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.

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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)
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 M3jScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HHN|IxKG6P M1PIflczKGh? M3TDcGROW09? MXfJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> MlqzNlU6OTZ4OUi=
CS-THL1 MmroRZBweHSxdHnjJGF{e2G7 NEC1OnUzPSCwTR?= MVPEUXNQ MV3JcoR2[2W|IHHwc5B1d3Orcx?= M2DUNFI2QTF4Nkm4
DoGKiT NGnxSnlCeG:ydH;0bYMhSXO|YYm= NF;LVG82OCCwTR?= Mn6zSG1UVw>? M{TDT2lv\HWlZYOgZZBweHSxc3nz NUfIe3d5OjV7MU[2PVg>
RS4-11 M1PZXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXT0VIlmPzJiaB?= MkPDTWM2OD1yLkC0NFIh|ryP MUOyOVY1QTd4OB?=
NALM-6 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHr0VoY4OiCq Mm\yTWM2OD5|IN88US=> M12zXlI2PjR7N{[4
SU-DHL-6 NETScm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjVVWwxNjhizszN MoHGTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> M33zS|I2PTlyOECz
OCI-Ly19 M4Hxd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fTbFEh|ryP NF3KVI1KdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MX6yOVU6ODhyMx?=
SU-DHL-6 NUnwNJZMTnWwY4Tpc44hSXO|YYm= MW[wMlc2KM7:TR?= M{HKNVE5KGh? NEnzUGJKdmO{ZXHz[ZMheHKxLYP1dpZqfmGuIIDyc5RmcW5iTVPMMVEh\XiycnXzd4lwdg>? MknuNlU2QTB6MEO=
KCL22 NUfiV2wyTnWwY4Tpc44hSXO|YYm= NETxTFMzKM7:TR?= NWfpTVE1PDhiaB?= MknHSG1UVw>? Mkn4TY5kemWjc3XzJGRPSSCocnHnZY1mdnSjdHnvci=> M1jvWVI2OzN|MkWy
LOUCY NGjkNXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqxNEDPxE1? NEHMPIw1QCCq Ml7hSG1UVw>? NEPRfVJKSzVyPUCuNFE{QSEQvF2= MVSyOVMxOTdyNB?=
ALL-SIL NGewWlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13QWVExKM7:TR?= NVzTVYRkPDhiaB?= NF62[o5FVVOR NWDTcoR2UUN3ME2wMlE5ODNizszN NFjvSZkzPTNyMUewOC=>
CUTLL1 M3;0O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\NNVAh|ryP M{XKdlQ5KGh? NYHNdGFVTE2VTx?= MUXJR|UxRTBwM{iyN{DPxE1? NHTlVVEzPTNyMUewOC=>
KOPTK1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\0fHBmOTBizszN NH;0e5E1QCCq M2jiR2ROW09? NYK3V4dmUUN3ME2wMlY1OzJizszN NXnxS41COjV|MEG3NFQ>
DND-41 NXfXcXk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O1PVExKM7:TR?= MXG0PEBp MVXEUXNQ NH7F[4VKSzVyPUGuPVY6PSEQvF2= M{LU[|I2OzBzN{C0
PF-382 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV6xNEDPxE1? M2rSelQ5KGh? NFvLVm1FVVOR M{PrdWlEPTB;Mj6xPFI1KM7:TR?= MXeyOVMxOTdyNB?=
KARPAS-45 NHXtUGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1W4NFExKM7:TR?= NV3RVm9JPDhiaB?= Mnz1SG1UVw>? MojaTWM2OD1|LkKyNlUh|ryP NXfRW5VqOjV|MEG3NFQ>
PEER NVjrPW91T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;jSVExKM7:TR?= MW[0PEBp MkL0SG1UVw>? NV7rUWpmUUN3ME20MlY1ODNizszN M2rBcVI2OzBzN{C0
CX-1 MoD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFmwbpcyODBizszN NIqye4s4OiCq MnzOTWM2OD14Lkeg{txO NYjVXlNjOjV{MEi4PFI>
LS147T MmDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;0fHZYOTByIN88US=> M1O3RlczKGh? NEW3dpFKSzVyPUK5MlUh|ryP MVOyOVIxQDh6Mh?=
HL-60 NXzyfVdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU[0PEBp MmHDTWM2ODxzIN88US=> NH;kT|UzPDN2NkGxOi=>
MOLM-13 MkfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXy0PEBp M374b2lEPTB:MTFOwG0> MoLHNlQ{PDZzMU[=
OCI-AML2 NV;5fHF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjDOFghcA>? NVHlTGtGUUN3MEyxJO69VQ>? MUCyOFM1PjFzNh?=
Kasumi-1 NYHONllJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXviU41YPDhiaB?= M2TyUmlEPTB:MTFOwG0> NXjwOWdyOjR|NE[xNVY>
KG-1 NFfzdpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPvbGk1QCCq NVXHdnV4UUN3MEyxJO69VQ>? NGTnXXEzPDN2NkGxOi=>
THP-1 MoW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmm5OFghcA>? M4mxWmlEPTB:MTFOwG0> MljDNlQ{PDZzMU[=
MOLM-14 NU\ZTY5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYf3ZVVWPDhiaB?= M{LBVGlEPTB:MTFOwG0> NWrFTVhVOjR|NE[xNVY>
MOLM-13 MVjBdI9xfG:2aXOgRZN{[Xl? M2TUN|UxKG6P NEPudWMzPCCq MWXBdI9xfG:|aYOgbY5lfWO2aX;u Mmr3NlQ{PDZzMU[=
HSB M4jwRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LYN|ExKM7:TR?= M3L4cVQ5KGh? MXHEUXNQ M4LEO2lEPTB;ND60OFgh|ryP NGj2O4MzPDN2Mkm0PC=>
MOLT4 Mn\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXoWnMyOCEQvF2= MknzOFghcA>? MlLySG1UVw>? M3G2dWlEPTB;ND6xOVQh|ryP Mlj0NlQ{PDJ7NEi=
SKW-3/KE-37 MlzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[xNEDPxE1? MnTWOFghcA>? NHLyWW5FVVOR NIHEeG5KSzVyPUCuO|EzKM7:TR?= M2rR[FI1OzR{OUS4
SUPT-11 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF6zW5oyOCEQvF2= MnTXOFghcA>? M3z0OWROW09? MVrJR|UxRTRwNEezJO69VQ>? Mmn2NlQ{PDJ7NEi=
JURKAT NFG3[VJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDCWG8yOCEQvF2= MWC0PEBp MnHYSG1UVw>? M1Kw[mlEPTB;ND64PVMh|ryP MoPrNlQ{PDJ7NEi=
CCRF-CEM NFvUPZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLnXJI3OTBizszN MojtOFghcA>? NU\O[4NFTE2VTx?= MXvJR|UxRTFwM{[wJO69VQ>? M3jsbVI1OzR{OUS4
LOUCY NV3JRXcxSXCxcITveIlkKEG|c3H5 MYCyJO69VQ>? MnTOOFghcA>? NHO3NlZFVVOR MoTVRZBweHSxc3nzJIlv\HWldHnvci=> NVLZTlhrOjR|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 <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