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.

Price Stock Quantity  
USD 680 In stock
USD 270 In stock
USD 970 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

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

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

Validation & Quality Control

Customer Product Validation(2)

Quality Control & MSDS

Bcl-2 Inhibitors with Unique Features

  • Pan Bcl-2 Inhibitor

    ABT-263 (Navitoclax) Bcl-xL, Ki≤ 0.5 nM; Bcl-2, Ki≤ 1 nM; Bcl-w, Ki≤ 1 nM.

  • Bcl-2 Inhibitor in Clinical Trial

    Obatoclax Mesylate (GX15-070) Phase II for leukemia, lymphoma, myelofibrosis, and mastocytosis.

  • Newest Bcl-2 Family Activator

    BAM7 Direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.

  • Classic Bcl-2 Inhibitor

    ABT-737 BH3-mimetic inhibitor, Bcl-xL, EC50=78.7 nM; Bcl-2, EC50=30.3 nM; Bcl-w, EC50=197.8 nM.

Product Information

  • Compare Bcl-2 Inhibitors
    Compare Bcl-2 Products
  • 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-THL1NUXmdnVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1zRbFIxKG6PMl3yO|IhcA>?MV3EUXNQNEL4NI9KdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>?NXLwT3J1OjV7MU[2PVg>
CS-THL1MYfBdI9xfG:2aXOgRZN{[Xl?M3XPfVI2KG6PMm\6SG1UVw>?Ml7XTY5lfWOnczDhdI9xfG:|aYO=MoW2NlU6OTZ4OUi=
DoGKiTNWLOXnRzSXCxcITveIlkKEG|c3H5NELwNlE2OCCwTR?=NXzmb4dKTE2VTx?=NHvNboVKdmS3Y3XzJIFxd3C2b4Ppdy=>MVSyOVkyPjZ7OB?=
RS4-11M4Sxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NF\DXnc4OiCqMknzTWM2OD1yLkC0NFIh|ryPMlntNlU3PDl5Nki=
NALM-6NIHTbFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3rIelczKGh?NYixfVdJUUN3ME6zJO69VQ>?NYjTW|NiOjV4NEm3Olg>
SU-DHL-6NG\DTWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MnzBNE45KM7:TR?=M1qxZWlvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6MoXONlU2QTB6MEO=
OCI-Ly19M1;He2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3TncVEh|ryPMkDUTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk>M3rOZVI2PTlyOECz
SU-DHL-6NGrYcllHfW6ldHnvckBCe3OjeR?=M1jQVFAvPzVizszNMly0NVghcA>?MY\JcoNz\WG|ZYOgdJJwNXO3co\peoFtKHC{b4TlbY4hVUOOLUGg[ZhxemW|c3nvci=>Mn3oNlU2QTB6MEO=
KCL22MnjWSpVv[3Srb36gRZN{[Xl?NVLIVVk1OiEQvF2=MkToOFghcA>?MYDEUXNQMn\QTY5kemWjc3XzJGRPSSCocnHnZY1mdnSjdHnvci=>NEGyXGkzPTN|M{K1Ni=>
LOUCYNVPrU3I3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXnQb3BjOTBizszNNX[4R|d2PDhiaB?=MkDPSG1UVw>?MVPJR|UxRTBwMEGzPUDPxE1?NH3LRY0zPTNyMUewOC=>
ALL-SILNEjtZ3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NWjGSmxROTBizszNNVzGb|NoPDhiaB?=MYnEUXNQNWPkdmgzUUN3ME2wMlE5ODNizszNM4PxZVI2OzBzN{C0
CUTLL1Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M4rzU|ExKM7:TR?=MkC1OFghcA>?MnvXSG1UVw>?NXjydZh1UUN3ME2wMlM5OjNizszNNH64RYMzPTNyMUewOC=>
KOPTK1MnnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MoWwNVAh|ryPM3Ww[VQ5KGh?NWnDXoNKTE2VTx?=MkLXTWM2OD1yLk[0N|Ih|ryPNVXJ[I9UOjV|MEG3NFQ>
DND-41NIXOWoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MU[xNEDPxE1?M3fUNFQ5KGh?Ml3sSG1UVw>?NVHOZphSUUN3ME2xMlk3QTVizszNMlL2NlU{ODF5MES=
PF-382NYPleGZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVf5XnEyOTBizszNNIjnb|g1QCCqMorJSG1UVw>?NUHHdI83UUN3ME2yMlE5OjRizszNMX:yOVMxOTdyNB?=
KARPAS-45M1;IOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NIH2cYMyOCEQvF2=NYfJXGdZPDhiaB?=M2\Z[WROW09?MX3JR|UxRTNwMkKyOUDPxE1?NXzF[49pOjV|MEG3NFQ>
PEERNIrGVYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M4PXOVExKM7:TR?=NYPhbGdJPDhiaB?=NFfOcoVFVVORM{jIeWlEPTB;ND62OFA{KM7:TR?=NW\HWmcxOjV|MEG3NFQ>
CX-1NFvRTolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MVKxNFAh|ryPMljWO|IhcA>?MmXrTWM2OD14Lkeg{txOM2nYclI2OjB6OEiy
LS147TMlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NImzUnEyODBizszNMYi3NkBpM2XUSmlEPTB;MkmuOUDPxE1?NF;BNoUzPTJyOEi4Ni=>
HL-60MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3[zVVQ5KGh?NEXQd3BKSzVyPEGg{txOMmjUNlQ{PDZzMU[=
MOLM-13MnexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NF63S|E1QCCqNUWw[pZ1UUN3MEyxJO69VQ>?M{DJSlI1OzR4MUG2
OCI-AML2MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NH3LXIs1QCCqMmK5TWM2ODxzIN88US=>MVOyOFM1PjFzNh?=
Kasumi-1NYq4bHM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXjDS2lNPDhiaB?=Mo\zTWM2ODxzIN88US=>NHzR[HUzPDN2NkGxOi=>
KG-1M4j1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NX\rT4w{PDhiaB?=MkSwTWM2ODxzIN88US=>NYrUXpR3OjR|NE[xNVY>
THP-1NWLzZm91T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFfvPGE1QCCqNELYPG1KSzVyPEGg{txONF;jWYYzPDN2NkGxOi=>
MOLM-14NYPwbI5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2W3d|Q5KGh?NELseFJKSzVyPEGg{txONFLqfoszPDN2NkGxOi=>
MOLM-13MmTHRZBweHSxdHnjJGF{e2G7MmnTOVAhdk1?MmXLNlQhcA>?MXXBdI9xfG:|aYOgbY5lfWO2aX;uNEXjZ2YzPDN2NkGxOi=>
HSBMnzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mo[2NVAh|ryPMlLOOFghcA>?MWXEUXNQMlG2TWM2OD12LkS0PEDPxE1?NYL6VoszOjR|NEK5OFg>
MOLT4NX:3bYN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NGfueIsyOCEQvF2=NWrsd3hXPDhiaB?=NX\Gboc{TE2VTx?=NY[5WmJpUUN3ME20MlE2PCEQvF2=MXeyOFM1Ojl2OB?=
SKW-3/KE-37NYDVWWg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{O2WlExKM7:TR?=Ml\EOFghcA>?NIfZOY9FVVORMoHMTWM2OD1yLkexNkDPxE1?MWKyOFM1Ojl2OB?=
SUPT-11NH\MUm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Mn\QNVAh|ryPM2\qeFQ5KGh?NIDYUVdFVVORNX\pToZTUUN3ME20MlQ4OyEQvF2=MmjYNlQ{PDJ7NEi=
JURKATMYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NHTlZlMyOCEQvF2=NHLvOpg1QCCqMne0SG1UVw>?NXT5XmFHUUN3ME20Mlg6OyEQvF2=MVmyOFM1Ojl2OB?=
CCRF-CEMMYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NH[0W2oyOCEQvF2=MnvMOFghcA>?MkfaSG1UVw>?MU\JR|UxRTFwM{[wJO69VQ>?MYOyOFM1Ojl2OB?=
LOUCYNYLIb4RTSXCxcITveIlkKEG|c3H5MWOyJO69VQ>?M2Owd|Q5KGh?NEPMN4ZFVVORMlnRRZBweHSxc3nzJIlv\HWldHnvci=>MYOyOFM1Ojl2OB?=

... 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 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02756897 Not yet recruiting Leukemia|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma M.D. Anderson Cancer Center|AbbVie August 2016 Phase 2
NCT02755597 Not yet recruiting Relapsed/Refractory Multiple Myeloma AbbVie|Genentech, Inc. 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
NCT02756611 Not yet recruiting Chronic Lymphocytic Leukemia AbbVie May 2016 Phase 3
NCT02677324 Recruiting Waldenstrom Macroglobulinemia Dana-Farber Cancer Institute|AbbVie April 2016 Phase 2

view more

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 warmed (115.14 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 20 mg/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)-

Customer Product Validation (2)


Click to enlarge
Rating
Source Mol Oncol 2014 10.1016/j.molonc.2014.09.008. Venetoclax (ABT-199, GDC-0199) purchased from Selleck
Method Western blot
Cell Lines THP-1 cells
Concentrations 0.5, 1, 2 uM
Incubation Time 8 h
Results To determine if Bcl-2 plays a role, we used the Bcl-2 selective BH3 mimetic ABT-199 to treat THP-1 cells, alone or in combination with cytarabine for 8 h. Western blotting and densitometry measurements indicate that ABT-199 significantly increased cytarabine-induced γH2AX levels.

Click to enlarge
Rating
Source J Biol Chem 2014 289(23), 16190-9. Venetoclax (ABT-199, GDC-0199) purchased from Selleck
Method PLA2 Activity Assay
Cell Lines CLL cells
Concentrations 0-10000 nM
Incubation Time 6 h
Results The BCL2-specific inhibitor, ABT-199 obviously inhibited proliferation of CLL cells, which had effected on a low concentration.

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.

* Indicates a Required Field

Related Bcl-2 Products

  • A-1210477

    A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.

  • MI-773 (SAR405838)

    MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

  • ABT-263 (Navitoclax)

    ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.

  • ABT-737

    ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.

  • UMI-77

    UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.

  • Obatoclax Mesylate (GX15-070)

    Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.

    Features:Potential 1st-in-class small molecule antagonist of Bcl-2 designed to inhibit all relevant Bcl-2 family members, including Mcl-1.

  • TW-37

    TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.

  • Sabutoclax

    Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.

  • AT101

    AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. Phase 2.

Recently Viewed Items

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
Contact Us