Venetoclax (ABT-199)

For research use only.

Catalog No.S8048 Synonyms: GDC-0199

406 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.

Selleck's Venetoclax (ABT-199) has been cited by 406 publications

Purity & Quality Control

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 M2X6SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHKdWJMOjBibl2= NGnEdY04OiCq NHLifHpFVVOR MYfJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> NF6zboI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUmxOlY6QCd-MkW5NVY3QTh:L3G+
CS-THL1 MXLBdI9xfG:2aXOgRZN{[Xl? MYGyOUBvVQ>? MnTKSG1UVw>? NXTLfXJTUW6mdXPld{BieG:ydH;zbZM> MmHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7MU[2PVgoRjJ3OUG2Olk5RC:jPh?=
DoGKiT NGr2ZnNCeG:ydH;0bYMhSXO|YYm= MVu1NEBvVQ>? M1;4O2ROW09? NEH4NYVKdmS3Y3XzJIFxd3C2b4Ppdy=> MmD1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7MU[2PVgoRjJ3OUG2Olk5RC:jPh?=
RS4-11 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUC3NkBp M{HOU2lEPTB;MD6wOFAzKM7:TR?= MnfrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NEm3OlgoRjJ3NkS5O|Y5RC:jPh?=
NALM-6 Mn;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XsS|czKGh? NYHvNINnUUN3ME6zJO69VQ>? MlvqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NEm3OlgoRjJ3NkS5O|Y5RC:jPh?=
SU-DHL-6 M4nzUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjSNE45KM7:TR?= NYTt[Wp7UW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7MEiwN{c,OjV3OUC4NFM9N2F-
OCI-Ly19 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LyPFEh|ryP Mo\wTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> MmDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUC4NFMoRjJ3NUmwPFA{RC:jPh?=
SU-DHL-6 NG\PTWhHfW6ldHnvckBCe3OjeR?= M1v5NFAvPzVizszN MmfWNVghcA>? MVLJcoNz\WG|ZYOgdJJwNXO3co\peoFtKHC{b4TlbY4hVUOOLUGg[ZhxemW|c3nvci=> M3q1PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUmwPFA{Lz5{NUW5NFgxOzxxYU6=
KCL22 NFPUeZdHfW6ldHnvckBCe3OjeR?= NX7GeJZmOiEQvF2= M2XmelQ5KGh? NEXyUI9FVVOR NEnTb3VKdmO{ZXHz[ZMhTE6DIH\yZYdidWWwdHH0bY9v NFzGb3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOzN|I2Oid-MkWzN|MzPTJ:L3G+
LOUCY MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXKO5FyOTBizszN NVjxfVFlPDhiaB?= NUS1[Hp2TE2VTx?= NIjiXYdKSzVyPUCuNFE{QSEQvF2= NF71UIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
ALL-SIL NYnHOnFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\1bYQyOCEQvF2= NWjld|JoPDhiaB?= NHuyVYJFVVOR MWrJR|UxRTBwMUiwN{DPxE1? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
CUTLL1 M{joWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELxW4EyOCEQvF2= NE[xbZM1QCCq M3\1TGROW09? M1rtRWlEPTB;MD6zPFI{KM7:TR?= NXnLTnJERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNFE4ODRpPkK1N|AyPzB2PD;hQi=>
KOPTK1 M3HaSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXyxNEDPxE1? M4XmdVQ5KGh? Mk\kSG1UVw>? NUTMepp1UUN3ME2wMlY1OzJizszN MnrSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
DND-41 NUnwOZl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqxNEDPxE1? M1PYdFQ5KGh? NVG2TndqTE2VTx?= NFj0b3hKSzVyPUGuPVY6PSEQvF2= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
PF-382 M1TJ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjKNVAh|ryP M4XTfFQ5KGh? MmXoSG1UVw>? M1rMbWlEPTB;Mj6xPFI1KM7:TR?= M2q5OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{CxO|A1Lz5{NUOwNVcxPDxxYU6=
KARPAS-45 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWxNEDPxE1? MVm0PEBp NGDMZ|ZFVVOR NITYemZKSzVyPUOuNlIzPSEQvF2= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
PEER M1nEbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2xNEDPxE1? M1Xw[lQ5KGh? NIq0N2lFVVOR NG[zd|lKSzVyPUSuOlQxOyEQvF2= NUDVRVF3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNFE4ODRpPkK1N|AyPzB2PD;hQi=>
CX-1 M3vpd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1exclExOCEQvF2= NUPre4hPPzJiaB?= NFniZ2RKSzVyPU[uO{DPxE1? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJyOEi4Nkc,OjV{MEi4PFI9N2F-
LS147T MoHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXqd5dZOTByIN88US=> MoHYO|IhcA>? NWPMRVdDUUN3ME2yPU42KM7:TR?= NGWxOGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKwPFg5Oid-MkWyNFg5QDJ:L3G+
HL-60 M2DOS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWC0PEBp MVvJR|UxRDFizszN M{DMXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
MOLM-13 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{f0O|Q5KGh? MnPyTWM2ODxzIN88US=> M1fVRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
OCI-AML2 M2HiPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVq0PEBp MnPKTWM2ODxzIN88US=> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
Kasumi-1 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIH3TnU1QCCq MoXSTWM2ODxzIN88US=> NGq5cFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
KG-1 NVzaWo9HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrne|k1QCCq M2DmTGlEPTB:MTFOwG0> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
THP-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPEUok1QCCq M2rJSmlEPTB:MTFOwG0> NIjD[VQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
MOLM-14 NW[0c4ZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPtOFghcA>? M{judmlEPTB:MTFOwG0> M{fJV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
MOLM-13 Mo\0RZBweHSxdHnjJGF{e2G7 NUfOSodkPTBibl2= MV:yOEBp NYrVSINvSXCxcITvd4l{KGmwZIXjeIlwdg>? MmqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NE[xNVYoRjJ2M{S2NVE3RC:jPh?=
HSB M{[zOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XrR|ExKM7:TR?= M4nhWFQ5KGh? NWPiTVJDTE2VTx?= NX\ZZpFDUUN3ME20MlQ1QCEQvF2= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2Mkm0PEc,OjR|NEK5OFg9N2F-
MOLT4 MmjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjSPFkyOCEQvF2= MX60PEBp Ml\HSG1UVw>? MYrJR|UxRTRwMUW0JO69VQ>? MorPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEK5OFgoRjJ2M{SyPVQ5RC:jPh?=
SKW-3/KE-37 NETSdYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrBVlRHOTBizszN NFzEd|A1QCCq NVrCRYp5TE2VTx?= MYLJR|UxRTBwN{GyJO69VQ>? NITjN2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
SUPT-11 M1ztfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILZRWgyOCEQvF2= M2PweVQ5KGh? MnzwSG1UVw>? MknITWM2OD12LkS3N{DPxE1? M2\3RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
JURKAT Moj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfFbVVnOTBizszN Mm\QOFghcA>? M4X5SmROW09? NFjFRpdKSzVyPUSuPFk{KM7:TR?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2Mkm0PEc,OjR|NEK5OFg9N2F-
CCRF-CEM NEPrSFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX4NVAh|ryP MnXEOFghcA>? MkL5SG1UVw>? NHmyWWhKSzVyPUGuN|YxKM7:TR?= NHXzWXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
LOUCY M3Tac2Fxd3C2b4TpZ{BCe3OjeR?= NE\3d2QzKM7:TR?= MlzMOFghcA>? NFHyTodFVVOR NIH6OmhCeG:ydH;zbZMhcW6mdXP0bY9v NVy3UW9{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
RS4:11 MkHtR5l1d3SxeHnjbZR6KGG|c3H5 MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3N{c,Ojl2MEe5O|M9N2F-
RS4:11 MWDNWHMh[XO|YYm= Mnf5O|IhcA>? NX\DOmxjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyO|g{OzNpPkOwNlc5OzN|PD;hQi=>
RS4:11 MkTCUXRUKGG|c3H5 MlHDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7Mk[yOFcoRjJ6OUK2NlQ4RC:jPh?=
Toledo NULoSYNNVVSVIHHzd4F6 M1nZflczKGh? NX\xdFliRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyO|g{OzNpPkOwNlc5OzN|PD;hQi=>
NCI60 MmGxV3JDKGG|c3H5 NYr4c5pJPDhiaB?= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
RS4:11 MknvUXRVKGG|c3H5 MoLHNlQhcA>? Mo\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NUOxN|UoRjJ7NEWzNVM2RC:jPh?=
melanoma MnLiV3JDKGG|c3H5 MlPHOFghcA>? NWOwUYdJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
leukemia MniyV3JDKGG|c3H5 NXfsbZhkPDhiaB?= MmfhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
renal cancer NFHZZ29UWkJiYYPzZZk> NHPacZY1QCCq M4G4[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
non-small cell lung cancer NXPYfFA1W1KEIHHzd4F6 NF;kTGM1QCCq NVHYWIFORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
breast cancer NGf3SItUWkJiYYPzZZk> NXn0[Y5TPDhiaB?= NYPySJJLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
colon cancer MVfTVmIh[XO|YYm= MX60PEBp Mn:2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
ovarian cancer MojwV3JDKGG|c3H5 MlnzOFghcA>? NIrLOHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
CNS cancer NYTBclFFW1KEIHHzd4F6 Mnj3OFghcA>? NXHXVFY1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
prostate cancer NEKyNYxUWkJiYYPzZZk> Ml;sOFghcA>? NGXnVm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
Remb1 NIr2TWZOXFRiYYPzZZk> NWTYZ29tOjRiaB?= Mo\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NUOxN|UoRjJ7NEWzNVM2RC:jPh?=

... 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 (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 ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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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 SDS / COA (available on product pages).

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Dilution Calculator

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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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

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Molarity Calculator

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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 January 1 2022 Phase 4
NCT05025423 Not yet recruiting Drug: Venetoclax Oral Tablet [Venclexta] Mantle Cell Lymphoma Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|AbbVie September 15 2021 Phase 2
NCT04926285 Not yet recruiting Drug: Omacetaxine|Drug: Venetoclax Relapsed or Refractory Hematologic Malignancies University of Illinois at Chicago September 2021 Phase 1
NCT04722601 Not yet recruiting Drug: Venetoclax|Drug: Obinutuzumab|Drug: CC-486 Follicular Lymphoma University of Chicago 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