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
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

3 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.

    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 Ml2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlr2NlAhdk1? M1PtcVczKGh? Ml7TSG1UVw>? MVHJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> MYiyOVkyPjZ7OB?=
CS-THL1 NIflUWxCeG:ydH;0bYMhSXO|YYm= NID6SXMzPSCwTR?= NH;V[IVFVVOR Mn3FTY5lfWOnczDhdI9xfG:|aYO= NHnFZY0zPTlzNk[5PC=>
DoGKiT MWPBdI9xfG:2aXOgRZN{[Xl? NVjpfYE4PTBibl2= MVjEUXNQ M{DCdWlv\HWlZYOgZZBweHSxc3nz NWTFO4ZDOjV7MU[2PVg>
RS4-11 M{nUVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PJ[lczKGh? NHTLOXBKSzVyPUCuNFQxOiEQvF2= MV[yOVY1QTd4OB?=
NALM-6 M1rMTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXUO|IhcA>? NFv5OW9KSzVyPkOg{txO MVGyOVY1QTd4OB?=
SU-DHL-6 M{LsW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4T1TlAvQCEQvF2= NVjFOnRPUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? NX\LSploOjV3OUC4NFM>
OCI-Ly19 Mnu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVmxJO69VQ>? NVj5cZdyUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? NYjFV2c2OjV3OUC4NFM>
SU-DHL-6 MmX5SpVv[3Srb36gRZN{[Xl? NIjNXZQxNjd3IN88US=> MoH3NVghcA>? MX7JcoNz\WG|ZYOgdJJwNXO3co\peoFtKHC{b4TlbY4hVUOOLUGg[ZhxemW|c3nvci=> M4q5elI2PTlyOECz
KCL22 MmjOSpVv[3Srb36gRZN{[Xl? NF\TVY4zKM7:TR?= MkT5OFghcA>? NHfGXo9FVVOR MmnRTY5kemWjc3XzJGRPSSCocnHnZY1mdnSjdHnvci=> MnPtNlU{OzN{NUK=
LOUCY MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf0NVAh|ryP MnPZOFghcA>? MXXEUXNQ NWnYV3p5UUN3ME2wMlAyOzlizszN MViyOVMxOTdyNB?=
ALL-SIL NXrETpRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrSOnBXOTBizszN M2XTdVQ5KGh? M{XtNGROW09? MXzJR|UxRTBwMUiwN{DPxE1? MWmyOVMxOTdyNB?=
CUTLL1 M1v6PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3H1XlExKM7:TR?= NV;LNJFHPDhiaB?= MWrEUXNQ MkLLTWM2OD1yLkO4NlMh|ryP M2S4R|I2OzBzN{C0
KOPTK1 NUn4fo1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXixNEDPxE1? M3nMeVQ5KGh? MofYSG1UVw>? MWLJR|UxRTBwNkSzNkDPxE1? MWmyOVMxOTdyNB?=
DND-41 M4PBUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\jVnMyOCEQvF2= MmrQOFghcA>? NXnOZ49ZTE2VTx?= NYHUeZV2UUN3ME2xMlk3QTVizszN NUPGd2M3OjV|MEG3NFQ>
PF-382 M2DURWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWexNEDPxE1? MYW0PEBp MWjEUXNQ M{LU[2lEPTB;Mj6xPFI1KM7:TR?= Moi0NlU{ODF5MES=
KARPAS-45 NEnHZ3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIraUW8yOCEQvF2= M{nBbFQ5KGh? Mn\nSG1UVw>? NV:zXGV[UUN3ME2zMlIzOjVizszN M2PLO|I2OzBzN{C0
PEER NE[1UItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDLNJkyOCEQvF2= M17MVFQ5KGh? NUTm[|Q2TE2VTx?= NHzOV4RKSzVyPUSuOlQxOyEQvF2= NWP2ZpRiOjV|MEG3NFQ>
CX-1 M3XTOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\TcVZIOTByIN88US=> NXLnbllMPzJiaB?= MUHJR|UxRTZwNzFOwG0> MX:yOVIxQDh6Mh?=
LS147T M1LrSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml35NVAxKM7:TR?= MX23NkBp NGLDboRKSzVyPUK5MlUh|ryP MoXNNlUzODh6OEK=
HL-60 NXXD[2tVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[xPXU1QCCq NHLqfpNKSzVyPEGg{txO MlXsNlQ{PDZzMU[=
MOLM-13 MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[0PEBp MWHJR|UxRDFizszN MW[yOFM1PjFzNh?=
OCI-AML2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHnOFghcA>? NYnWcGlnUUN3MEyxJO69VQ>? MUWyOFM1PjFzNh?=
Kasumi-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPuOFghcA>? M13EXWlEPTB:MTFOwG0> NF7pbIkzPDN2NkGxOi=>
KG-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnlOFghcA>? M2LDXmlEPTB:MTFOwG0> NHHnfYYzPDN2NkGxOi=>
THP-1 NUjqb4hOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWO0PEBp NXTaZnlRUUN3MEyxJO69VQ>? NYLrW3lnOjR|NE[xNVY>
MOLM-14 M1[w[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfSc3Y1QCCq NUf3NFJrUUN3MEyxJO69VQ>? NFu5T4IzPDN2NkGxOi=>
MOLM-13 NHrKb29CeG:ydH;0bYMhSXO|YYm= MnPEOVAhdk1? M3Ltb|I1KGh? NHfHVIRCeG:ydH;zbZMhcW6mdXP0bY9v MYWyOFM1PjFzNh?=
HSB NUTneIRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3f0N|ExKM7:TR?= MmO2OFghcA>? NHyxZVNFVVOR M13MWmlEPTB;ND60OFgh|ryP MorENlQ{PDJ7NEi=
MOLT4 NV7Hb4dpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTLboYyOCEQvF2= NYP6ZW1ZPDhiaB?= MoLESG1UVw>? NUf2XmRmUUN3ME20MlE2PCEQvF2= MnfFNlQ{PDJ7NEi=
SKW-3/KE-37 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH1NVAh|ryP M3qydVQ5KGh? NHz0XWpFVVOR M3fWc2lEPTB;MD63NVIh|ryP MV[yOFM1Ojl2OB?=
SUPT-11 M3fr[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoG3NVAh|ryP NWiyTY9SPDhiaB?= M3PUcGROW09? NVfWdIxjUUN3ME20MlQ4OyEQvF2= M{Dr[VI1OzR{OUS4
JURKAT Ml\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[wNVAh|ryP NGLibIY1QCCq MVLEUXNQ MnrDTWM2OD12Lki5N{DPxE1? MlfINlQ{PDJ7NEi=
CCRF-CEM MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;kb|lSOTBizszN MnfoOFghcA>? MULEUXNQ M4e2b2lEPTB;MT6zOlAh|ryP NIjSdWgzPDN2Mkm0PC=>
LOUCY M37Wd2Fxd3C2b4TpZ{BCe3OjeR?= M{faeFIh|ryP NYXNRmkzPDhiaB?= NXHDcodqTE2VTx?= NWL6[VlWSXCxcITvd4l{KGmwZIXjeIlwdg>? Ml3BNlQ{PDJ7NEi=

... 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03583424 Recruiting Hematopoietic Cell Transplantation Recipient|Recurrent Diffuse Large B-Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Non-Hodgkin Lymphoma|Refractory Diffuse Large B-Cell Lymphoma|Refractory Follicular Lymphoma|Refractory Marginal Zone Lymphoma|Refractory Non-Hodgkin Lymphoma|Refractory Transformed Indolent Non-Hodgkin Lymphoma Ohio State University Comprehensive Cancer Center|National Cancer Institute (NCI) July 9 2018 Phase 1|Phase 2
NCT03379051 Recruiting Chronic Lymphocytic Leukemia TG Therapeutics Inc.|James P. Wilmot Cancer Center April 9 2018 Phase 1|Phase 2
NCT03415035 Recruiting Chronic Lymphocytic Leukemia (CLL) AbbVie March 9 2018 --
NCT03223610 Recruiting Lymphoma|Non-Hodgkin Lymphoma|Diffuse Large B-Cell Lymphoma|Burkitt Lymphoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) February 9 2018 Phase 1
NCT03236857 Recruiting Malignancies|Acute Lymphoblastic Leukemia (ALL)|Acute Myeloid Leukemia (AML)|Non-Hodgkin''s Lymphoma|Neuroblastoma AbbVie|Roche-Genentech November 9 2017 Phase 1
NCT02611323 Recruiting Non-Hodgkin''s Lymphoma Hoffmann-La Roche March 9 2016 Phase 1

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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.

Bcl-2 Signaling Pathway Map

Bcl-2 Inhibitors with Unique Features

Related Bcl-2 Products

Tags: buy Venetoclax (ABT-199, GDC-0199) | Venetoclax (ABT-199, GDC-0199) supplier | purchase Venetoclax (ABT-199, GDC-0199) | Venetoclax (ABT-199, GDC-0199) cost | Venetoclax (ABT-199, GDC-0199) manufacturer | order Venetoclax (ABT-199, GDC-0199) | Venetoclax (ABT-199, GDC-0199) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID