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.

Size Price Stock Quantity  
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 M3zZTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXyZoxLOjBibl2= MUC3NkBp M1zYVWROW09? NFGyUmhKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? NH\UeZUzPTlzNk[5PC=>
CS-THL1 NIi4[mNCeG:ydH;0bYMhSXO|YYm= MX6yOUBvVQ>? NYXW[4dUTE2VTx?= MXvJcoR2[2W|IHHwc5B1d3Orcx?= MYCyOVkyPjZ7OB?=
DoGKiT NFH3VJpCeG:ydH;0bYMhSXO|YYm= NEm5[XM2OCCwTR?= NIfTWXZFVVOR NUfLZlJPUW6mdXPld{BieG:ydH;zbZM> NXrCXVlDOjV7MU[2PVg>
RS4-11 M4HvXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn2bY44OiCq M1\s[GlEPTB;MD6wOFAzKM7:TR?= MWmyOVY1QTd4OB?=
NALM-6 NYr0VnBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUi3NkBp NHfaS2FKSzVyPkOg{txO NUewelZmOjV4NEm3Olg>
SU-DHL-6 Mmi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrqd44xNjhizszN Mk\pTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> MnP5NlU2QTB6MEO=
OCI-Ly19 Moj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlu5NUDPxE1? MW\Jcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> MnPQNlU2QTB6MEO=
SU-DHL-6 MXLGeY5kfGmxbjDBd5NigQ>? NXvZeVVbOC55NTFOwG0> MX[xPEBp MnnvTY5kemWjc3XzJJBzdy2|dYL2bZZidCCycn;0[YlvKE2FTD2xJIV5eHKnc4Ppc44> M1TnSlI2PTlyOECz
KCL22 NFT1fYtHfW6ldHnvckBCe3OjeR?= NFXE[5EzKM7:TR?= NHHMXJM1QCCq NFnXNZpFVVOR MYTJcoNz\WG|ZYOgSG5CKG[{YXfhcYVvfGG2aX;u MoDoNlU{OzN{NUK=
LOUCY NInFeGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXmzWWl[OTBizszN NFiwVJc1QCCq NGPkUW5FVVOR M4LGSWlEPTB;MD6wNVM6KM7:TR?= NWXLWY9wOjV|MEG3NFQ>
ALL-SIL M2K4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUiy[XRDOTBizszN M3e5b|Q5KGh? M2rxb2ROW09? MX3JR|UxRTBwMUiwN{DPxE1? NXLj[FFTOjV|MEG3NFQ>
CUTLL1 M1vqSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPsU2YyOCEQvF2= NV;iVZNpPDhiaB?= NIm1XI9FVVOR NYH5bHl2UUN3ME2wMlM5OjNizszN NF:3fZUzPTNyMUewOC=>
KOPTK1 NH\DdmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjGO2p2OTBizszN MY[0PEBp M2P0[mROW09? M1LtVWlEPTB;MD62OFMzKM7:TR?= MWCyOVMxOTdyNB?=
DND-41 NYSxWHdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3OxcFExKM7:TR?= NE\nOXA1QCCq NFf1[ZBFVVOR Mlz2TWM2OD1zLkm2PVUh|ryP NF:zelgzPTNyMUewOC=>
PF-382 NEDZZm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWS4PJFUOTBizszN MkjvOFghcA>? M17RcWROW09? MYrJR|UxRTJwMUiyOEDPxE1? M3S2elI2OzBzN{C0
KARPAS-45 MmTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\MO5JSOTBizszN MUW0PEBp MnLZSG1UVw>? MVvJR|UxRTNwMkKyOUDPxE1? MUOyOVMxOTdyNB?=
PEER NYrj[o1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqxNEDPxE1? NWi4cmRSPDhiaB?= NYPSTI86TE2VTx?= NGGxUFVKSzVyPUSuOlQxOyEQvF2= MVOyOVMxOTdyNB?=
CX-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXyNVAxKM7:TR?= M1fkbVczKGh? MX3JR|UxRTZwNzFOwG0> M3HZZVI2OjB6OEiy
LS147T NXfJZ5hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrlR4IyODBizszN MmjIO|IhcA>? NYO3N2xjUUN3ME2yPU42KM7:TR?= MUCyOVIxQDh6Mh?=
HL-60 NHThbYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlT3OFghcA>? MXfJR|UxRDFizszN M2\KW|I1OzR4MUG2
MOLM-13 M3HIVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jnPVQ5KGh? Mn\3TWM2ODxzIN88US=> MUKyOFM1PjFzNh?=
OCI-AML2 NXXHSo1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnVN|NVPDhiaB?= NGr2bmZKSzVyPEGg{txO M{\DTFI1OzR4MUG2
Kasumi-1 M1mxWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PYZVQ5KGh? NXfiWo9RUUN3MEyxJO69VQ>? NIW4PFMzPDN2NkGxOi=>
KG-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVm0PEBp M2\kbWlEPTB:MTFOwG0> MkD5NlQ{PDZzMU[=
THP-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTNTpg1QCCq NEH1cZpKSzVyPEGg{txO NWDXOlVTOjR|NE[xNVY>
MOLM-14 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlOzOFghcA>? NXPKXHdGUUN3MEyxJO69VQ>? MnfpNlQ{PDZzMU[=
MOLM-13 NHrR[llCeG:ydH;0bYMhSXO|YYm= NXLSc3BOPTBibl2= M1zyOVI1KGh? NGS2bppCeG:ydH;zbZMhcW6mdXP0bY9v MkD2NlQ{PDZzMU[=
HSB NYL5d5V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjoOY8yOCEQvF2= M3z5XVQ5KGh? NHzZRYFFVVOR NETkN3ZKSzVyPUSuOFQ5KM7:TR?= MUGyOFM1Ojl2OB?=
MOLT4 NH;Lc3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\yOoxnOTBizszN M4TYNVQ5KGh? Mk[wSG1UVw>? MWLJR|UxRTRwMUW0JO69VQ>? MV:yOFM1Ojl2OB?=
SKW-3/KE-37 NU\JeZZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYSxNEDPxE1? MYK0PEBp MofJSG1UVw>? M3\JNmlEPTB;MD63NVIh|ryP MnXJNlQ{PDJ7NEi=
SUPT-11 M2fIdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHZNVAh|ryP MYW0PEBp MVLEUXNQ NG\YdZRKSzVyPUSuOFc{KM7:TR?= M4ex[lI1OzR{OUS4
JURKAT MnO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWexNEDPxE1? M4mxUFQ5KGh? MYfEUXNQ NWi5WYtzUUN3ME20Mlg6OyEQvF2= NEnuPIUzPDN2Mkm0PC=>
CCRF-CEM NYnxSYhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVqwSYttOTBizszN NYGw[HNZPDhiaB?= MYjEUXNQ NG\iPY1KSzVyPUGuN|YxKM7:TR?= M3zxSVI1OzR{OUS4
LOUCY MnLrRZBweHSxdHnjJGF{e2G7 NXn5Xo1mOiEQvF2= M2jkelQ5KGh? MnrlSG1UVw>? MXTBdI9xfG:|aYOgbY5lfWO2aX;u MXWyOFM1Ojl2OB?=

... 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
+ 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
+ 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
+ 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 2016 Phase 2
NCT02755597 Recruiting Relapsed/Refractory Multiple Myeloma AbbVie|Genentech, Inc. July 2016 Phase 3
NCT02640833 Withdrawn Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|Non-Hodgkin Lymphoma AbbVie|Infinity Pharmaceuticals, Inc. July 2016 Phase 1
NCT02756611 Recruiting Chronic Lymphocytic Leukemia AbbVie June 2016 Phase 3
NCT02758665 Not yet recruiting Leukemia, Lymphocytic, Chronic University of Ulm|German CLL Study Group|Roche Pharma AG|Janssen-Cilag Ltd. June 2016 Phase 2
NCT02677324 Recruiting Waldenstrom Macroglobulinemia Dana-Farber Cancer Institute|AbbVie April 2016 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