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 M2[5OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnqT2wzOCCwTR?= MonMO|IhcA>? NHGx[3BFVVOR MVTJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> Mlf6NlU6OTZ4OUi=
CS-THL1 MWTBdI9xfG:2aXOgRZN{[Xl? M1zYflI2KG6P MorxSG1UVw>? NHHjOWZKdmS3Y3XzJIFxd3C2b4Ppdy=> M2PvZ|I2QTF4Nkm4
DoGKiT MoTWRZBweHSxdHnjJGF{e2G7 NYPCUHFWPTBibl2= NHTYXFFFVVOR MmmxTY5lfWOnczDhdI9xfG:|aYO= MlHTNlU6OTZ4OUi=
RS4-11 M{\YS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVy3NkBp M4OxPWlEPTB;MD6wOFAzKM7:TR?= Ml\NNlU3PDl5Nki=
NALM-6 NIKw[I9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUiz[o5iPzJiaB?= NYDv[WJzUUN3ME6zJO69VQ>? NV62[VJqOjV4NEm3Olg>
SU-DHL-6 NXXGWmYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1GwbVAvQCEQvF2= NUTPTolGUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? MmLYNlU2QTB6MEO=
OCI-Ly19 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[xJO69VQ>? NIrqfYpKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MXGyOVU6ODhyMx?=
SU-DHL-6 NUT5d4JnTnWwY4Tpc44hSXO|YYm= MkTBNE44PSEQvF2= NVvwRmlVOThiaB?= NGLGXJlKdmO{ZXHz[ZMheHKxLYP1dpZqfmGuIIDyc5RmcW5iTVPMMVEh\XiycnXzd4lwdg>? M2rDWFI2PTlyOECz
KCL22 MlPrSpVv[3Srb36gRZN{[Xl? NWXMVVh[OiEQvF2= NWDCdGFPPDhiaB?= M4Hn[mROW09? M2XGcmlv[3KnYYPld{BFVkFiZoLh[4Fu\W62YYTpc44> MoqwNlU{OzN{NUK=
LOUCY M{HWVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWKxNEDPxE1? MVO0PEBp MmT1SG1UVw>? NV3COHRzUUN3ME2wMlAyOzlizszN MX6yOVMxOTdyNB?=
ALL-SIL MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYGxNEDPxE1? NE[2OXY1QCCq NVLhenlKTE2VTx?= M{e5U2lEPTB;MD6xPFA{KM7:TR?= MmXnNlU{ODF5MES=
CUTLL1 NHPoNpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWxNEDPxE1? NFf0Snk1QCCq MVfEUXNQ NH;id3FKSzVyPUCuN|gzOyEQvF2= NGTvU5gzPTNyMUewOC=>
KOPTK1 NVTCTnZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV25RWExOTBizszN M2jWW|Q5KGh? MVHEUXNQ MWjJR|UxRTBwNkSzNkDPxE1? M{fQ[|I2OzBzN{C0
DND-41 M1LFS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3H0PFExKM7:TR?= NVX5[lNKPDhiaB?= MlziSG1UVw>? M2rHTmlEPTB;MT65Olk2KM7:TR?= NInzcoYzPTNyMUewOC=>
PF-382 NYHkSmJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPrNVAh|ryP MUC0PEBp MVfEUXNQ M2nT[GlEPTB;Mj6xPFI1KM7:TR?= MWGyOVMxOTdyNB?=
KARPAS-45 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PLZ|ExKM7:TR?= MVe0PEBp M2T4SmROW09? NFTKflBKSzVyPUOuNlIzPSEQvF2= M2TCN|I2OzBzN{C0
PEER MoXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDkSpEyOCEQvF2= M3PQPVQ5KGh? NW\pUFJiTE2VTx?= MVfJR|UxRTRwNkSwN{DPxE1? M{nVNFI2OzBzN{C0
CX-1 MmeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXPO41MOTByIN88US=> MWe3NkBp MXrJR|UxRTZwNzFOwG0> MYKyOVIxQDh6Mh?=
LS147T MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYOxNFAh|ryP NIjMPXQ4OiCq NGnofpBKSzVyPUK5MlUh|ryP NEOyeXozPTJyOEi4Ni=>
HL-60 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1SwNFQ5KGh? MYfJR|UxRDFizszN NHvKblIzPDN2NkGxOi=>
MOLM-13 MoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmq1OFghcA>? MlXwTWM2ODxzIN88US=> MmHrNlQ{PDZzMU[=
OCI-AML2 M1r5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYi0PEBp NEHWZoNKSzVyPEGg{txO MUWyOFM1PjFzNh?=
Kasumi-1 NV7OSodbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DnZlQ5KGh? Mmn6TWM2ODxzIN88US=> MU[yOFM1PjFzNh?=
KG-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzyRpdKPDhiaB?= Ml;RTWM2ODxzIN88US=> MXuyOFM1PjFzNh?=
THP-1 NUTUW5VOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TldlQ5KGh? NVziNXlqUUN3MEyxJO69VQ>? MX:yOFM1PjFzNh?=
MOLM-14 NULyOIxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTiOFghcA>? NFrrPXBKSzVyPEGg{txO M1qwW|I1OzR4MUG2
MOLM-13 M1K5NGFxd3C2b4TpZ{BCe3OjeR?= M1HlS|UxKG6P M4HsOVI1KGh? M2nZbmFxd3C2b4Ppd{BqdmS3Y4Tpc44> NIXCbmMzPDN2NkGxOi=>
HSB NXPLeZNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWxNEDPxE1? NX;IT2R6PDhiaB?= NVn0dGJRTE2VTx?= MVLJR|UxRTRwNES4JO69VQ>? MX:yOFM1Ojl2OB?=
MOLT4 MkWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDhT3gyOCEQvF2= MW[0PEBp MojaSG1UVw>? NHWzbIpKSzVyPUSuNVU1KM7:TR?= NEDLbmczPDN2Mkm0PC=>
SKW-3/KE-37 NFX3NppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXYVmwyOCEQvF2= NUf3[I9jPDhiaB?= M1jQcGROW09? MoC0TWM2OD1yLkexNkDPxE1? NXrHW3p1OjR|NEK5OFg>
SUPT-11 M3naVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzkfWsyOCEQvF2= NWTGXVc2PDhiaB?= NXvNe3dJTE2VTx?= MUPJR|UxRTRwNEezJO69VQ>? NXK1PGhOOjR|NEK5OFg>
JURKAT Mn2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\pNVAh|ryP MUC0PEBp M4PHWGROW09? M3\OV2lEPTB;ND64PVMh|ryP Moq2NlQ{PDJ7NEi=
CCRF-CEM MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmq3NVAh|ryP MYq0PEBp MmqzSG1UVw>? M1fCU2lEPTB;MT6zOlAh|ryP MXeyOFM1Ojl2OB?=
LOUCY MUDBdI9xfG:2aXOgRZN{[Xl? MnnRNkDPxE1? MmKyOFghcA>? M4G4W2ROW09? MoX6RZBweHSxc3nzJIlv\HWldHnvci=> MYSyOFM1Ojl2OB?=

... 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