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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
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 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP2NlAhdk1? Mnf6O|IhcA>? NGfyNXhFVVOR NHT4epdKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? M{OwOFI2QTF4Nkm4
CS-THL1 MUPBdI9xfG:2aXOgRZN{[Xl? MkTJNlUhdk1? M1T0ZWROW09? NIPCT2tKdmS3Y3XzJIFxd3C2b4Ppdy=> MlfYNlU6OTZ4OUi=
DoGKiT M4rZZ2Fxd3C2b4TpZ{BCe3OjeR?= NInBb2k2OCCwTR?= NVzTfmJXTE2VTx?= MmHmTY5lfWOnczDhdI9xfG:|aYO= MnS3NlU6OTZ4OUi=
RS4-11 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELLOFI4OiCq MnTITWM2OD1yLkC0NFIh|ryP MYKyOVY1QTd4OB?=
NALM-6 NUjsVlc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\nZ3kxPzJiaB?= MYfJR|UxRjNizszN M2HVWFI2PjR7N{[4
SU-DHL-6 MoTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLINE45KM7:TR?= NH3JcW5KdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? M{PRZ|I2PTlyOECz
OCI-Ly19 MlvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV22UYhjOSEQvF2= MV\Jcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> MYOyOVU6ODhyMx?=
SU-DHL-6 NGXp[VFHfW6ldHnvckBCe3OjeR?= MVWwMlc2KM7:TR?= MWCxPEBp NYL4N2h[UW6lcnXhd4V{KHC{bz3zeZJ3cX[jbDDwdo91\WmwIF3DUE0yKGW6cILld5Nqd25? NUHqV3ZpOjV3OUC4NFM>
KCL22 NF\4OlJHfW6ldHnvckBCe3OjeR?= MWSyJO69VQ>? NIHRTHU1QCCq NX7mWW9CTE2VTx?= NXXMSHRNUW6lcnXhd4V{KESQQTDmdoFo[W2nboTheIlwdg>? M1\EPVI2OzN|MkWy
LOUCY M2Tu[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6xNEDPxE1? M4PUU|Q5KGh? M3vreGROW09? M2XFd2lEPTB;MD6wNVM6KM7:TR?= NHzTVnYzPTNyMUewOC=>
ALL-SIL MmXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17ifVExKM7:TR?= Mmn1OFghcA>? MULEUXNQ NWPXUZVPUUN3ME2wMlE5ODNizszN M4TsNVI2OzBzN{C0
CUTLL1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmxNEDPxE1? MVm0PEBp MmnGSG1UVw>? NXLsSWh5UUN3ME2wMlM5OjNizszN MkTUNlU{ODF5MES=
KOPTK1 NH\WeodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjJfXBLOTBizszN NF64U4M1QCCq NXnPfpNkTE2VTx?= NELyR|BKSzVyPUCuOlQ{OiEQvF2= NVrSdlA1OjV|MEG3NFQ>
DND-41 Mlr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DnXVExKM7:TR?= MXi0PEBp MlPHSG1UVw>? MU\JR|UxRTFwOU[5OUDPxE1? NGHCSnkzPTNyMUewOC=>
PF-382 M{TsSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljYNVAh|ryP M4mzR|Q5KGh? MX;EUXNQ M2fRcWlEPTB;Mj6xPFI1KM7:TR?= MoroNlU{ODF5MES=
KARPAS-45 NIDKe5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnCVIoyOCEQvF2= M2nKNlQ5KGh? NHn6co1FVVOR MWHJR|UxRTNwMkKyOUDPxE1? MoS0NlU{ODF5MES=
PEER MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUixNEDPxE1? MmrSOFghcA>? NHWzVldFVVOR NGTKfmVKSzVyPUSuOlQxOyEQvF2= NHTUT4YzPTNyMUewOC=>
CX-1 Mk[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PVVFExOCEQvF2= MknDO|IhcA>? MUDJR|UxRTZwNzFOwG0> NWC1S5FlOjV{MEi4PFI>
LS147T MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;hXmQyODBizszN NF21V4o4OiCq MWjJR|UxRTJ7LkWg{txO MYOyOVIxQDh6Mh?=
HL-60 MnPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHu1WXo1QCCq NXXmcG0yUUN3MEyxJO69VQ>? M1;LWFI1OzR4MUG2
MOLM-13 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLw[ZdDPDhiaB?= NVH0fnNTUUN3MEyxJO69VQ>? M1fzTFI1OzR4MUG2
OCI-AML2 M3zYUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;OZ|hDPDhiaB?= M4HKU2lEPTB:MTFOwG0> NFHVbZozPDN2NkGxOi=>
Kasumi-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHKyeWc1QCCq NYHVdVdEUUN3MEyxJO69VQ>? M1K3cFI1OzR4MUG2
KG-1 NWPR[oFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnDOlJXPDhiaB?= NFTsS2pKSzVyPEGg{txO NH7k[lczPDN2NkGxOi=>
THP-1 NWnzcnNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fkWlQ5KGh? MnPoTWM2ODxzIN88US=> NX7jTnU{OjR|NE[xNVY>
MOLM-14 M2DiOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3vR3k{PDhiaB?= NGDwO3dKSzVyPEGg{txO M3Pj[FI1OzR4MUG2
MOLM-13 MXXBdI9xfG:2aXOgRZN{[Xl? NXXNSZN1PTBibl2= MWKyOEBp Ml3xRZBweHSxc3nzJIlv\HWldHnvci=> NHzmXpQzPDN2NkGxOi=>
HSB NWXUc|NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlKxNVAh|ryP MV20PEBp MVXEUXNQ MWDJR|UxRTRwNES4JO69VQ>? MoT4NlQ{PDJ7NEi=
MOLT4 MlvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELJXowyOCEQvF2= NWf5OXU1PDhiaB?= M13HPWROW09? MUjJR|UxRTRwMUW0JO69VQ>? Mnr2NlQ{PDJ7NEi=
SKW-3/KE-37 NEf0WWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHkb5JyOTBizszN M3LHeVQ5KGh? MV\EUXNQ MnLWTWM2OD1yLkexNkDPxE1? MXqyOFM1Ojl2OB?=
SUPT-11 MnfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIP6cVEyOCEQvF2= NWLVZVNbPDhiaB?= M4jNcmROW09? MmHwTWM2OD12LkS3N{DPxE1? NFy3SYwzPDN2Mkm0PC=>
JURKAT MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPqNVAh|ryP MYK0PEBp NEHj[FJFVVOR M2PtOWlEPTB;ND64PVMh|ryP NHnyT3IzPDN2Mkm0PC=>
CCRF-CEM M4qzTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XUUVExKM7:TR?= MWq0PEBp MoezSG1UVw>? Ml;XTWM2OD1zLkO2NEDPxE1? NEfOcZAzPDN2Mkm0PC=>
LOUCY MmDTRZBweHSxdHnjJGF{e2G7 Ml\ONkDPxE1? M2POVlQ5KGh? NYjpSoZpTE2VTx?= NGPxOG1CeG:ydH;zbZMhcW6mdXP0bY9v M4jNXVI1OzR{OUS4

... 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 (115.14 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO+50% PEG 300+5% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 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