Venetoclax (ABT-199)

For research use only. Not for use in humans.

製品コードS8048 別名:GDC-0199

Venetoclax (ABT-199)化学構造

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.

サイズ 価格(税別)  
JPY 46800
JPY 163000
JPY 432500
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バルク問合せ

文献中Selleckの製品使用例(423)

製品安全説明書

Bcl-2阻害剤の選択性比較

生物活性

製品説明 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.
特性 Re-engineered version of ABT-263 (Navitoclax).
ターゲット
Bcl-2 [1]
(Cell-free assay)
<0.01 nM(Ki)
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CS-THL1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrBcI8zOCCwTR?= M2fwNFczKGh? MnPLSG1UVw>? MnvBTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> M4HL[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUG2Olk5Lz5{NUmxOlY6QDxxYU6=
CS-THL1 NW\udJcxSXCxcITveIlkKEG|c3H5 M4fMUlI2KG6P NXPrPVV3TE2VTx?= M1nSTGlv\HWlZYOgZZBweHSxc3nz NYTZSphQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5NVY3QThpPkK1PVE3Pjl6PD;hQi=>
DoGKiT M2HWfmFxd3C2b4TpZ{BCe3OjeR?= MofjOVAhdk1? MkTtSG1UVw>? MW\JcoR2[2W|IHHwc5B1d3Orcx?= M1TaWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUG2Olk5Lz5{NUmxOlY6QDxxYU6=
RS4-11 NUL3T3Y4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXe3NkBp NGrRWVBKSzVyPUCuNFQxOiEQvF2= M4HwNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkS5O|Y5Lz5{NU[0PVc3QDxxYU6=
NALM-6 NVTsSWdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHXTGFYPzJiaB?= Mlr3TWM2OD5|IN88US=> MmP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NEm3OlgoRjJ3NkS5O|Y5RC:jPh?=
SU-DHL-6 MmXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjrTJllOC56IN88US=> MXTJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7MEiwN{c,OjV3OUC4NFM9N2F-
OCI-Ly19 NWrORWpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHL[XkyKM7:TR?= NWDKUGtiUW6qaXLpeJMh[2WubDDndo94fGhiYYPz[ZN{\WRiYomgZ4VtdCC4aXHibYxqfHl? NYT3fXV7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1PVA5ODNpPkK1OVkxQDB|PD;hQi=>
SU-DHL-6 NWDKOHd1TnWwY4Tpc44hSXO|YYm= NXHOeGFkOC55NTFOwG0> MUSxPEBp NGH3OWpKdmO{ZXHz[ZMheHKxLYP1dpZqfmGuIIDyc5RmcW5iTVPMMVEh\XiycnXzd4lwdg>? MlPCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUC4NFMoRjJ3NUmwPFA{RC:jPh?=
KCL22 NY\a[FM1TnWwY4Tpc44hSXO|YYm= NFXaOnkzKM7:TR?= NUfaWVNbPDhiaB?= MkDISG1UVw>? MnrrTY5kemWjc3XzJGRPSSCocnHnZY1mdnSjdHnvci=> NVXYOmM4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|MzPTJpPkK1N|M{OjV{PD;hQi=>
LOUCY MnvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXWxNEDPxE1? M323RVQ5KGh? Mn7WSG1UVw>? MU\JR|UxRTBwMEGzPUDPxE1? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
ALL-SIL MnzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nOfVExKM7:TR?= MkTROFghcA>? NF;V[mlFVVOR MoGwTWM2OD1yLkG4NFMh|ryP M1[1TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{CxO|A1Lz5{NUOwNVcxPDxxYU6=
CUTLL1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjzW4syOCEQvF2= M4LuWFQ5KGh? MVzEUXNQ NXXaWGE2UUN3ME2wMlM5OjNizszN M{TyXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{CxO|A1Lz5{NUOwNVcxPDxxYU6=
KOPTK1 NFey[ZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;EN4UyOCEQvF2= MUK0PEBp NW[4NG9GTE2VTx?= Mn;QTWM2OD1yLk[0N|Ih|ryP NFTSeWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
DND-41 M{DlWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm1O|JJOTBizszN NV3DW2d2PDhiaB?= NXvu[JBlTE2VTx?= NFy1em5KSzVyPUGuPVY6PSEQvF2= MofGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
PF-382 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\GcYUyOCEQvF2= NIDGWFQ1QCCq NFLDT5pFVVOR MVfJR|UxRTJwMUiyOEDPxE1? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
KARPAS-45 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnrNVAh|ryP NXTudJpSPDhiaB?= NV\qc3VxTE2VTx?= MmrJTWM2OD1|LkKyNlUh|ryP MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
PEER Mly0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTu[IoyOCEQvF2= MoK5OFghcA>? NYPnUnVLTE2VTx?= NHv2O5ZKSzVyPUSuOlQxOyEQvF2= NGrrSGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
CX-1 M1\vcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPvNVAxKM7:TR?= MmG0O|IhcA>? MmP4TWM2OD14Lkeg{txO MmnmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MEi4PFIoRjJ3MkC4PFgzRC:jPh?=
LS147T MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmxNFAh|ryP NFPFVI44OiCq M3fzcWlEPTB;MkmuOUDPxE1? MlWzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MEi4PFIoRjJ3MkC4PFgzRC:jPh?=
HL-60 MkGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfCNZpuPDhiaB?= MlrpTWM2ODxzIN88US=> NGXpZoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
MOLM-13 NVzzZlJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PPNVQ5KGh? MoHyTWM2ODxzIN88US=> NFHwfJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
OCI-AML2 NYPaPGlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPNOFghcA>? NWraR3d4UUN3MEyxJO69VQ>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
Kasumi-1 NWTWdW14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYC0PEBp M3P2PGlEPTB:MTFOwG0> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
KG-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLyOFghcA>? MlTiTWM2ODxzIN88US=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
THP-1 NX7zRZhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7vUHlrPDhiaB?= M4TPXGlEPTB:MTFOwG0> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
MOLM-14 NF3UTFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nhUFQ5KGh? MYXJR|UxRDFizszN MnTCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NE[xNVYoRjJ2M{S2NVE3RC:jPh?=
MOLM-13 M3jMemFxd3C2b4TpZ{BCe3OjeR?= MYG1NEBvVQ>? M3;wOVI1KGh? MleyRZBweHSxc3nzJIlv\HWldHnvci=> MnjCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NE[xNVYoRjJ2M{S2NVE3RC:jPh?=
HSB MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPWcoJoOTBizszN NVLGOlBNPDhiaB?= NHW0WZhFVVOR NFTTRY1KSzVyPUSuOFQ5KM7:TR?= MkTKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEK5OFgoRjJ2M{SyPVQ5RC:jPh?=
MOLT4 M3;zS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTxXZV5OTBizszN NILQTWQ1QCCq M1XtSWROW09? NWrRWplEUUN3ME20MlE2PCEQvF2= M{[yOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
SKW-3/KE-37 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fxblExKM7:TR?= MWe0PEBp NX3wXlVmTE2VTx?= MVLJR|UxRTBwN{GyJO69VQ>? NGHpcFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
SUPT-11 M2jlWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxNEDPxE1? M1LmNVQ5KGh? MWHEUXNQ M2fNXmlEPTB;ND60O|Mh|ryP MkDQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEK5OFgoRjJ2M{SyPVQ5RC:jPh?=
JURKAT MkP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV6xNEDPxE1? NHHqflM1QCCq MWTEUXNQ M4nsSGlEPTB;ND64PVMh|ryP MlX5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEK5OFgoRjJ2M{SyPVQ5RC:jPh?=
CCRF-CEM NUTYPHRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\NNVAh|ryP NXnyfXJ{PDhiaB?= MYTEUXNQ M{PaTWlEPTB;MT6zOlAh|ryP MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2Mkm0PEc,OjR|NEK5OFg9N2F-
LOUCY M3j2TmFxd3C2b4TpZ{BCe3OjeR?= M2LpV|Ih|ryP M1znO|Q5KGh? NXHIVGY1TE2VTx?= NIrXbIVCeG:ydH;zbZMhcW6mdXP0bY9v NFLKfVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
RS4:11 MUDDfZRwfG:6aXPpeJkh[XO|YYm= NX\4dXc3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzNpPkK5OFA4QTd|PD;hQi=>
RS4:11 MnzNUXRUKGG|c3H5 M{HIUFczKGh? M1PQclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMke4N|M{Lz5|MEK3PFM{OzxxYU6=
RS4:11 MmjiUXRUKGG|c3H5 M4LGTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUK2NlQ4Lz5{OEmyOlI1PzxxYU6=
Toledo NYC1ZllKVVSVIHHzd4F6 NGDSe5I4OiCq MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ5OEOzN{c,OzB{N{izN|M9N2F-
NCI60 NWLmR4NHW1KEIHHzd4F6 NVPxSZM6PDhiaB?= M{jzcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
RS4:11 NG\nfHROXFRiYYPzZZk> NV76eZVxOjRiaB?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR3M{GzOUc,Ojl2NUOxN|U9N2F-
melanoma MUXTVmIh[XO|YYm= NIHVdXk1QCCq NGjLXW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
leukemia MoXnV3JDKGG|c3H5 MnH5OFghcA>? MkfCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
renal cancer M37hUHNTSiCjc4PhfS=> MYi0PEBp NYrLW|d[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
non-small cell lung cancer NFu4SFFUWkJiYYPzZZk> NX;LO3A1PDhiaB?= MnPBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
breast cancer M1nsZ3NTSiCjc4PhfS=> MknPOFghcA>? NIS4SYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
colon cancer MmjWV3JDKGG|c3H5 NXXRUld2PDhiaB?= Mn;LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
ovarian cancer NULFWpBUW1KEIHHzd4F6 NHLOS2s1QCCq M4ezO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
CNS cancer MVnTVmIh[XO|YYm= MX:0PEBp MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
prostate cancer M3jUUXNTSiCjc4PhfS=> NHrlbpY1QCCq M2nv[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
Remb1 M4PEUW1VXCCjc4PhfS=> MXqyOEBp M{HCOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEWzNVM2Lz5{OUS1N|E{PTxxYU6=

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アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
- 合併

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.
細胞試験: [1]
- 合併
  • 細胞株: NHL, DLBCL, MCL, AML and ALL cell lines
  • 濃度: ~1 μM
  • 反応時間: 48 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[1]
- 合併
  • 動物モデル: Female C.B-17 SCID mice (DoHH2 and Granta-519 xenografts) and female C.B-17 SCID-beige mice (RS4;11 and Toledo xenografts)
  • 投薬量: ~100 mg/kg
  • 投与方法: Orally
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (115.14 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+50% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 868.44
化学式

C45H50ClN7O7S

CAS No. 1257044-40-8
Storage powder
in solvent
別名 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

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    Could you please offer some advice on the half-life of the drug ?

  • 回答:

    According to the reference (https://www.ncbi.nlm.nih.gov/pubmed/24212376), the half-life of ABT-199 in dogs is 12.9 hr.

  • 質問2:

    how to prepare the working solution for mice including how to dissolve the powder?

  • 回答:

    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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