW09? MnjETWM2OD1zLkO2NEDPxE1? NHO2N2EzPDN2Mkm0PC=>
LOUCY M1jJdmFxd3C2b4TpZ{BCe3OjeR?= M3LMT|Ih|ryP M1TOblQ5KGh? NWXa[29lTE2VTx?= NXX2WY4zSXCxcITvd4l{KGmwZIXjeIlwdg>? MnXXNlQ{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:
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
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

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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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