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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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 MlHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfDVJUzOCCwTR?= M3LkZVczKGh? MljnSG1UVw>? MoLJTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> MYKyOVkyPjZ7OB?=
CS-THL1 MVrBdI9xfG:2aXOgRZN{[Xl? MkK4NlUhdk1? M3;2e2ROW09? M1juVGlv\HWlZYOgZZBweHSxc3nz NYX1VZB6OjV7MU[2PVg>
DoGKiT MmnYRZBweHSxdHnjJGF{e2G7 MoHZOVAhdk1? MV\EUXNQ MnjTTY5lfWOnczDhdI9xfG:|aYO= M1jBZ|I2QTF4Nkm4
RS4-11 NIP4d4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3lO|IhcA>? M4rWXWlEPTB;MD6wOFAzKM7:TR?= NFribZIzPTZ2OUe2PC=>
NALM-6 NXS2fZN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXS3NkBp NVfHSHdoUUN3ME6zJO69VQ>? MmmzNlU3PDl5Nki=
SU-DHL-6 MkfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDzVmUxNjhizszN NHfRZZRKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? M{T6dlI2PTlyOECz
OCI-Ly19 MkPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3v[HN{OSEQvF2= M2nlXWlvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 NFjQbIgzPTV7MEiwNy=>
SU-DHL-6 MmrySpVv[3Srb36gRZN{[Xl? NGW0dHcxNjd3IN88US=> NVjxPYNMOThiaB?= MYjJcoNz\WG|ZYOgdJJwNXO3co\peoFtKHC{b4TlbY4hVUOOLUGg[ZhxemW|c3nvci=> M37CO|I2PTlyOECz
KCL22 NGjtNpRHfW6ldHnvckBCe3OjeR?= M3PuXVIh|ryP MY[0PEBp MYXEUXNQ NIHGTmxKdmO{ZXHz[ZMhTE6DIH\yZYdidWWwdHH0bY9v NFTpfXEzPTN|M{K1Ni=>
LOUCY MlzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITYc3EyOCEQvF2= NICyWVQ1QCCq MXPEUXNQ MYjJR|UxRTBwMEGzPUDPxE1? NEfB[oozPTNyMUewOC=>
ALL-SIL NFyzdXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XPbVExKM7:TR?= M1nzTVQ5KGh? MWXEUXNQ MXHJR|UxRTBwMUiwN{DPxE1? MWOyOVMxOTdyNB?=
CUTLL1 M2PjNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDMNVAh|ryP NIn4eFM1QCCq NWjGVpR4TE2VTx?= MVLJR|UxRTBwM{iyN{DPxE1? M1T0O|I2OzBzN{C0
KOPTK1 MlnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HDWlExKM7:TR?= MWC0PEBp M2TSRmROW09? NETqN5FKSzVyPUCuOlQ{OiEQvF2= M2PUblI2OzBzN{C0
DND-41 MmPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuxNEDPxE1? MXu0PEBp M4rTbmROW09? MmXRTWM2OD1zLkm2PVUh|ryP NYXUeHdZOjV|MEG3NFQ>
PF-382 MmG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmxNEDPxE1? NF22Nmg1QCCq NH3EO5BFVVOR M4\iV2lEPTB;Mj6xPFI1KM7:TR?= MlX0NlU{ODF5MES=
KARPAS-45 NGSxOnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTHWWVTOTBizszN M{DNXVQ5KGh? NXv4RVFuTE2VTx?= NYHhUWk6UUN3ME2zMlIzOjVizszN MYiyOVMxOTdyNB?=
PEER MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYOxNEDPxE1? NEHWS4s1QCCq NYThb2tETE2VTx?= MoTPTWM2OD12Lk[0NFMh|ryP MWKyOVMxOTdyNB?=
CX-1 Mn;LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuxNFAh|ryP NVjh[2pvPzJiaB?= M{H4NmlEPTB;Nj63JO69VQ>? MmnqNlUzODh6OEK=
LS147T MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LsbFExOCEQvF2= NWSw[JpqPzJiaB?= NFXQ[3hKSzVyPUK5MlUh|ryP MojHNlUzODh6OEK=
HL-60 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\uSVQ5KGh? MmTPTWM2ODxzIN88US=> M4mybFI1OzR4MUG2
MOLM-13 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmH3OFghcA>? M3zWWGlEPTB:MTFOwG0> M3;ndFI1OzR4MUG2
OCI-AML2 MoXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIq4Rmg1QCCq MUfJR|UxRDFizszN Mnm4NlQ{PDZzMU[=
Kasumi-1 Mn3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\YUVQ5KGh? NHyyZYZKSzVyPEGg{txO MVuyOFM1PjFzNh?=
KG-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHNOFghcA>? NYjhSnVTUUN3MEyxJO69VQ>? M{fDblI1OzR4MUG2
THP-1 NEDpcG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTXOFghcA>? Mn6zTWM2ODxzIN88US=> M3To[|I1OzR4MUG2
MOLM-14 MmfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXThVZloPDhiaB?= NV\GUHo3UUN3MEyxJO69VQ>? NFPTO3ozPDN2NkGxOi=>
MOLM-13 NGXWSJFCeG:ydH;0bYMhSXO|YYm= NIXIUYc2OCCwTR?= MX6yOEBp MYfBdI9xfG:|aYOgbY5lfWO2aX;u MljjNlQ{PDZzMU[=
HSB NGXQ[25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETEN|UyOCEQvF2= NI\ofmE1QCCq NWHwNFQ3TE2VTx?= MUnJR|UxRTRwNES4JO69VQ>? MV2yOFM1Ojl2OB?=
MOLT4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUSxNEDPxE1? MXy0PEBp NFHlSW5FVVOR MmTUTWM2OD12LkG1OEDPxE1? NUTudI8yOjR|NEK5OFg>
SKW-3/KE-37 M3;KNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOxNEDPxE1? MUG0PEBp M3fjOGROW09? MWHJR|UxRTBwN{GyJO69VQ>? M4q2N|I1OzR{OUS4
SUPT-11 MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvRUXQyOCEQvF2= NU\RcmV[PDhiaB?= NF;EeYdFVVOR MYXJR|UxRTRwNEezJO69VQ>? NVLNbHF7OjR|NEK5OFg>
JURKAT NVTWflR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\FSlExKM7:TR?= MkLHOFghcA>? Ml:xSG1UVw>? MUTJR|UxRTRwOEmzJO69VQ>? NXuzfGtzOjR|NEK5OFg>
CCRF-CEM M4m0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYexNEDPxE1? NUjxdGhwPDhiaB?= NVLBb|NOTE2VTx?= M1znWWlEPTB;MT6zOlAh|ryP NIX4clkzPDN2Mkm0PC=>
LOUCY NFrYc4tCeG:ydH;0bYMhSXO|YYm= NULOTo9WOiEQvF2= MWm0PEBp MoHxSG1UVw>? NV\vRmNZSXCxcITvd4l{KGmwZIXjeIlwdg>? NWjrdlBVOjR|NEK5OFg>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Mcl-1 / Bcl-xl / Bcl-2 / Bak / NOXA / Bim; 

PubMed: 30663221     


A549 cells were treated with Ibr-7, ABT-199 or a combination for 2 or 4 h. Total RNA was extracted from A549 cells to undergo RT-qPCR assay.

PARP / Cleaved PARP / Caspase 3 / Cleaved caspase3 / p-S6(Ser236/236); 

PubMed: 30663221     


A549 cells were treated with Ibr-7, ABT-199 or a combination for 24 h before western blotting assay. 

30663221
Growth inhibition assay
Cell death; 

PubMed: 28714472     


The indicated cell lines, treated with 2 μM doxorubicin±1 or 2 μM ABT-199, were quantified by annexin-V staining at 24 h for H2171 and H446 or at 48 h for H196 and SW1271 (mean±s.d., n=3). 

Cell viability; 

PubMed: 29876007     


TNBC cells were cultured with the indicated doses of ABT-199 (μM) for 48 h. 

28714472 29876007
Immunofluorescence
Bcl-2 / Mcl-1; 

PubMed: 28767232     


HEK293T cells cotransfected with the plasmids. Upon transfection, DMSO carrier control, 0.5 μM ABT-199, 10 μM A1210477, or a combination of both 0.5 μM ABT-199 and 10 μM A1210447 were added to the cells. After 30 h, the cells were analyzed for GFP and RFP expression by fluorescence microscopy.

28767232
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