Venetoclax (ABT-199)

For research use only.

Catalog No.S8048 Synonyms: GDC-0199

399 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 399 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 M4Swfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fzUlIxKG6P NUT2SYlbPzJiaB?= MonGSG1UVw>? MXvJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTlzNk[5PEc,OjV7MU[2PVg9N2F-
CS-THL1 NX3a[nlFSXCxcITveIlkKEG|c3H5 NWLEdmRQOjVibl2= NGHTdG1FVVOR NEXNS5pKdmS3Y3XzJIFxd3C2b4Ppdy=> MoTWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7MU[2PVgoRjJ3OUG2Olk5RC:jPh?=
DoGKiT MX7BdI9xfG:2aXOgRZN{[Xl? NUDZTHFTPTBibl2= MlvFSG1UVw>? NHXsWWpKdmS3Y3XzJIFxd3C2b4Ppdy=> NG\xSpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUmxOlY6QCd-MkW5NVY3QTh:L3G+
RS4-11 M4PEVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnlcnFPPzJiaB?= MYDJR|UxRTBwMESwNkDPxE1? M4LkZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkS5O|Y5Lz5{NU[0PVc3QDxxYU6=
NALM-6 NYDOPW95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVG3NkBp MlvBTWM2OD5|IN88US=> NUfpSpNqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OFk4PjhpPkK1OlQ6PzZ6PD;hQi=>
SU-DHL-6 M13wRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW0NE45KM7:TR?= NXnqXpZQUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7MEiwN{c,OjV3OUC4NFM9N2F-
OCI-Ly19 NVj4SldWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[xJO69VQ>? MlHoTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> MkXQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUC4NFMoRjJ3NUmwPFA{RC:jPh?=
SU-DHL-6 M1rxNWZ2dmO2aX;uJGF{e2G7 M2n6TFAvPzVizszN NEfpT2MyQCCq M2HF[2lv[3KnYYPld{Bxem9vc4Xyeol3[WxicILveIVqdiCPQ1ytNUBmgHC{ZYPzbY9v NHjjNFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW5NFgxOyd-MkW1PVA5ODN:L3G+
KCL22 MVjGeY5kfGmxbjDBd5NigQ>? MoDYNkDPxE1? NVjBUllyPDhiaB?= MXjEUXNQ M1\wfWlv[3KnYYPld{BFVkFiZoLh[4Fu\W62YYTpc44> MnLCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{OyOVIoRjJ3M{OzNlUzRC:jPh?=
LOUCY NWToOnUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXS4UZNxOTBizszN MWO0PEBp NWS5eGZwTE2VTx?= Mo\VTWM2OD1yLkCxN|kh|ryP MmPMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
ALL-SIL MoLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnnNVAh|ryP NVHRW3ByPDhiaB?= NFjRWWtFVVOR NW\EVoV4UUN3ME2wMlE5ODNizszN NGLiPIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
CUTLL1 MnX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33aXlExKM7:TR?= NHfwcWQ1QCCq M3zvR2ROW09? MYjJR|UxRTBwM{iyN{DPxE1? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
KOPTK1 M{C5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWGxNEDPxE1? NX\SZ5hQPDhiaB?= MVfEUXNQ M{\MSmlEPTB;MD62OFMzKM7:TR?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
DND-41 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HrUVExKM7:TR?= MoTEOFghcA>? NYezeJJwTE2VTx?= MXrJR|UxRTFwOU[5OUDPxE1? MkDKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
PF-382 NY\ROJRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVixNEDPxE1? MkP0OFghcA>? MknGSG1UVw>? NXni[Yc5UUN3ME2yMlE5OjRizszN NEnPfGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
KARPAS-45 M3vtR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXENVAh|ryP MVm0PEBp MoHWSG1UVw>? NXmydnZPUUN3ME2zMlIzOjVizszN Mke1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
PEER NUjQPVdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlH0NVAh|ryP MkjGOFghcA>? MorkSG1UVw>? MnWxTWM2OD12Lk[0NFMh|ryP NEO4eJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
CX-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXUbWcyODBizszN M4nTSFczKGh? Mk\ETWM2OD14Lkeg{txO M3\XTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkC4PFgzLz5{NUKwPFg5OjxxYU6=
LS147T M4n5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkD3NVAxKM7:TR?= M3Tab|czKGh? NEnrRoVKSzVyPUK5MlUh|ryP M3T4[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkC4PFgzLz5{NUKwPFg5OjxxYU6=
HL-60 MmT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TyNVQ5KGh? NXPHbYp1UUN3MEyxJO69VQ>? NIeybXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
MOLM-13 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWe0PEBp M3i2SWlEPTB:MTFOwG0> NILjWmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
OCI-AML2 NXPWNXJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXi5PIVTPDhiaB?= NGX4NWVKSzVyPEGg{txO NFjkc3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
Kasumi-1 MmjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnMR5I1QCCq M{nRVGlEPTB:MTFOwG0> M1S0TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
KG-1 Mm\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfudFh1PDhiaB?= NVLpdGZ4UUN3MEyxJO69VQ>? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
THP-1 MluxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmS0OFghcA>? NHOwXW1KSzVyPEGg{txO MmnmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NE[xNVYoRjJ2M{S2NVE3RC:jPh?=
MOLM-14 NIHwXolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWi0PEBp NGLrPVZKSzVyPEGg{txO NW\JVZZCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
MOLM-13 M4j6bGFxd3C2b4TpZ{BCe3OjeR?= M4TVXlUxKG6P MXyyOEBp NFvGZnRCeG:ydH;zbZMhcW6mdXP0bY9v NXz3WJNDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
HSB MoK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Tte|ExKM7:TR?= NFnVR4I1QCCq M2\COmROW09? MnjMTWM2OD12LkS0PEDPxE1? NVWzXJRGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
MOLT4 NXq2flBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzFNVAh|ryP MXq0PEBp M2S1e2ROW09? M3ryNmlEPTB;ND6xOVQh|ryP NV;JSVRiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
SKW-3/KE-37 M37HfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOxNEDPxE1? MX60PEBp NUfIXW96TE2VTx?= M4rmN2lEPTB;MD63NVIh|ryP NWjJd2tbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
SUPT-11 M1XwTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzBOHRQOTBizszN NHv6RXc1QCCq MVTEUXNQ M2nYTWlEPTB;ND60O|Mh|ryP M{TRb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
JURKAT NIDC[I5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LYPVExKM7:TR?= NIS5UJA1QCCq NIPtOlFFVVOR MYTJR|UxRTRwOEmzJO69VQ>? MlzyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEK5OFgoRjJ2M{SyPVQ5RC:jPh?=
CCRF-CEM M{TSbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojpNVAh|ryP MXO0PEBp NITpO5hFVVOR NGnZOlZKSzVyPUGuN|YxKM7:TR?= NInFWYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
LOUCY M3PIXWFxd3C2b4TpZ{BCe3OjeR?= MnKxNkDPxE1? M3i1TVQ5KGh? M{j0WWROW09? NUS5UYtbSXCxcITvd4l{KGmwZIXjeIlwdg>? NEXrXpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
RS4:11 M4rRb2N6fG:2b4jpZ4l1gSCjc4PhfS=> Ml:5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2MEe5O|MoRjJ7NEC3PVc{RC:jPh?=
RS4:11 NULVZY5KVVSVIHHzd4F6 NWXoW|RxPzJiaB?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ5OEOzN{c,OzB{N{izN|M9N2F-
RS4:11 M{W3VW1VWyCjc4PhfS=> Mm\wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7Mk[yOFcoRjJ6OUK2NlQ4RC:jPh?=
Toledo NG\RXmJOXFNiYYPzZZk> M1PwfFczKGh? M2excFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMke4N|M{Lz5|MEK3PFM{OzxxYU6=
NCI60 NG[wdXdUWkJiYYPzZZk> NWXleXZ1PDhiaB?= Mlf1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
RS4:11 MnS1UXRVKGG|c3H5 M13lWFI1KGh? NEnKbGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS1N|E{PSd-Mkm0OVMyOzV:L3G+
melanoma MUnTVmIh[XO|YYm= MWe0PEBp MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
leukemia NXK0eGlKW1KEIHHzd4F6 MkflOFghcA>? NGLwbWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
renal cancer MWrTVmIh[XO|YYm= NX2zUpFLPDhiaB?= M13FXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
non-small cell lung cancer M3LkWHNTSiCjc4PhfS=> MWK0PEBp MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
breast cancer NYHzTJB5W1KEIHHzd4F6 MYe0PEBp Ml;YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
colon cancer MVLTVmIh[XO|YYm= M4DEVVQ5KGh? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
ovarian cancer M3nWSHNTSiCjc4PhfS=> MonFOFghcA>? NYThUWZoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
CNS cancer MV3TVmIh[XO|YYm= Mn[wOFghcA>? Ml;iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
prostate cancer NWDsN4lMW1KEIHHzd4F6 MWi0PEBp MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
Remb1 NVPYUmViVVSWIHHzd4F6 Ml7FNlQhcA>? NWnFPFh7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OVMyOzVpPkK5OFU{OTN3PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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. 

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.

30663221
Growth inhibition assay
Cell viability; 

PubMed: 29876007     


TNBC cells were cultured with the indicated doses of ABT-199 (μM) for 48 h. 

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). 

29876007 28714472
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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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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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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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04790045 Not yet recruiting Drug: Venetoclax Chronic Lymphocytic Leukemia Paolo Ghia|IRCCS San Raffaele May 1 2021 Phase 4
NCT04813263 Recruiting -- Acute Myeloid Leukemia (AML) AbbVie April 8 2021 --
NCT04810598 Not yet recruiting Drug: Venetoclax Renal Impairment|Renal Disease AbbVie|Roche-Genentech March 20 2021 Phase 1

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