Venetoclax (ABT-199, GDC-0199)

Catalog No.S8048

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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Venetoclax (ABT-199, GDC-0199) Chemical Structure

Venetoclax (ABT-199, GDC-0199) Chemical Structure
Molecular Weight: 868.44

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Product Information

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  • Research Area
  • Inhibition Profile

Product Description

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.
Targets Bcl-2 [1]
(Cell-free assay)
Bcl-xL [1]
(Cell-free assay)
Bcl-w [1]
(Cell-free assay)
Mcl-1 [1]
(Cell-free assay)
IC50 <0.01 nM(Ki) 48 nM(Ki) 245 nM(Ki) >444 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
CS-THL1MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2jjVVIxKG6PNWLFeINxPzJiaB?=NVzXPWk5TE2VTx?=NFjpXXpKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>?MX6yOVkyPjZ7OB?=
CS-THL1MVTBdI9xfG:2aXOgRZN{[Xl?NVryNIdtOjVibl2=MVzEUXNQM1nEe2lv\HWlZYOgZZBweHSxc3nzMlrhNlU6OTZ4OUi=
DoGKiTNIXnR2JCeG:ydH;0bYMhSXO|YYm=MlfQOVAhdk1?MoftSG1UVw>?MVrJcoR2[2W|IHHwc5B1d3Orcx?=NUXsfZNZOjV7MU[2PVg>
RS4-11NEj3PWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MYC3NkBpM4O2bGlEPTB;MD6wOFAzKM7:TR?=NFHTNZEzPTZ2OUe2PC=>
NALM-6M4XVSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NF21b4w4OiCqM3vVTmlEPTB-MzFOwG0>M4XkXVI2PjR7N{[4
SU-DHL-6M17CRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4rn[|AvQCEQvF2=NXKzW4xlUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl?NXzVSmRpOjV3OUC4NFM>
OCI-Ly19NXq3eGg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NX25WIFSOSEQvF2=Mn3nTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk>MYeyOVU6ODhyMx?=
SU-DHL-6NFPncGVHfW6ldHnvckBCe3OjeR?=NXfEUHdHOC55NTFOwG0>NIXlelUyQCCqMn3JTY5kemWjc3XzJJBzdy2|dYL2bZZidCCycn;0[YlvKE2FTD2xJIV5eHKnc4Ppc44>M{S2W|I2PTlyOECz
KCL22M2m0N2Z2dmO2aX;uJGF{e2G7MYKyJO69VQ>?NV7pfWNYPDhiaB?=MYnEUXNQMnHnTY5kemWjc3XzJGRPSSCocnHnZY1mdnSjdHnvci=>MX:yOVM{OzJ3Mh?=
LOUCYMUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MWGxNEDPxE1?NYDmVGVbPDhiaB?=MY\EUXNQMXHJR|UxRTBwMEGzPUDPxE1?NHj0epAzPTNyMUewOC=>
ALL-SILMnrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MXmxNEDPxE1?NEDC[W81QCCqM4LEWGROW09?NEHVcJNKSzVyPUCuNVgxOyEQvF2=MYeyOVMxOTdyNB?=
CUTLL1Mo\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MV:xNEDPxE1?M3TnPVQ5KGh?NVHINZZNTE2VTx?=NFLVOYdKSzVyPUCuN|gzOyEQvF2=M1T0dlI2OzBzN{C0
KOPTK1Mm[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M{HKZlExKM7:TR?=NWDPWnl1PDhiaB?=M4HaSGROW09?NIG4ZVFKSzVyPUCuOlQ{OiEQvF2=NF3oeYUzPTNyMUewOC=>
DND-41MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGfaOYsyOCEQvF2=MVS0PEBpNILtSINFVVORMoTkTWM2OD1zLkm2PVUh|ryPM1HwUVI2OzBzN{C0
PF-382NYWxNXNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MWSxNEDPxE1?M4nufFQ5KGh?M3e4UGROW09?MnXITWM2OD1{LkG4NlQh|ryPMnLoNlU{ODF5MES=
KARPAS-45MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mlq1NVAh|ryPNGfYWW01QCCqNEHGc4hFVVORNXLkRYR6UUN3ME2zMlIzOjVizszNMkP2NlU{ODF5MES=
PEERMorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MnHFNVAh|ryPM1PVe|Q5KGh?MYjEUXNQNFjDXZdKSzVyPUSuOlQxOyEQvF2=MmTONlU{ODF5MES=
CX-1Mn36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYTLdYJrOTByIN88US=>NWTONY5jPzJiaB?=Mkj0TWM2OD14Lkeg{txOMlXzNlUzODh6OEK=
LS147TMnXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIHvS4EyODBizszNNVvycmttPzJiaB?=MYPJR|UxRTJ7LkWg{txOMUiyOVIxQDh6Mh?=
HL-60NYDpcGt[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVm0V2Y{PDhiaB?=Ml3mTWM2ODxzIN88US=>NH;udIgzPDN2NkGxOi=>
MOLM-13M{nwVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MX60PEBpMknxTWM2ODxzIN88US=>MYCyOFM1PjFzNh?=
OCI-AML2NVzkcG83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mk[3OFghcA>?NIDEZ4VKSzVyPEGg{txOMU[yOFM1PjFzNh?=
Kasumi-1MkKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1z2XVQ5KGh?NX60bpdDUUN3MEyxJO69VQ>?MV:yOFM1PjFzNh?=
KG-1MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2fYSVQ5KGh?M{PTZ2lEPTB:MTFOwG0>NWrVOZk2OjR|NE[xNVY>
THP-1MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NULvbYNKPDhiaB?=MnrkTWM2ODxzIN88US=>MojrNlQ{PDZzMU[=
MOLM-14NF;BO3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFvHO2w1QCCqMULJR|UxRDFizszNMWmyOFM1PjFzNh?=
MOLM-13MmTJRZBweHSxdHnjJGF{e2G7MnrmOVAhdk1?NUPE[INtOjRiaB?=NHPQN2RCeG:ydH;zbZMhcW6mdXP0bY9vM4HscVI1OzR4MUG2
HSBNWjnNldVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NGTNVHIyOCEQvF2=MnmyOFghcA>?M{PiNGROW09?NHTVZpJKSzVyPUSuOFQ5KM7:TR?=M2XJNFI1OzR{OUS4
MOLT4M3\LPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHzocYUyOCEQvF2=MYS0PEBpNF[1XYZFVVORM2LHV2lEPTB;ND6xOVQh|ryPNE\xcmMzPDN2Mkm0PC=>
SKW-3/KE-37MoryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmLPNVAh|ryPMVq0PEBpNIHZdGhFVVORM{nLVWlEPTB;MD63NVIh|ryPNXnI[m5FOjR|NEK5OFg>
SUPT-11Ml61S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYL2RoNUOTBizszNNFKwfVc1QCCqNXX3N4tPTE2VTx?=M4nk[mlEPTB;ND60O|Mh|ryPNF;BNlMzPDN2Mkm0PC=>
JURKATMoX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmLSNVAh|ryPNE\J[Xc1QCCqM17BSGROW09?M{HOe2lEPTB;ND64PVMh|ryPNHi0VmkzPDN2Mkm0PC=>
CCRF-CEMMXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MmrHNVAh|ryPNHWzdFI1QCCqM3j3PGROW09?M{DucmlEPTB;MT6zOlAh|ryPMVqyOFM1Ojl2OB?=
LOUCYM3HwdGFxd3C2b4TpZ{BCe3OjeR?=Mk\BNkDPxE1?NEPWN4M1QCCqNFywS4FFVVORMXnBdI9xfG:|aYOgbY5lfWO2aX;uNHSxfIQzPDN2Mkm0PC=>

... 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]
Features Re-engineered version of ABT-263 (Navitoclax).

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [1]

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.

Animal Study: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Souers AJ, et al. Nat Med, 2013, 19(2), 202-208.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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 2016 Phase 2
NCT02755597 Recruiting Relapsed/Refractory Multiple Myeloma AbbVie|Genentech, Inc. July 2016 Phase 3
NCT02640833 Withdrawn Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|Non-Hodgkin Lymphoma AbbVie|Infinity Pharmaceuticals, Inc. July 2016 Phase 1
NCT02756611 Recruiting Chronic Lymphocytic Leukemia AbbVie June 2016 Phase 3
NCT02758665 Not yet recruiting Leukemia, Lymphocytic, Chronic University of Ulm|German CLL Study Group|Roche Pharma AG|  ...more University of Ulm|German CLL Study Group|Roche Pharma AG|Janssen-Cilag Ltd. June 2016 Phase 2

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Chemical Information

Download Venetoclax (ABT-199, GDC-0199) SDF
Molecular Weight (MW) 868.44
Formula

C45H50ClN7O7S

CAS No. 1257044-40-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL warming (115.14 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 5% DMSO+50% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name Benzamide, 4-[4-[[2-(4-chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-

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.

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.

Tel: +1-832-582-8158 Ext:3

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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