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 M{Tlb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[yNEBvVQ>? MXS3NkBp M4\5b2ROW09? M13uc2lvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 NFXP[2czPTlzNk[5PC=>
CS-THL1 MnzjRZBweHSxdHnjJGF{e2G7 MXyyOUBvVQ>? NX\XUIl3TE2VTx?= NV;BTmVmUW6mdXPld{BieG:ydH;zbZM> MoXxNlU6OTZ4OUi=
DoGKiT NWPYbYluSXCxcITveIlkKEG|c3H5 NITvT4Y2OCCwTR?= Mn;mSG1UVw>? M{jy[Wlv\HWlZYOgZZBweHSxc3nz M3jkVFI2QTF4Nkm4
RS4-11 MlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHK5VXg4OiCq MUTJR|UxRTBwMESwNkDPxE1? M3;h[VI2PjR7N{[4
NALM-6 MlvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTiO|IhcA>? M4DWXWlEPTB-MzFOwG0> MVGyOVY1QTd4OB?=
SU-DHL-6 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rBd|AvQCEQvF2= MX\Jcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> NUjFbJRrOjV3OUC4NFM>
OCI-Ly19 M4DIcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnBTY1iOSEQvF2= NFrUUIdKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? NEPvRlQzPTV7MEiwNy=>
SU-DHL-6 NEHycpNHfW6ldHnvckBCe3OjeR?= NH3vNIUxNjd3IN88US=> MUWxPEBp NUOyWY1YUW6lcnXhd4V{KHC{bz3zeZJ3cX[jbDDwdo91\WmwIF3DUE0yKGW6cILld5Nqd25? MV[yOVU6ODhyMx?=
KCL22 NGT2OJhHfW6ldHnvckBCe3OjeR?= MkG5NkDPxE1? MYq0PEBp MVfEUXNQ M4fxXmlv[3KnYYPld{BFVkFiZoLh[4Fu\W62YYTpc44> M{S5S|I2OzN|MkWy
LOUCY M3nNWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYG2U21xOTBizszN M3XzSFQ5KGh? MVrEUXNQ MY\JR|UxRTBwMEGzPUDPxE1? NUPiT5RxOjV|MEG3NFQ>
ALL-SIL MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPabZYyOCEQvF2= NVzV[41wPDhiaB?= MYrEUXNQ NWL5ZXZiUUN3ME2wMlE5ODNizszN NGf1RVEzPTNyMUewOC=>
CUTLL1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILr[JcyOCEQvF2= M{HvWVQ5KGh? NHPMUnBFVVOR M{TEdmlEPTB;MD6zPFI{KM7:TR?= M4rMb|I2OzBzN{C0
KOPTK1 M4rmcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT3NVAh|ryP MXy0PEBp NVzZU3FSTE2VTx?= MW\JR|UxRTBwNkSzNkDPxE1? MWSyOVMxOTdyNB?=
DND-41 MkK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{T3fVExKM7:TR?= NHTm[VY1QCCq NVvQXW9jTE2VTx?= MWrJR|UxRTFwOU[5OUDPxE1? NFHTRm4zPTNyMUewOC=>
PF-382 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjtNVAh|ryP NUe5enVEPDhiaB?= MVPEUXNQ M{\qRWlEPTB;Mj6xPFI1KM7:TR?= NIjiO3czPTNyMUewOC=>
KARPAS-45 M1zJfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOxNEDPxE1? NELlNI41QCCq NH\Odm5FVVOR MlnzTWM2OD1|LkKyNlUh|ryP M3LSR|I2OzBzN{C0
PEER MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G2SFExKM7:TR?= MVS0PEBp M3LnPGROW09? MoWxTWM2OD12Lk[0NFMh|ryP Ml;qNlU{ODF5MES=
CX-1 MkfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULJNVFbOTByIN88US=> M{LGUFczKGh? NVzEXnE6UUN3ME22Mlch|ryP MWeyOVIxQDh6Mh?=
LS147T NX\QW4VCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;Zd|VqOTByIN88US=> M3HNT|czKGh? Mn:2TWM2OD1{OT61JO69VQ>? NYr5ZXZXOjV{MEi4PFI>
HL-60 NFrBe2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HvNVQ5KGh? MYjJR|UxRDFizszN MXGyOFM1PjFzNh?=
MOLM-13 Mk\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXO0PEBp NYS2ZotsUUN3MEyxJO69VQ>? M2\3N|I1OzR4MUG2
OCI-AML2 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rOclQ5KGh? NW\FT|lIUUN3MEyxJO69VQ>? M17qZlI1OzR4MUG2
Kasumi-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHvdYdEPDhiaB?= MYDJR|UxRDFizszN MXKyOFM1PjFzNh?=
KG-1 M{Hx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfZOFghcA>? M1fsVGlEPTB:MTFOwG0> MYKyOFM1PjFzNh?=
THP-1 NXHBcZpbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGGybGo1QCCq MUXJR|UxRDFizszN M1myR|I1OzR4MUG2
MOLM-14 NHf0UVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fPbVQ5KGh? MmXlTWM2ODxzIN88US=> M1jWflI1OzR4MUG2
MOLM-13 NGrifVhCeG:ydH;0bYMhSXO|YYm= NUDKOHdqPTBibl2= NXjVVWt3OjRiaB?= NFvNTJpCeG:ydH;zbZMhcW6mdXP0bY9v MnrTNlQ{PDZzMU[=
HSB NH3Wc|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4n2ZlExKM7:TR?= M{PZcVQ5KGh? MoXNSG1UVw>? MU\JR|UxRTRwNES4JO69VQ>? NELmfpQzPDN2Mkm0PC=>
MOLT4 NXrPU|g{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LW[VExKM7:TR?= NV\ZTGhYPDhiaB?= NFPKdG5FVVOR NH20XWtKSzVyPUSuNVU1KM7:TR?= NYPLO|VlOjR|NEK5OFg>
SKW-3/KE-37 M4HIXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXnZXQyOCEQvF2= MVW0PEBp NVvDdnROTE2VTx?= M1fPe2lEPTB;MD63NVIh|ryP NGqwcHAzPDN2Mkm0PC=>
SUPT-11 NFrQVJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnaeZB7OTBizszN NG\afFE1QCCq NE\nW|NFVVOR NHfFNnVKSzVyPUSuOFc{KM7:TR?= NH\Rd4EzPDN2Mkm0PC=>
JURKAT M1fjVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOxNEDPxE1? MUS0PEBp NYDKeIhKTE2VTx?= M3j0UWlEPTB;ND64PVMh|ryP M{HLUFI1OzR{OUS4
CCRF-CEM MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHm3emoyOCEQvF2= MXG0PEBp MXrEUXNQ NUXVO2F1UUN3ME2xMlM3OCEQvF2= NXL2WHU6OjR|NEK5OFg>
LOUCY MYjBdI9xfG:2aXOgRZN{[Xl? MUmyJO69VQ>? NH;PbXM1QCCq NIi3VppFVVOR MXrBdI9xfG:|aYOgbY5lfWO2aX;u NVm0W2V1OjR|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]

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