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 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke2NlAhdk1? NYriUoUzPzJiaB?= NIjuUpRFVVOR MnLBTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> MnewNlU6OTZ4OUi=
CS-THL1 M4HpW2Fxd3C2b4TpZ{BCe3OjeR?= MVSyOUBvVQ>? M3LoV2ROW09? MVXJcoR2[2W|IHHwc5B1d3Orcx?= NVr4XoUyOjV7MU[2PVg>
DoGKiT M3[ydmFxd3C2b4TpZ{BCe3OjeR?= MV21NEBvVQ>? NILtXllFVVOR M13WcWlv\HWlZYOgZZBweHSxc3nz M2XlV|I2QTF4Nkm4
RS4-11 NHHCS29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnKO|IhcA>? MVrJR|UxRTBwMESwNkDPxE1? NF3jTJEzPTZ2OUe2PC=>
NALM-6 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWS3NkBp MnTqTWM2OD5|IN88US=> NH3lcZkzPTZ2OUe2PC=>
SU-DHL-6 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrQXYQxNjhizszN NHnrRmVKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MoHlNlU2QTB6MEO=
OCI-Ly19 NH[yWlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPLSmd2OSEQvF2= MnK5TY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> M4LB[FI2PTlyOECz
SU-DHL-6 M3TRXGZ2dmO2aX;uJGF{e2G7 MlP2NE44PSEQvF2= MYGxPEBp MlP5TY5kemWjc3XzJJBzdy2|dYL2bZZidCCycn;0[YlvKE2FTD2xJIV5eHKnc4Ppc44> NYHwVndDOjV3OUC4NFM>
KCL22 M4npXGZ2dmO2aX;uJGF{e2G7 MlLQNkDPxE1? MXi0PEBp NEXDfYZFVVOR NEDi[GZKdmO{ZXHz[ZMhTE6DIH\yZYdidWWwdHH0bY9v M{SwVVI2OzN|MkWy
LOUCY MorsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkO2NVAh|ryP MnPoOFghcA>? NEOzN5NFVVOR MWPJR|UxRTBwMEGzPUDPxE1? MVuyOVMxOTdyNB?=
ALL-SIL NUfGVJl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvWNVAh|ryP MYm0PEBp MkPJSG1UVw>? NX:1UGpVUUN3ME2wMlE5ODNizszN M3rxOlI2OzBzN{C0
CUTLL1 NGruZ5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPvNVAh|ryP NFe0RVk1QCCq NEG1OpdFVVOR NF\iZpVKSzVyPUCuN|gzOyEQvF2= M4H2[lI2OzBzN{C0
KOPTK1 NH\o[XNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ezfVExKM7:TR?= Mn3ROFghcA>? M3LjZmROW09? NFHpd2lKSzVyPUCuOlQ{OiEQvF2= NUXOS|QxOjV|MEG3NFQ>
DND-41 NWjXdXhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnroNVAh|ryP MmrmOFghcA>? MkjmSG1UVw>? NHXlZ|BKSzVyPUGuPVY6PSEQvF2= NVTFSo9pOjV|MEG3NFQ>
PF-382 M1HueWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFftTVcyOCEQvF2= NXvO[o46PDhiaB?= NHrtSIdFVVOR Mk\6TWM2OD1{LkG4NlQh|ryP Ml3HNlU{ODF5MES=
KARPAS-45 NUX5cpZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\yNGc6OTBizszN NWLRe4c2PDhiaB?= NXTGU5BHTE2VTx?= NEjDSFRKSzVyPUOuNlIzPSEQvF2= MUmyOVMxOTdyNB?=
PEER NVv3THBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfQSlFPOTBizszN MUC0PEBp MXXEUXNQ MVjJR|UxRTRwNkSwN{DPxE1? NUfzXWY{OjV|MEG3NFQ>
CX-1 NFfz[2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrGNVAxKM7:TR?= M3HmbFczKGh? NULCU202UUN3ME22Mlch|ryP NX7De2cyOjV{MEi4PFI>
LS147T MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYixNFAh|ryP Mm\QO|IhcA>? NWLmO4hZUUN3ME2yPU42KM7:TR?= Ml7iNlUzODh6OEK=
HL-60 NV65N4ZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmxcYtDPDhiaB?= MX3JR|UxRDFizszN M2HGPVI1OzR4MUG2
MOLM-13 M{\Gcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTIOFghcA>? M{nzemlEPTB:MTFOwG0> Mn7UNlQ{PDZzMU[=
OCI-AML2 NFnle|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHXT5ZJPDhiaB?= NWnT[29{UUN3MEyxJO69VQ>? M{HuNFI1OzR4MUG2
Kasumi-1 NVrpbVZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTuOFghcA>? M4TjPGlEPTB:MTFOwG0> NWPh[Zh3OjR|NE[xNVY>
KG-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fNVVQ5KGh? NUfac5dTUUN3MEyxJO69VQ>? MmfXNlQ{PDZzMU[=
THP-1 NVHn[2JST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfaPI41QCCq NVXLeY17UUN3MEyxJO69VQ>? MUmyOFM1PjFzNh?=
MOLM-14 Ml3PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfyW|VGPDhiaB?= NUP0XFRbUUN3MEyxJO69VQ>? MYGyOFM1PjFzNh?=
MOLM-13 NX3F[2ViSXCxcITveIlkKEG|c3H5 MXS1NEBvVQ>? MVqyOEBp M2nzV2Fxd3C2b4Ppd{BqdmS3Y4Tpc44> MnnYNlQ{PDZzMU[=
HSB M2rNSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGxNEDPxE1? MoDZOFghcA>? M2PX[WROW09? MorWTWM2OD12LkS0PEDPxE1? MW[yOFM1Ojl2OB?=
MOLT4 Mkj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjjR20yOCEQvF2= NGXlWGE1QCCq NVTOVHNCTE2VTx?= M4XsV2lEPTB;ND6xOVQh|ryP NFPH[nYzPDN2Mkm0PC=>
SKW-3/KE-37 NFHpN4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKxNEDPxE1? MX60PEBp MUTEUXNQ NEjZfHBKSzVyPUCuO|EzKM7:TR?= NFTwUIQzPDN2Mkm0PC=>
SUPT-11 Mle4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkWzNVAh|ryP MWO0PEBp MVXEUXNQ NGW2d21KSzVyPUSuOFc{KM7:TR?= NIHINHczPDN2Mkm0PC=>
JURKAT NHHrUnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXOxNEDPxE1? NFTFcFY1QCCq MlPwSG1UVw>? MnrnTWM2OD12Lki5N{DPxE1? NWXVOIxTOjR|NEK5OFg>
CCRF-CEM MlHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHhbJVTOTBizszN NYfPc2diPDhiaB?= M{P2N2ROW09? NUXwWYFbUUN3ME2xMlM3OCEQvF2= MmnvNlQ{PDJ7NEi=
LOUCY NXv0WpFXSXCxcITveIlkKEG|c3H5 NFHQeHozKM7:TR?= NYnjWFlRPDhiaB?= NEKwe4VFVVOR NFO3O|ZCeG:ydH;zbZMhcW6mdXP0bY9v NYmybGtmOjR|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