Venetoclax (ABT-199)

For research use only.

Catalog No.S8048 Synonyms: GDC-0199

386 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 386 publications

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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. 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 Mn20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYGyNEBvVQ>? M2e4b|czKGh? M3H5RWROW09? NGjIbGxKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MkHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7MU[2PVgoRjJ3OUG2Olk5RC:jPh?=
CS-THL1 NX7rPItSSXCxcITveIlkKEG|c3H5 NVr6OIwyOjVibl2= MWjEUXNQ MnXOTY5lfWOnczDhdI9xfG:|aYO= NED0blE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUmxOlY6QCd-MkW5NVY3QTh:L3G+
DoGKiT NHL0OXNCeG:ydH;0bYMhSXO|YYm= NIe4TXk2OCCwTR?= NEHhc5FFVVOR Mk\BTY5lfWOnczDhdI9xfG:|aYO= NXXKRnhCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5NVY3QThpPkK1PVE3Pjl6PD;hQi=>
RS4-11 M4DUfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUC3NkBp M{DYOGlEPTB;MD6wOFAzKM7:TR?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ2OUe2PEc,OjV4NEm3Olg9N2F-
NALM-6 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnraO|IhcA>? MVXJR|UxRjNizszN M3fXb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkS5O|Y5Lz5{NU[0PVc3QDxxYU6=
SU-DHL-6 M{KxS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33XXlAvQCEQvF2= NIPuPIpKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7MEiwN{c,OjV3OUC4NFM9N2F-
OCI-Ly19 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjhR|MyKM7:TR?= MmDtTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7MEiwN{c,OjV3OUC4NFM9N2F-
SU-DHL-6 MUfGeY5kfGmxbjDBd5NigQ>? NFm3WJExNjd3IN88US=> NX;lSWREOThiaB?= MWjJcoNz\WG|ZYOgdJJwNXO3co\peoFtKHC{b4TlbY4hVUOOLUGg[ZhxemW|c3nvci=> NIrTNnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW5NFgxOyd-MkW1PVA5ODN:L3G+
KCL22 MmnySpVv[3Srb36gRZN{[Xl? MnT0NkDPxE1? NITPPVk1QCCq MV7EUXNQ MVjJcoNz\WG|ZYOgSG5CKG[{YXfhcYVvfGG2aX;u NYjYO5V7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|MzPTJpPkK1N|M{OjV{PD;hQi=>
LOUCY M3WwS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXTNVAh|ryP MVK0PEBp M{PaO2ROW09? MnnOTWM2OD1yLkCxN|kh|ryP MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
ALL-SIL MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWWxNEDPxE1? M1XtUVQ5KGh? MYjEUXNQ NWXyeZZEUUN3ME2wMlE5ODNizszN MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
CUTLL1 NYr6WIZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfy[nE2OTBizszN NYTPSGxmPDhiaB?= MmDRSG1UVw>? NFH4eppKSzVyPUCuN|gzOyEQvF2= M3K5cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{CxO|A1Lz5{NUOwNVcxPDxxYU6=
KOPTK1 NUL6UppET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXpNVAh|ryP NXXqb25DPDhiaB?= MWTEUXNQ NVHWfYpkUUN3ME2wMlY1OzJizszN MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
DND-41 NEHRNFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\mNVAh|ryP NVn4N|FDPDhiaB?= NX7CUXBKTE2VTx?= NXTKXJd1UUN3ME2xMlk3QTVizszN NIjJcpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
PF-382 NVPhNWtTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nxOFExKM7:TR?= MU[0PEBp NI\1cpVFVVOR NGfUS|RKSzVyPUKuNVgzPCEQvF2= NIPqdIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
KARPAS-45 M2PXeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWOxNEDPxE1? NITxW|M1QCCq NU\zVZFyTE2VTx?= NYT3doVmUUN3ME2zMlIzOjVizszN M{jsfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{CxO|A1Lz5{NUOwNVcxPDxxYU6=
PEER NUTyTI1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7Qfm9jOTBizszN MX60PEBp NXTudXpDTE2VTx?= M4qw[2lEPTB;ND62OFA{KM7:TR?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
CX-1 NUnxUYpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknvNVAxKM7:TR?= MlzNO|IhcA>? M3rBUWlEPTB;Nj63JO69VQ>? NHfle4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKwPFg5Oid-MkWyNFg5QDJ:L3G+
LS147T NICzU5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP6fHVtOTByIN88US=> M1PjclczKGh? NV33UFF1UUN3ME2yPU42KM7:TR?= MnfOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MEi4PFIoRjJ3MkC4PFgzRC:jPh?=
HL-60 Mnf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVm0PEBp M2rOSmlEPTB:MTFOwG0> MoLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NE[xNVYoRjJ2M{S2NVE3RC:jPh?=
MOLM-13 MnPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXiZ4c1QCCq MoX3TWM2ODxzIN88US=> NWTZUohPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
OCI-AML2 Moj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVy0PEBp MV\JR|UxRDFizszN M3jWTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
Kasumi-1 M1nSPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TGRVQ5KGh? M3rPbWlEPTB:MTFOwG0> MlrPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NE[xNVYoRjJ2M{S2NVE3RC:jPh?=
KG-1 NYnpOnRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfnOFghcA>? M4TKOGlEPTB:MTFOwG0> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
THP-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfZe2RvPDhiaB?= NXPPVIhzUUN3MEyxJO69VQ>? MnHMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NE[xNVYoRjJ2M{S2NVE3RC:jPh?=
MOLM-14 NIS5VJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVe0PEBp MUPJR|UxRDFizszN NFThfVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
MOLM-13 NITI[GZCeG:ydH;0bYMhSXO|YYm= MXG1NEBvVQ>? Mli4NlQhcA>? NF2zVYxCeG:ydH;zbZMhcW6mdXP0bY9v NYXrUVVERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
HSB NFvuPGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEK5fnUyOCEQvF2= M3LvV|Q5KGh? MYHEUXNQ NGH2OYxKSzVyPUSuOFQ5KM7:TR?= NH3pemM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
MOLT4 NEm0T5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TNTFExKM7:TR?= Ml;qOFghcA>? M{nuc2ROW09? M1LOVGlEPTB;ND6xOVQh|ryP NUHYSXhSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
SKW-3/KE-37 NYLwOlJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\jRVExKM7:TR?= NX;SfW1PPDhiaB?= NIrWfnNFVVOR NIT5XGtKSzVyPUCuO|EzKM7:TR?= M3vwWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
SUPT-11 NVvT[2hoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\FZlExKM7:TR?= NECwOlk1QCCq Mn\3SG1UVw>? MWnJR|UxRTRwNEezJO69VQ>? MlPBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEK5OFgoRjJ2M{SyPVQ5RC:jPh?=
JURKAT MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWOxNEDPxE1? NH\TbZE1QCCq M{[0e2ROW09? MoX2TWM2OD12Lki5N{DPxE1? NV7XdldmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
CCRF-CEM NYLSW45uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\kNVAh|ryP NFTaZpc1QCCq Ml3USG1UVw>? MVrJR|UxRTFwM{[wJO69VQ>? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2Mkm0PEc,OjR|NEK5OFg9N2F-
LOUCY MnvJRZBweHSxdHnjJGF{e2G7 MYSyJO69VQ>? MX20PEBp M3HIcGROW09? M4jn[mFxd3C2b4Ppd{BqdmS3Y4Tpc44> NEfRc3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
RS4:11 M1nL[WN6fG:2b4jpZ4l1gSCjc4PhfS=> NWXiRXhNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzNpPkK5OFA4QTd|PD;hQi=>
RS4:11 MoDJUXRUKGG|c3H5 NImzNGI4OiCq NXzCSIdLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyO|g{OzNpPkOwNlc5OzN|PD;hQi=>
RS4:11 NYTUc|I5VVSVIHHzd4F6 NFvzXmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEmyOlI1Pyd-Mki5NlYzPDd:L3G+
Toledo NFXuVHhOXFNiYYPzZZk> MmjQO|IhcA>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ5OEOzN{c,OzB{N{izN|M9N2F-
NCI60 M2P6Z3NTSiCjc4PhfS=> NU\2NGxkPDhiaB?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
RS4:11 NYLGe|VVVVSWIHHzd4F6 NGf2c48zPCCq M3ixSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEWzNVM2Lz5{OUS1N|E{PTxxYU6=
melanoma NH;vbHZUWkJiYYPzZZk> Ml;vOFghcA>? NHXYZZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
leukemia M{fBdnNTSiCjc4PhfS=> M2PuVlQ5KGh? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
renal cancer M1nLO3NTSiCjc4PhfS=> NWPDRWFjPDhiaB?= NFfEXlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
non-small cell lung cancer MXrTVmIh[XO|YYm= NGn1XnE1QCCq MonLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
breast cancer M{mz[XNTSiCjc4PhfS=> NFzseWw1QCCq NXLTeFc1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
colon cancer MWTTVmIh[XO|YYm= NHvwdYc1QCCq NInDfpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
ovarian cancer MkPhV3JDKGG|c3H5 NV\Lc5N{PDhiaB?= NUi1VYJVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
CNS cancer NIrsS41UWkJiYYPzZZk> M3:4XVQ5KGh? NFHUTYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
prostate cancer MnHjV3JDKGG|c3H5 NH;sbpM1QCCq NVrjd|d1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
Remb1 NIDFZ3ZOXFRiYYPzZZk> MUSyOEBp M2DjTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEWzNVM2Lz5{OUS1N|E{PTxxYU6=

... 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]
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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]
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  • 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]
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  • 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04572763 Not yet recruiting Drug: Copanlisib|Drug: Venetoclax Diffuse Large B Cell Lymphoma|Relapsed Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma Dana-Farber Cancer Institute|AbbVie|Bayer September 2021 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.

Handling Instructions

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

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

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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