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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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

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 NUfsTo9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PTeVIxKG6P MXO3NkBp MmrsSG1UVw>? Ml\RTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NGXMVpUzPTlzNk[5PC=>
CS-THL1 MmX0RZBweHSxdHnjJGF{e2G7 MVSyOUBvVQ>? MV;EUXNQ NXP4fXlSUW6mdXPld{BieG:ydH;zbZM> NIDWTI4zPTlzNk[5PC=>
DoGKiT MYXBdI9xfG:2aXOgRZN{[Xl? MlzOOVAhdk1? NWrLU4tlTE2VTx?= Mo\pTY5lfWOnczDhdI9xfG:|aYO= M{\JcVI2QTF4Nkm4
RS4-11 M3LF[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4ryWVczKGh? NYixe4U4UUN3ME2wMlA1ODJizszN NIDKSoQzPTZ2OUe2PC=>
NALM-6 M2jObGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTDO|IhcA>? NFq3TnpKSzVyPkOg{txO MW[yOVY1QTd4OB?=
SU-DHL-6 M3\DOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jmd|AvQCEQvF2= M4nnfGlvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 MoqzNlU2QTB6MEO=
OCI-Ly19 MoT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTXNUDPxE1? MlnXTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> MmHrNlU2QTB6MEO=
SU-DHL-6 M4\JPWZ2dmO2aX;uJGF{e2G7 MYKwMlc2KM7:TR?= NHvmd3EyQCCq NYnodoxsUW6lcnXhd4V{KHC{bz3zeZJ3cX[jbDDwdo91\WmwIF3DUE0yKGW6cILld5Nqd25? NY\NXIp4OjV3OUC4NFM>
KCL22 M17EZ2Z2dmO2aX;uJGF{e2G7 M1zN[|Ih|ryP Ml\IOFghcA>? MWHEUXNQ NW\Q[|dLUW6lcnXhd4V{KESQQTDmdoFo[W2nboTheIlwdg>? M2DlS|I2OzN|MkWy
LOUCY NGn2[5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfVNVAh|ryP NF\Ebpc1QCCq MYPEUXNQ NXSwSlBXUUN3ME2wMlAyOzlizszN NGToPHAzPTNyMUewOC=>
ALL-SIL MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXGxNEDPxE1? Mm\COFghcA>? MWfEUXNQ Ml;STWM2OD1yLkG4NFMh|ryP NVO1SGU4OjV|MEG3NFQ>
CUTLL1 NVPSe5hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXexNEDPxE1? NX62OmVTPDhiaB?= M2j0XmROW09? Mo\qTWM2OD1yLkO4NlMh|ryP NXXaeXB1OjV|MEG3NFQ>
KOPTK1 Mne3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjObHpTOTBizszN MnzBOFghcA>? MWHEUXNQ NVPhWW9ZUUN3ME2wMlY1OzJizszN MWmyOVMxOTdyNB?=
DND-41 NXfQZmpbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkmzNVAh|ryP M3zEXFQ5KGh? MmnWSG1UVw>? NGTGPYRKSzVyPUGuPVY6PSEQvF2= NIrPNG0zPTNyMUewOC=>
PF-382 MmXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37TS|ExKM7:TR?= MlXKOFghcA>? M3z1XGROW09? Mom1TWM2OD1{LkG4NlQh|ryP MYWyOVMxOTdyNB?=
KARPAS-45 NH;ufHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV2xNEDPxE1? M3PoSFQ5KGh? NWXvWFM1TE2VTx?= NWjkcpAyUUN3ME2zMlIzOjVizszN MXKyOVMxOTdyNB?=
PEER MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmxNEDPxE1? MoPnOFghcA>? MlLxSG1UVw>? NYjyZ|NLUUN3ME20MlY1ODNizszN MlW4NlU{ODF5MES=
CX-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTRNVAxKM7:TR?= MWK3NkBp M1nKT2lEPTB;Nj63JO69VQ>? NIiyTlEzPTJyOEi4Ni=>
LS147T NULRUoxQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvv[GE3OTByIN88US=> MmHEO|IhcA>? NIPZ[2RKSzVyPUK5MlUh|ryP M33Y[lI2OjB6OEiy
HL-60 M2TRdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHBcIc1QCCq Mn32TWM2ODxzIN88US=> NI\VZ5QzPDN2NkGxOi=>
MOLM-13 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[0PEBp M{T1PGlEPTB:MTFOwG0> NITHbokzPDN2NkGxOi=>
OCI-AML2 NI[zO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmryOFghcA>? MYPJR|UxRDFizszN M4PXdlI1OzR4MUG2
Kasumi-1 MmLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrGOFghcA>? NVnWeJRuUUN3MEyxJO69VQ>? NUPJbJM5OjR|NE[xNVY>
KG-1 NFLGN4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvrOFghcA>? M3G5UmlEPTB:MTFOwG0> NH3k[GczPDN2NkGxOi=>
THP-1 M1\VZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHvV5Q1QCCq M3HDNWlEPTB:MTFOwG0> NWfyN4M5OjR|NE[xNVY>
MOLM-14 MoLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrxXno1QCCq MoHqTWM2ODxzIN88US=> MmnmNlQ{PDZzMU[=
MOLM-13 NIL6PIhCeG:ydH;0bYMhSXO|YYm= MmPWOVAhdk1? MWiyOEBp MoDoRZBweHSxc3nzJIlv\HWldHnvci=> NIjUeIUzPDN2NkGxOi=>
HSB Mk[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfDU5ZKOTBizszN M{LzZVQ5KGh? NHizT49FVVOR MWLJR|UxRTRwNES4JO69VQ>? NGfaSpczPDN2Mkm0PC=>
MOLT4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYW2e|V{OTBizszN NYDqWY1[PDhiaB?= M1z6ZmROW09? NF7jZY9KSzVyPUSuNVU1KM7:TR?= MVWyOFM1Ojl2OB?=
SKW-3/KE-37 NYj6b3dET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml65NVAh|ryP NWTwSIdpPDhiaB?= NHPCV5JFVVOR M3rndWlEPTB;MD63NVIh|ryP NIHXS|gzPDN2Mkm0PC=>
SUPT-11 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVexNEDPxE1? NHjNS4w1QCCq MlfkSG1UVw>? NVqydlBkUUN3ME20MlQ4OyEQvF2= M3ToblI1OzR{OUS4
JURKAT NIG2SFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmxNEDPxE1? NHXsO|A1QCCq NW\ld2RRTE2VTx?= NIDaT41KSzVyPUSuPFk{KM7:TR?= NGj0XHAzPDN2Mkm0PC=>
CCRF-CEM M2LT[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7rOGMyOCEQvF2= NVHt[2ZyPDhiaB?= MkjWSG1UVw>? MXjJR|UxRTFwM{[wJO69VQ>? MnHvNlQ{PDJ7NEi=
LOUCY MYrBdI9xfG:2aXOgRZN{[Xl? MV:yJO69VQ>? MXu0PEBp NWf6enRwTE2VTx?= Mnf3RZBweHSxc3nzJIlv\HWldHnvci=> MkHUNlQ{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 individually and in order:
5% DMSO+50% PEG 300+5% Tween 80+ddH2O
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
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 7, 2016 Phase 2
NCT03036904 Not yet recruiting Diffuse Large B-Cell Lymphoma|High Grade B-Cell Lymphoma Weill Medical College of Cornell University|Genentech, Inc.|Massachusetts General Hospital|M.D. Anderson Cancer Center February 6, 2017 Phase 1
NCT02951117 Not yet recruiting Multiple Myeloma AbbVie May 2017 Phase 1
NCT02966756 Not yet recruiting Chronic Lymphocytic Leukemia (CLL) AbbVie|Genentech/Roche April 2017 Phase 2
NCT02966782 Not yet recruiting Myelodysplastic Syndromes (MDS) AbbVie|Genentech, Inc. March 2017 Phase 1
NCT03045328 Not yet recruiting Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma Steven E. Coutre|Stanford University March 2017 Phase 1|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