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 452 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 NH;sN29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlq4NlAhdk1? NHvNNVY4OiCq NF3kN|RFVVOR MlHQTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NGH3bZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUmxOlY6QCd-MkW5NVY3QTh:L3G+
CS-THL1 MkS5RZBweHSxdHnjJGF{e2G7 M2HqR|I2KG6P NYSxfHl5TE2VTx?= M3\jeGlv\HWlZYOgZZBweHSxc3nz M4DxbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUG2Olk5Lz5{NUmxOlY6QDxxYU6=
DoGKiT M2TUZWFxd3C2b4TpZ{BCe3OjeR?= NVezZ3VsPTBibl2= NVO5d4tiTE2VTx?= NGPJU|lKdmS3Y3XzJIFxd3C2b4Ppdy=> M1fXN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUG2Olk5Lz5{NUmxOlY6QDxxYU6=
RS4-11 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV23NkBp M2jJc2lEPTB;MD6wOFAzKM7:TR?= NV;rUGNORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OFk4PjhpPkK1OlQ6PzZ6PD;hQi=>
NALM-6 NFPHVHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLFWIdWPzJiaB?= NEX6fFhKSzVyPkOg{txO Mo\TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NEm3OlgoRjJ3NkS5O|Y5RC:jPh?=
SU-DHL-6 MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17mbFAvQCEQvF2= MnLaTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NYTObnhORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1PVA5ODNpPkK1OVkxQDB|PD;hQi=>
OCI-Ly19 M3PneWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTOVodjOSEQvF2= NYWyZYxDUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? NWPlUpFNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1PVA5ODNpPkK1OVkxQDB|PD;hQi=>
SU-DHL-6 NU\NOnFsTnWwY4Tpc44hSXO|YYm= M{nWRVAvPzVizszN NGrzUWYyQCCq M2m0emlv[3KnYYPld{Bxem9vc4Xyeol3[WxicILveIVqdiCPQ1ytNUBmgHC{ZYPzbY9v MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7MEiwN{c,OjV3OUC4NFM9N2F-
KCL22 MVrGeY5kfGmxbjDBd5NigQ>? MX:yJO69VQ>? MY[0PEBp NULi[|Y{TE2VTx?= MVTJcoNz\WG|ZYOgSG5CKG[{YXfhcYVvfGG2aX;u NUjaeZJORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|MzPTJpPkK1N|M{OjV{PD;hQi=>
LOUCY M4PxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX1dZl4OTBizszN NILCVo01QCCq NH;WbWxFVVOR MnjFTWM2OD1yLkCxN|kh|ryP NHnqW|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
ALL-SIL NHL6RYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLMdoVyOTBizszN NIfG[o81QCCq MmP0SG1UVw>? MmnSTWM2OD1yLkG4NFMh|ryP MnnCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
CUTLL1 NYj1VHZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rZOlExKM7:TR?= MkXNOFghcA>? MnPCSG1UVw>? NFnBZ3dKSzVyPUCuN|gzOyEQvF2= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
KOPTK1 MnXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT0UGpSOTBizszN NUT6WllFPDhiaB?= NVftRoFSTE2VTx?= NX7ScWxMUUN3ME2wMlY1OzJizszN NFjNVoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
DND-41 MoTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUWxNEDPxE1? M{nPT|Q5KGh? NHLHWlBFVVOR NFTseXJKSzVyPUGuPVY6PSEQvF2= M2[1R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{CxO|A1Lz5{NUOwNVcxPDxxYU6=
PF-382 NUS2UpltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXCZ|YyOCEQvF2= NXrIdIF1PDhiaB?= NVnNW4x4TE2VTx?= MlHRTWM2OD1{LkG4NlQh|ryP Moj5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
KARPAS-45 M2TNSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELCZnoyOCEQvF2= MWm0PEBp NInDS3NFVVOR MXLJR|UxRTNwMkKyOUDPxE1? M4m1NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{CxO|A1Lz5{NUOwNVcxPDxxYU6=
PEER Mnn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HpNlExKM7:TR?= NFW1XlE1QCCq NHuzOHVFVVOR MkW3TWM2OD12Lk[0NFMh|ryP NVHEeI83RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNFE4ODRpPkK1N|AyPzB2PD;hQi=>
CX-1 M4T0[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSxNFAh|ryP NVvrboxCPzJiaB?= MXXJR|UxRTZwNzFOwG0> NGLWVok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKwPFg5Oid-MkWyNFg5QDJ:L3G+
LS147T MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXVNVAxKM7:TR?= M1rzVVczKGh? NH62R|RKSzVyPUK5MlUh|ryP MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJyOEi4Nkc,OjV{MEi4PFI9N2F-
HL-60 NWrCWZhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnCWnBwPDhiaB?= MmL6TWM2ODxzIN88US=> Mkn4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NE[xNVYoRjJ2M{S2NVE3RC:jPh?=
MOLM-13 NFTYWmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jrXVQ5KGh? MXfJR|UxRDFizszN MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
OCI-AML2 NFrvOFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrqOFghcA>? MWXJR|UxRDFizszN M3X4Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
Kasumi-1 M3Hk[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjlO3M1QCCq NV7mVnZtUUN3MEyxJO69VQ>? NFXjTG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
KG-1 NGjjW5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3qwOVQ5KGh? NVfEUYRXUUN3MEyxJO69VQ>? NIDxRWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
THP-1 NEK5fJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXK0PEBp MX3JR|UxRDFizszN NUTQfll6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
MOLM-14 NIjaT4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\F[m01QCCq M3;Cb2lEPTB:MTFOwG0> NW\EO3ZsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
MOLM-13 NGnNZXRCeG:ydH;0bYMhSXO|YYm= NEDKSXo2OCCwTR?= NGn4Z|EzPCCq NGHjN4NCeG:ydH;zbZMhcW6mdXP0bY9v M3jUSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
HSB MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\kNnEyOCEQvF2= MVe0PEBp M{PRU2ROW09? MmnYTWM2OD12LkS0PEDPxE1? NYfOcmdVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
MOLT4 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXGxNEDPxE1? NX;mNlJXPDhiaB?= M3PuTmROW09? NGHtcldKSzVyPUSuNVU1KM7:TR?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2Mkm0PEc,OjR|NEK5OFg9N2F-
SKW-3/KE-37 NXjtem01T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYCxNEDPxE1? M2L0fVQ5KGh? MVjEUXNQ NH;YcZVKSzVyPUCuO|EzKM7:TR?= Mme4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEK5OFgoRjJ2M{SyPVQ5RC:jPh?=
SUPT-11 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSxNEDPxE1? MnfvOFghcA>? NYLldlkzTE2VTx?= NWnXUoE{UUN3ME20MlQ4OyEQvF2= NIm4dpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
JURKAT NITyTVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXz1O5RUOTBizszN NIDLTWg1QCCq NFrGcZRFVVOR NE\lbGhKSzVyPUSuPFk{KM7:TR?= Mme5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEK5OFgoRjJ2M{SyPVQ5RC:jPh?=
CCRF-CEM MlrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrv[ms{OTBizszN NFS1d|E1QCCq MWXEUXNQ NHfXUJRKSzVyPUGuN|YxKM7:TR?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2Mkm0PEc,OjR|NEK5OFg9N2F-
LOUCY NU[1SotxSXCxcITveIlkKEG|c3H5 MlTzNkDPxE1? NEjpdHc1QCCq Mo\OSG1UVw>? NH;TTXBCeG:ydH;zbZMhcW6mdXP0bY9v NIe3eII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
RS4:11 M{nJfmN6fG:2b4jpZ4l1gSCjc4PhfS=> NULhbFZmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzNpPkK5OFA4QTd|PD;hQi=>
RS4:11 MnK3UXRUKGG|c3H5 MoC4O|IhcA>? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ5OEOzN{c,OzB{N{izN|M9N2F-
RS4:11 M4XaXW1VWyCjc4PhfS=> MknqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7Mk[yOFcoRjJ6OUK2NlQ4RC:jPh?=
Toledo NV71bIZyVVSVIHHzd4F6 NIj1elk4OiCq MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ5OEOzN{c,OzB{N{izN|M9N2F-
NCI60 MYrTVmIh[XO|YYm= M3;WflQ5KGh? NV3oVXBNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
RS4:11 NV7CdXpEVVSWIHHzd4F6 NEXpNW4zPCCq NXPjeo9wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OVMyOzVpPkK5OFU{OTN3PD;hQi=>
melanoma NHL4folUWkJiYYPzZZk> MYS0PEBp NX;CVVJ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
leukemia M4Hw[XNTSiCjc4PhfS=> M4nzSFQ5KGh? NUn0UVhYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
renal cancer M1\5[nNTSiCjc4PhfS=> MWq0PEBp MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
non-small cell lung cancer NHnPe3BUWkJiYYPzZZk> MXu0PEBp MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
breast cancer Mn;XV3JDKGG|c3H5 NEfON3E1QCCq NW\5PHpmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
colon cancer NYTaRpRbW1KEIHHzd4F6 NWPVVJhyPDhiaB?= MnzVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
ovarian cancer NWPtfopLW1KEIHHzd4F6 MnTEOFghcA>? NFjXNXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
CNS cancer MXLTVmIh[XO|YYm= M{PLUVQ5KGh? NVzNdotURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
prostate cancer M1jUO3NTSiCjc4PhfS=> NXrV[plJPDhiaB?= NXL3fY5oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
Remb1 MXjNWHQh[XO|YYm= MYGyOEBp NVPzTFVIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OVMyOzVpPkK5OFU{OTN3PD;hQi=>
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.

2.5mg/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
NCT05464836 Not yet recruiting Drug: CB-103|Drug: Venetoclax Leukemia Lymphoblastic|Leukemia M.D. Anderson Cancer Center December 30 2022 Phase 2
NCT05360160 Not yet recruiting Drug: SNDX-5613|Drug: Venetoclax|Drug: ASTX727 Acute Myeloid Leukemia M.D. Anderson Cancer Center|Astex Pharmaceuticals Inc.|Syndax Pharmaceuticals Inc. October 31 2022 Phase 1|Phase 2
NCT05226455 Not yet recruiting Drug: venetoclax + azacitidine +/- donor lymphocyte infusion MDS|AML Groupe Francophone des Myelodysplasies|AbbVie September 1 2022 Phase 1|Phase 2
NCT05053659 Recruiting Drug: Loncastuximab tesirine|Drug: Venetoclax Relapsed Non Hodgkin Lymphoma|Refractory Non-Hodgkin Lymphoma Brian Hill MD PhD|Case Comprehensive Cancer Center September 2022 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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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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