Venetoclax (ABT-199)

For research use only.

Catalog No.S8048 Synonyms: GDC-0199

356 publications

Venetoclax (ABT-199) Chemical Structure

CAS No. 1257044-40-8

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. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.

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Selleck's Venetoclax (ABT-199) has been cited by 356 publications

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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. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. 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 Mm\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuyNEBvVQ>? NFfRcFk4OiCq NUH3N4dKTE2VTx?= M4DvOmlvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 MUGyOVkyPjZ7OB?=
CS-THL1 NX7iVGV1SXCxcITveIlkKEG|c3H5 MmrxNlUhdk1? MYTEUXNQ NIfJV45KdmS3Y3XzJIFxd3C2b4Ppdy=> M1H4NlI2QTF4Nkm4
DoGKiT MoHhRZBweHSxdHnjJGF{e2G7 NEHXN2k2OCCwTR?= NXnObpFOTE2VTx?= NYfEbpFiUW6mdXPld{BieG:ydH;zbZM> NEDJSmEzPTlzNk[5PC=>
RS4-11 NXHodXB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\k[VczKGh? M{HyfGlEPTB;MD6wOFAzKM7:TR?= M3fpXFI2PjR7N{[4
NALM-6 M1XW[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzl[444OiCq MUPJR|UxRjNizszN MUOyOVY1QTd4OB?=
SU-DHL-6 MkPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PueFAvQCEQvF2= MojXTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NHzrbHIzPTV7MEiwNy=>
OCI-Ly19 MkPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fTdFEh|ryP MkC0TY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> MknZNlU2QTB6MEO=
SU-DHL-6 NFvNNFRHfW6ldHnvckBCe3OjeR?= M1e5RlAvPzVizszN NVrCRll4OThiaB?= MoewTY5kemWjc3XzJJBzdy2|dYL2bZZidCCycn;0[YlvKE2FTD2xJIV5eHKnc4Ppc44> NUPVRVFGOjV3OUC4NFM>
KCL22 NFzvZZBHfW6ldHnvckBCe3OjeR?= MmfNNkDPxE1? MlPFOFghcA>? NUPScG1RTE2VTx?= NIPPcldKdmO{ZXHz[ZMhTE6DIH\yZYdidWWwdHH0bY9v MYiyOVM{OzJ3Mh?=
LOUCY NHqydZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;ENVAh|ryP Mo\JOFghcA>? MlXDSG1UVw>? MlzTTWM2OD1yLkCxN|kh|ryP NV7tO4hlOjV|MEG3NFQ>
ALL-SIL Ml7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGxNEDPxE1? NXPiToJqPDhiaB?= NV3LN5hMTE2VTx?= MlKyTWM2OD1yLkG4NFMh|ryP M3W1RlI2OzBzN{C0
CUTLL1 MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrhUHMyOCEQvF2= MVu0PEBp NVnTdJM{TE2VTx?= M{jMdGlEPTB;MD6zPFI{KM7:TR?= M{DsWlI2OzBzN{C0
KOPTK1 NVLaWYJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3KwWFExKM7:TR?= MX:0PEBp MVzEUXNQ M2rWOGlEPTB;MD62OFMzKM7:TR?= MnLJNlU{ODF5MES=
DND-41 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLINVAh|ryP MnqzOFghcA>? M1npRmROW09? M125ZmlEPTB;MT65Olk2KM7:TR?= MWCyOVMxOTdyNB?=
PF-382 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjYNVAh|ryP MmnkOFghcA>? NGPjTXhFVVOR MkDwTWM2OD1{LkG4NlQh|ryP M{D1dVI2OzBzN{C0
KARPAS-45 NHjSbY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XLdFExKM7:TR?= NXTGfFFIPDhiaB?= MXLEUXNQ NYThUYFnUUN3ME2zMlIzOjVizszN NF7KWo0zPTNyMUewOC=>
PEER MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fWSlExKM7:TR?= NIjCOW41QCCq MnvtSG1UVw>? Ml;QTWM2OD12Lk[0NFMh|ryP M2HZe|I2OzBzN{C0
CX-1 NH\ZZohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jUU|ExOCEQvF2= M4fWT|czKGh? M37tN2lEPTB;Nj63JO69VQ>? M2P6PFI2OjB6OEiy
LS147T NGToflVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUSxNFAh|ryP MUW3NkBp M17XcWlEPTB;MkmuOUDPxE1? Mki5NlUzODh6OEK=
HL-60 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUm2dIhpPDhiaB?= MknlTWM2ODxzIN88US=> Mmr6NlQ{PDZzMU[=
MOLM-13 NEO1flZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:0PEBp M1jne2lEPTB:MTFOwG0> M2XDSVI1OzR4MUG2
OCI-AML2 NGTte|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjvOFghcA>? NXPD[FF6UUN3MEyxJO69VQ>? NE\yWG0zPDN2NkGxOi=>
Kasumi-1 M3LZWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfvOFghcA>? NEjOd2lKSzVyPEGg{txO MnXPNlQ{PDZzMU[=
KG-1 MlLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIW0TWc1QCCq Ml25TWM2ODxzIN88US=> NWjHeWlEOjR|NE[xNVY>
THP-1 NIHWTJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWO0PEBp MYrJR|UxRDFizszN NUe4coZ4OjR|NE[xNVY>
MOLM-14 M33Ud2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO0PEBp MX\JR|UxRDFizszN M1;Ze|I1OzR4MUG2
MOLM-13 MWnBdI9xfG:2aXOgRZN{[Xl? NXXESFRzPTBibl2= MV:yOEBp NUHDe25uSXCxcITvd4l{KGmwZIXjeIlwdg>? MoK1NlQ{PDZzMU[=
HSB MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVGydGVmOTBizszN NIDCZ241QCCq MnqySG1UVw>? MXzJR|UxRTRwNES4JO69VQ>? NXO4dWUzOjR|NEK5OFg>
MOLT4 NGHUSVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkn2NVAh|ryP M{DIe|Q5KGh? M17tfWROW09? NYPHclY4UUN3ME20MlE2PCEQvF2= Mmr0NlQ{PDJ7NEi=
SKW-3/KE-37 M1fLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfoNVAh|ryP Mof3OFghcA>? MXXEUXNQ NETpUWJKSzVyPUCuO|EzKM7:TR?= M2r6fVI1OzR{OUS4
SUPT-11 NHGzdJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPwZooyOCEQvF2= NXfYdIpRPDhiaB?= NET3PJFFVVOR NX\mPJpRUUN3ME20MlQ4OyEQvF2= NHixbYIzPDN2Mkm0PC=>
JURKAT NX7v[VNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37adFExKM7:TR?= MlXzOFghcA>? MWLEUXNQ MXTJR|UxRTRwOEmzJO69VQ>? MV2yOFM1Ojl2OB?=
CCRF-CEM M3nvT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKxNEDPxE1? MWC0PEBp NGS3SVVFVVOR M120W2lEPTB;MT6zOlAh|ryP MVKyOFM1Ojl2OB?=
LOUCY MV3BdI9xfG:2aXOgRZN{[Xl? M1HVc|Ih|ryP NUnFc3VyPDhiaB?= MUHEUXNQ NIjtZXBCeG:ydH;zbZMhcW6mdXP0bY9v MlnHNlQ{PDJ7NEi=

... 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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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)
  • 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 GDC-0199
Smiles CC1(CCC(=C(C1)C2=CC=C(C=C2)Cl)CN3CCN(CC3)C4=CC(=C(C=C4)C(=O)NS(=O)(=O)C5=CC(=C(C=C5)NCC6CCOCC6)[N+](=O)[O-])OC7=CN=C8C(=C7)C=CN8)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04298918 Recruiting Drug: Placebo|Drug: Venetoclax|Drug: Trastuzumab emtansine Breast Cancer Hoffmann-La Roche September 15 2020 Phase 1|Phase 2
NCT04284787 Not yet recruiting Drug: Azacitidine|Biological: Pembrolizumab|Drug: Venetoclax Acute Myeloid Leukemia|Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome|Secondary Acute Myeloid Leukemia National Cancer Institute (NCI) September 8 2020 Phase 2
NCT04501939 Not yet recruiting Drug: Cirmtuzumab|Drug: Venetoclax Chronic Lymphocytic Leukemia University of California San Diego|Oncternal Therapeutics Inc August 31 2020 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:

    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