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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Cited by 25 Publications

6 Customer Reviews

  • (C) OCI-AML2 cells were cultured for 1 day with or without the indicated doses of CB-839 and ABT-199; apoptosis was evaluated based on Annexin V staining. (D) MOLM-14 cells were cultured for 1 day with or without the indicated doses of CB-839 and ABT-199; apoptosis was evaluated based on Annexin-V staining. Histograms show data that are representative of 3 independent experiments. The response of the combination was compared with its single agents against the widely used Loewe model for drug-with-itself dose additivity using Chalice software26 and presented as an isobologram. *P < .05, **P < .01, ***P < .001.

    Blood, 2015, 126(11):1346-56. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

    (b) MV4-11 cells were treated in vitro with ABT-199 (0.01, 0.1, 1 or 10 μM) with or without BL-8040 (20 μM) for 24 h in 1% FCS RPMI medium. The percentage of dead cells (PI+ cells) was evaluated by FACS. (c) miR-15a and miR-16-1 transfections were performed using Lipofectamine 2000 transfection reagent. At 72 h post-transfection, cells were stained with Annexin-V and PI. FACS plots and numerical data of % cells are shown. The results are expressed as the mean±s.d. and were analyzed using Student’s t-test (*P ⩽0.05 compared with control).

    Leukemia, 2017, 31(11):2336-2346. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

  • MDA-MB-468 cells were treated with BETd-246 (50 nM), BM-1197 (250 nM), ABT-263 (250 nM), ABT-199 (250 nM) or A-1155463 (250 nM) as indicated for 24 h for Annexin V-PI apoptosis analysis. Data are the mean ± SEM (n=3).

    Cancer Res, 2017, 77(9):2476-2487. Venetoclax (ABT-199, GDC-0199) purchased from Selleck.

    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.

  • C33A cells were treated with ABC294640 (5 μmol/L), together with/out ABT-737 (200 nM) or GDC-0199 (200 nM), cells were further cultured for indicated time, cell growth (MTT assay, (A) and apoptosis (Histone DNA ELISA assay, (B) were tested.

    Oncotarget, 2017, 9(2):2384-2394. 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 NHvJToFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4OzWFIxKG6P NGHid2g4OiCq NX;EWJptTE2VTx?= NVXxPWlSUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? NUjvelF2OjV7MU[2PVg>
CS-THL1 NETGXnpCeG:ydH;0bYMhSXO|YYm= M2m4V|I2KG6P MlviSG1UVw>? MWDJcoR2[2W|IHHwc5B1d3Orcx?= M4HPUVI2QTF4Nkm4
DoGKiT MlzORZBweHSxdHnjJGF{e2G7 NVXvUYNtPTBibl2= NG\aclZFVVOR MlSyTY5lfWOnczDhdI9xfG:|aYO= Ml\xNlU6OTZ4OUi=
RS4-11 M1Prcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUGzeXo3PzJiaB?= NHLNRmxKSzVyPUCuNFQxOiEQvF2= MYCyOVY1QTd4OB?=
NALM-6 NWjDWWZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rsfFczKGh? MWfJR|UxRjNizszN M2nOe|I2PjR7N{[4
SU-DHL-6 MlHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmm3NE45KM7:TR?= Mm[wTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NUTGfXNZOjV3OUC4NFM>
OCI-Ly19 MoO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGxJO69VQ>? MU\Jcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> MkP0NlU2QTB6MEO=
SU-DHL-6 NIfIVnVHfW6ldHnvckBCe3OjeR?= NFX5eIcxNjd3IN88US=> NWjmRmdlOThiaB?= M2nxNWlv[3KnYYPld{Bxem9vc4Xyeol3[WxicILveIVqdiCPQ1ytNUBmgHC{ZYPzbY9v NEPaSGkzPTV7MEiwNy=>
KCL22 MoLDSpVv[3Srb36gRZN{[Xl? M4\PNVIh|ryP NXHUbnRSPDhiaB?= NWPmb|FFTE2VTx?= MofFTY5kemWjc3XzJGRPSSCocnHnZY1mdnSjdHnvci=> NI\FUpAzPTN|M{K1Ni=>
LOUCY NVLxUWlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:xNEDPxE1? MX20PEBp MUHEUXNQ NUnXT|F[UUN3ME2wMlAyOzlizszN MXeyOVMxOTdyNB?=
ALL-SIL MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUCxNEDPxE1? MVe0PEBp M1zNXWROW09? MXXJR|UxRTBwMUiwN{DPxE1? MWSyOVMxOTdyNB?=
CUTLL1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DIN|ExKM7:TR?= NVvDfXF4PDhiaB?= M2LXTWROW09? NV3S[Gw{UUN3ME2wMlM5OjNizszN MUiyOVMxOTdyNB?=
KOPTK1 MoK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHpNVAh|ryP MVy0PEBp M3L0O2ROW09? MWjJR|UxRTBwNkSzNkDPxE1? Mm\NNlU{ODF5MES=
DND-41 Mn2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPhNVAh|ryP Mkj2OFghcA>? NYjmTml7TE2VTx?= MWDJR|UxRTFwOU[5OUDPxE1? MXqyOVMxOTdyNB?=
PF-382 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{i2S|ExKM7:TR?= NGjpV4M1QCCq MlLxSG1UVw>? MmH3TWM2OD1{LkG4NlQh|ryP NFHidGIzPTNyMUewOC=>
KARPAS-45 NWDoTnNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLXNVAh|ryP MYW0PEBp M4jOTmROW09? M3\vbGlEPTB;Mz6yNlI2KM7:TR?= NFLIWo0zPTNyMUewOC=>
PEER NIfIZ5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;PNGwyOCEQvF2= NV;iOHo1PDhiaB?= MVnEUXNQ NXjkeJg5UUN3ME20MlY1ODNizszN M2rm[lI2OzBzN{C0
CX-1 NYPT[YhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVuxNFAh|ryP MWC3NkBp NV3HTFI1UUN3ME22Mlch|ryP MknvNlUzODh6OEK=
LS147T NHr3WW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:xNFAh|ryP NIfrfIs4OiCq NEPMcpRKSzVyPUK5MlUh|ryP MkLsNlUzODh6OEK=
HL-60 MmXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3WWHBxPDhiaB?= MXfJR|UxRDFizszN MY[yOFM1PjFzNh?=
MOLM-13 NEXoWZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojqOFghcA>? MkDxTWM2ODxzIN88US=> NYftfXk4OjR|NE[xNVY>
OCI-AML2 M4HqVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUi0PEBp NGPpNlFKSzVyPEGg{txO NW\vOVIxOjR|NE[xNVY>
Kasumi-1 NIGwfHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDSfmg1QCCq MkXaTWM2ODxzIN88US=> MX:yOFM1PjFzNh?=
KG-1 NFfGS4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfaUph5PDhiaB?= M3z6dmlEPTB:MTFOwG0> M3XiSVI1OzR4MUG2
THP-1 MlHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkG5OFghcA>? NVfjRlZNUUN3MEyxJO69VQ>? NYfLOHVyOjR|NE[xNVY>
MOLM-14 NGjTRWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHR[W5HPDhiaB?= NYjpWog1UUN3MEyxJO69VQ>? NH7MUYszPDN2NkGxOi=>
MOLM-13 MV\BdI9xfG:2aXOgRZN{[Xl? NGO2c2E2OCCwTR?= MW[yOEBp M4jzdGFxd3C2b4Ppd{BqdmS3Y4Tpc44> NXzzPXJbOjR|NE[xNVY>
HSB MmrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoK0NVAh|ryP MmD2OFghcA>? MXHEUXNQ MYXJR|UxRTRwNES4JO69VQ>? M2DXO|I1OzR{OUS4
MOLT4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XYdFExKM7:TR?= NF7RXHo1QCCq M1HEVmROW09? NUnyUWozUUN3ME20MlE2PCEQvF2= M3S2Z|I1OzR{OUS4
SKW-3/KE-37 M4DWZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVyxNEDPxE1? MWi0PEBp NEL2bZlFVVOR MWHJR|UxRTBwN{GyJO69VQ>? NIrqPIczPDN2Mkm0PC=>
SUPT-11 Ml\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlG3NVAh|ryP NWjzcoVLPDhiaB?= M{TLeWROW09? Ml[wTWM2OD12LkS3N{DPxE1? MUCyOFM1Ojl2OB?=
JURKAT NWHEfZZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\yNVAh|ryP NUH5SYNFPDhiaB?= MVrEUXNQ MXzJR|UxRTRwOEmzJO69VQ>? M4rWSFI1OzR{OUS4
CCRF-CEM M4TZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrtS|EyOCEQvF2= MWS0PEBp M2DCOmROW09? M{LVPWlEPTB;MT6zOlAh|ryP M3H1UFI1OzR{OUS4
LOUCY NXHKe45kSXCxcITveIlkKEG|c3H5 Mm[1NkDPxE1? M3ThUFQ5KGh? M3O0NGROW09? NYm1R2pZSXCxcITvd4l{KGmwZIXjeIlwdg>? NUC3Zlg3OjR|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(Data is from Selleck tests instead of citations):
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
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03872180 Not yet recruiting CCND1 Positive|Mantle Cell Lymphoma|t(11;14) Positive Emory University|Genentech Inc. March 1 2020 Phase 2
NCT03872180 Not yet recruiting CCND1 Positive|Mantle Cell Lymphoma|t(11;14) Positive Emory University|Genentech Inc. March 1 2020 Phase 2
NCT03884972 Not yet recruiting Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) December 1 2019 Phase 1
NCT03884972 Not yet recruiting Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) December 1 2019 Phase 1
NCT03868722 Not yet recruiting CLL Rigshospitalet Denmark|Stichting Hemato-Oncologie voor Volwassenen Nederland|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Karolinska Institutet August 1 2019 Phase 2|Phase 3
NCT03868722 Not yet recruiting CLL Rigshospitalet Denmark|Stichting Hemato-Oncologie voor Volwassenen Nederland|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Karolinska Institutet August 1 2019 Phase 2|Phase 3

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Could you please offer some advice on the half-life of the drug ?

  • Answer:

    According to the reference (https://www.ncbi.nlm.nih.gov/pubmed/24212376), the half-life of ABT-199 in dogs is 12.9 hr.

  • Question 2:

    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