Venetoclax (ABT-199)

Catalog No.S8048 Synonyms: GDC-0199

For research use only.

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.

Venetoclax (ABT-199) Chemical Structure

CAS No. 1257044-40-8

Selleck's Venetoclax (ABT-199) has been cited by 450 publications

Purity & Quality Control

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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 M1KwSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjkXGFnOjBibl2= M3LjNlczKGh? NH\aZ4lFVVOR NGL4coxKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MlPOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7MU[2PVgoRjJ3OUG2Olk5RC:jPh?=
CS-THL1 MWTBdI9xfG:2aXOgRZN{[Xl? M3;X[FI2KG6P NVjZ[JJ3TE2VTx?= M1HUUmlv\HWlZYOgZZBweHSxc3nz MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTlzNk[5PEc,OjV7MU[2PVg9N2F-
DoGKiT NGfXNVFCeG:ydH;0bYMhSXO|YYm= NYfSdmdtPTBibl2= MnPQSG1UVw>? M3TXfWlv\HWlZYOgZZBweHSxc3nz M2j1T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUG2Olk5Lz5{NUmxOlY6QDxxYU6=
RS4-11 NYOxSZNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjSO|IhcA>? M{P2WmlEPTB;MD6wOFAzKM7:TR?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ2OUe2PEc,OjV4NEm3Olg9N2F-
NALM-6 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe3PGo6PzJiaB?= M{WyfGlEPTB-MzFOwG0> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ2OUe2PEc,OjV4NEm3Olg9N2F-
SU-DHL-6 NX71Onl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\vW|MxNjhizszN Mn\qTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7MEiwN{c,OjV3OUC4NFM9N2F-
OCI-Ly19 NYHLemFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LHZ|Eh|ryP NVnJPI46UW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? MoLyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUC4NFMoRjJ3NUmwPFA{RC:jPh?=
SU-DHL-6 MYTGeY5kfGmxbjDBd5NigQ>? NXviO3F7OC55NTFOwG0> NFvnRXkyQCCq MVTJcoNz\WG|ZYOgdJJwNXO3co\peoFtKHC{b4TlbY4hVUOOLUGg[ZhxemW|c3nvci=> MojBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUC4NFMoRjJ3NUmwPFA{RC:jPh?=
KCL22 M3fXemZ2dmO2aX;uJGF{e2G7 MX[yJO69VQ>? M{jSSFQ5KGh? MojOSG1UVw>? MYXJcoNz\WG|ZYOgSG5CKG[{YXfhcYVvfGG2aX;u MkTLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{OyOVIoRjJ3M{OzNlUzRC:jPh?=
LOUCY MoL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvo[5gyOCEQvF2= Ml;sOFghcA>? NHXne3BFVVOR Mn3oTWM2OD1yLkCxN|kh|ryP MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
ALL-SIL M2HaTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInLN|YyOCEQvF2= MmX3OFghcA>? NGLneGhFVVOR NInwdlJKSzVyPUCuNVgxOyEQvF2= NIHyVFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
CUTLL1 NVn5S25UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3jRnpDOTBizszN MVO0PEBp M1u0bGROW09? NFvycnJKSzVyPUCuN|gzOyEQvF2= NHryT4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
KOPTK1 NXXXPVFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYKxNEDPxE1? MkfEOFghcA>? NG\wXYlFVVOR MXLJR|UxRTBwNkSzNkDPxE1? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
DND-41 M3PXb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXKNVAh|ryP M1Ts[|Q5KGh? NELjOWRFVVOR NHT5cGRKSzVyPUGuPVY6PSEQvF2= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
PF-382 NGC3Z2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\LU2tiOTBizszN NEL1RWI1QCCq MVrEUXNQ M1fnXWlEPTB;Mj6xPFI1KM7:TR?= NGDGW5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
KARPAS-45 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIe4eJQyOCEQvF2= NEHmVlA1QCCq MXvEUXNQ NGmwZnBKSzVyPUOuNlIzPSEQvF2= NXHtZ2t6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNFE4ODRpPkK1N|AyPzB2PD;hQi=>
PEER M13HWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDMNVAh|ryP MUS0PEBp MlTHSG1UVw>? NITGRpVKSzVyPUSuOlQxOyEQvF2= MoP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
CX-1 NWHtSIptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH0NVAxKM7:TR?= NVTtZnNiPzJiaB?= MXvJR|UxRTZwNzFOwG0> NGTs[VM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKwPFg5Oid-MkWyNFg5QDJ:L3G+
LS147T MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfyNWcyODBizszN M1f2NlczKGh? NFv1Z4xKSzVyPUK5MlUh|ryP M3TZe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkC4PFgzLz5{NUKwPFg5OjxxYU6=
HL-60 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlT5OFghcA>? NFTsUIZKSzVyPEGg{txO NUTwc2Y4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
MOLM-13 NEfFWoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonKOFghcA>? NW[ycYxQUUN3MEyxJO69VQ>? NVrwZYJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
OCI-AML2 MoOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnH0OFghcA>? NWLxU5hNUUN3MEyxJO69VQ>? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
Kasumi-1 NGfqR29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfsOFghcA>? M3nIdGlEPTB:MTFOwG0> NYfFe2F[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
KG-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fQRVQ5KGh? MYHJR|UxRDFizszN NX;JNFZqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
THP-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XrNVQ5KGh? NYDRb2hOUUN3MEyxJO69VQ>? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
MOLM-14 MlTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYm0PEBp M2jac2lEPTB:MTFOwG0> MmnFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NE[xNVYoRjJ2M{S2NVE3RC:jPh?=
MOLM-13 MV;BdI9xfG:2aXOgRZN{[Xl? MUi1NEBvVQ>? MlyyNlQhcA>? NHPKdmNCeG:ydH;zbZMhcW6mdXP0bY9v M13icFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
HSB NU\sUII2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LGTFExKM7:TR?= MWi0PEBp NV7rU3p1TE2VTx?= Ml7mTWM2OD12LkS0PEDPxE1? NUfm[VZbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
MOLT4 NVPIOXo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37CSFExKM7:TR?= M2rEO|Q5KGh? MXXEUXNQ MoHwTWM2OD12LkG1OEDPxE1? NV21doV4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
SKW-3/KE-37 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3KT|ZOOTBizszN MX20PEBp MWXEUXNQ M{XUb2lEPTB;MD63NVIh|ryP NYrmdmxmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
SUPT-11 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7sNVAh|ryP NYjSPXYxPDhiaB?= M4fl[WROW09? M4q4OmlEPTB;ND60O|Mh|ryP M1rKblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
JURKAT NWTzS45WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTDbYNXOTBizszN NFH1U5U1QCCq NFvkcWtFVVOR NWO0XIJZUUN3ME20Mlg6OyEQvF2= M1zMOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
CCRF-CEM MnHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOxNEDPxE1? NGO2NXA1QCCq NHfBUGRFVVOR NXS3PGV6UUN3ME2xMlM3OCEQvF2= M4nHVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
LOUCY NHv1eG5CeG:ydH;0bYMhSXO|YYm= Mn72NkDPxE1? M36zbFQ5KGh? M3zCRWROW09? MmqxRZBweHSxc3nzJIlv\HWldHnvci=> NV7Hdm57RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
RS4:11 M1T2NGN6fG:2b4jpZ4l1gSCjc4PhfS=> NEG0PYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSwO|k4Oyd-Mkm0NFc6PzN:L3G+
RS4:11 MUnNWHMh[XO|YYm= Mn63O|IhcA>? M2jwdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMke4N|M{Lz5|MEK3PFM{OzxxYU6=
RS4:11 MYfNWHMh[XO|YYm= NV60dpZ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5NlYzPDdpPkK4PVI3OjR5PD;hQi=>
Toledo MYfNWHMh[XO|YYm= M4rEeVczKGh? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ5OEOzN{c,OzB{N{izN|M9N2F-
NCI60 NX7HVFNZW1KEIHHzd4F6 M{\mb|Q5KGh? M17FNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
RS4:11 MVfNWHQh[XO|YYm= NUnrbJhtOjRiaB?= NHTCdmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS1N|E{PSd-Mkm0OVMyOzV:L3G+
melanoma NYrNfnZ4W1KEIHHzd4F6 MXy0PEBp NF;JUHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
leukemia NUPFUIF2W1KEIHHzd4F6 MnnSOFghcA>? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
renal cancer MmfuV3JDKGG|c3H5 MoDLOFghcA>? NGTIeo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
non-small cell lung cancer NYTndVB5W1KEIHHzd4F6 M1jKe|Q5KGh? MkDGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
breast cancer MVvTVmIh[XO|YYm= NHzyWnc1QCCq M4P4WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
colon cancer NWT0eZRZW1KEIHHzd4F6 MlXGOFghcA>? NHK5TIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
ovarian cancer NEnnNYdUWkJiYYPzZZk> MVe0PEBp NHj4ZWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
CNS cancer M4O1fXNTSiCjc4PhfS=> NXrTT3VLPDhiaB?= NEToOXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
prostate cancer M2[1cXNTSiCjc4PhfS=> MoLQOFghcA>? MmXXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
Remb1 NVvofItMVVSWIHHzd4F6 NFzyeZMzPCCq M{TEc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEWzNVM2Lz5{OUS1N|E{PTxxYU6=
Assay
Methods Test Index PMID
Western blot Mcl-1 / Bcl-xl / Bcl-2 / Bak / NOXA / Bim ; PARP / Cleaved PARP / Caspase 3 / Cleaved caspase3 / p-S6(Ser236/236) 30663221
Growth inhibition assay Cell death ; Cell viability 28714472 29876007
Immunofluorescence Bcl-2 / Mcl-1 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 (from 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 Research:[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 Research:[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)
  • Dosages: ~100 mg/kg
  • Administration: Orally

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 868.44
Formula

C45H50ClN7O7S

CAS No. 1257044-40-8
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05053659 Not yet recruiting Drug: Loncastuximab tesirine|Drug: Venetoclax Relapsed Non Hodgkin Lymphoma|Refractory Non-Hodgkin Lymphoma Brian Hill MD PhD|Case Comprehensive Cancer Center March 2022 Phase 1
NCT05155709 Not yet recruiting Drug: siremadlin|Drug: venetoclax|Drug: azacitidine Acute Myeloid Leukemia Novartis Pharmaceuticals|Novartis February 24 2022 Phase 1|Phase 2
NCT04790045 Not yet recruiting Drug: Venetoclax Chronic Lymphocytic Leukemia Paolo Ghia|IRCCS San Raffaele January 1 2022 Phase 4
NCT05074355 Not yet recruiting Drug: Azacitidine|Drug: Venetoclax Myeloproliferative Neoplasm|BCR-ABL Negative University Health Network Toronto December 6 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
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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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