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(450)

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 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfjNlAhdk1? NHHDRVE4OiCq NWLBcXJZTE2VTx?= MnvKTY5pcWKrdIOgZ4VtdCCpcn;3eIgh[XO|ZYPz[YQh[nliY3XscEB3cWGkaXzpeJk> NHT0SYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUmxOlY6QCd-MkW5NVY3QTh:L3G+
CS-THL1 MlO1RZBweHSxdHnjJGF{e2G7 MnXwNlUhdk1? NVn2OFduTE2VTx?= M4HKUGlv\HWlZYOgZZBweHSxc3nz MlfZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7MU[2PVgoRjJ3OUG2Olk5RC:jPh?=
DoGKiT M1rKV2Fxd3C2b4TpZ{BCe3OjeR?= M4\RWVUxKG6P MonOSG1UVw>? NUXP[Gh7UW6mdXPld{BieG:ydH;zbZM> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTlzNk[5PEc,OjV7MU[2PVg9N2F-
RS4-11 MlvLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfyNJNEPzJiaB?= MX\JR|UxRTBwMESwNkDPxE1? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ2OUe2PEc,OjV4NEm3Olg9N2F-
NALM-6 MnnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fPelczKGh? M4nRPWlEPTB-MzFOwG0> MoLBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NEm3OlgoRjJ3NkS5O|Y5RC:jPh?=
SU-DHL-6 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DudlAvQCEQvF2= NHO1emlKdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MmC1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUC4NFMoRjJ3NUmwPFA{RC:jPh?=
OCI-Ly19 NUjTeFcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmCyNUDPxE1? M2O4fWlvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 NVHo[4tZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1PVA5ODNpPkK1OVkxQDB|PD;hQi=>
SU-DHL-6 NVzxe5RzTnWwY4Tpc44hSXO|YYm= MY[wMlc2KM7:TR?= NUnGbI12OThiaB?= M4PH[2lv[3KnYYPld{Bxem9vc4Xyeol3[WxicILveIVqdiCPQ1ytNUBmgHC{ZYPzbY9v MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7MEiwN{c,OjV3OUC4NFM9N2F-
KCL22 M3nMWGZ2dmO2aX;uJGF{e2G7 MnL2NkDPxE1? MofyOFghcA>? MoHESG1UVw>? MUHJcoNz\WG|ZYOgSG5CKG[{YXfhcYVvfGG2aX;u MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN|M{K1Nkc,OjV|M{OyOVI9N2F-
LOUCY MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOxNEDPxE1? NIL4XoI1QCCq NGTVO5JFVVOR MUfJR|UxRTBwMEGzPUDPxE1? NEKxboY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
ALL-SIL NUj3SpdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUKxNEDPxE1? MXW0PEBp NIjUdJhFVVOR MmrxTWM2OD1yLkG4NFMh|ryP Mm\UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
CUTLL1 MoLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELLeZoyOCEQvF2= NXrJ[pY4PDhiaB?= MmWxSG1UVw>? M3zQW2lEPTB;MD6zPFI{KM7:TR?= MojyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
KOPTK1 NVXnbYM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYn3UVh2OTBizszN MVq0PEBp MmLTSG1UVw>? MWPJR|UxRTBwNkSzNkDPxE1? NXHYdpplRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNFE4ODRpPkK1N|AyPzB2PD;hQi=>
DND-41 MmLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TaPFExKM7:TR?= Ml2wOFghcA>? NUHRTmttTE2VTx?= MljPTWM2OD1zLkm2PVUh|ryP NGWwRZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
PF-382 NIrldWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7nNVAh|ryP NFjIToI1QCCq NYHKT|I6TE2VTx?= MmnETWM2OD1{LkG4NlQh|ryP M3fleVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{CxO|A1Lz5{NUOwNVcxPDxxYU6=
KARPAS-45 NVPFSJlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOxNEDPxE1? MkK3OFghcA>? M13UdWROW09? MojvTWM2OD1|LkKyNlUh|ryP M2DGblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{CxO|A1Lz5{NUOwNVcxPDxxYU6=
PEER MnzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{juWlExKM7:TR?= MWq0PEBp M1HtfWROW09? NU\oWmpjUUN3ME20MlY1ODNizszN MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
CX-1 NGDxSlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[xNFAh|ryP NX3BRnZVPzJiaB?= MXPJR|UxRTZwNzFOwG0> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJyOEi4Nkc,OjV{MEi4PFI9N2F-
LS147T Mo\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUO5W2ZtOTByIN88US=> MnTtO|IhcA>? NU\a[oRHUUN3ME2yPU42KM7:TR?= Mn;IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MEi4PFIoRjJ3MkC4PFgzRC:jPh?=
HL-60 M37BUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHHcVY1QCCq MYDJR|UxRDFizszN M3X1R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
MOLM-13 NIrUe3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\UblQ5KGh? Mk[xTWM2ODxzIN88US=> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
OCI-AML2 NU\rU3p3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\oOFghcA>? NIDNXlFKSzVyPEGg{txO NHHNRlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
Kasumi-1 M4ewNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvlOFghcA>? NEm1O2dKSzVyPEGg{txO M2niblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
KG-1 MkToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTBN3M{PDhiaB?= NEO2XHlKSzVyPEGg{txO NEX0TJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
THP-1 Mmf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\1fFQ5KGh? MnrFTWM2ODxzIN88US=> NX33XmJMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
MOLM-14 NFfSNopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTCNXc1QCCq NX7aOlNmUUN3MEyxJO69VQ>? NFLyOHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
MOLM-13 NGO1R4JCeG:ydH;0bYMhSXO|YYm= M3PQNFUxKG6P MmTJNlQhcA>? MormRZBweHSxc3nzJIlv\HWldHnvci=> NHvMTWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
HSB M3zUTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrlWGVmOTBizszN M4rF[VQ5KGh? MX;EUXNQ M{HmTWlEPTB;ND60OFgh|ryP M2LtNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
MOLT4 NYLnfFFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGe0fZEyOCEQvF2= MYW0PEBp MlLXSG1UVw>? MnHGTWM2OD12LkG1OEDPxE1? M{LScFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
SKW-3/KE-37 NXnr[mVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jDflExKM7:TR?= NGLlcGg1QCCq Ml7DSG1UVw>? MYXJR|UxRTBwN{GyJO69VQ>? NGi1TmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
SUPT-11 M3;qOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOxNEDPxE1? NETlclg1QCCq NFLHcmNFVVOR MkHWTWM2OD12LkS3N{DPxE1? M1jaT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
JURKAT NWL2emhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLCdGoyOCEQvF2= M1zsSlQ5KGh? M1;0SWROW09? M3z2OWlEPTB;ND64PVMh|ryP MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2Mkm0PEc,OjR|NEK5OFg9N2F-
CCRF-CEM NUfzRndvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlq4NVAh|ryP Mo\COFghcA>? NILmN45FVVOR MXHJR|UxRTFwM{[wJO69VQ>? NHPKb2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
LOUCY NFjFdWJCeG:ydH;0bYMhSXO|YYm= M4nMS|Ih|ryP MkPJOFghcA>? NILmNoxFVVOR MkTpRZBweHSxc3nzJIlv\HWldHnvci=> MlvMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEK5OFgoRjJ2M{SyPVQ5RC:jPh?=
RS4:11 M4\kRWN6fG:2b4jpZ4l1gSCjc4PhfS=> MonXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2MEe5O|MoRjJ7NEC3PVc{RC:jPh?=
RS4:11 M3HEdG1VWyCjc4PhfS=> NX7oTJozPzJiaB?= M1;tNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMke4N|M{Lz5|MEK3PFM{OzxxYU6=
RS4:11 M2rHbG1VWyCjc4PhfS=> M1HYOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUK2NlQ4Lz5{OEmyOlI1PzxxYU6=
Toledo M4rOd21VWyCjc4PhfS=> MljCO|IhcA>? NUWzeYJ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyO|g{OzNpPkOwNlc5OzN|PD;hQi=>
NCI60 NILRVJJUWkJiYYPzZZk> MV20PEBp MnPPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
RS4:11 NEL1eoROXFRiYYPzZZk> NX;jenJsOjRiaB?= Ml;tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NUOxN|UoRjJ7NEWzNVM2RC:jPh?=
melanoma M{fsW3NTSiCjc4PhfS=> NVe4c5BtPDhiaB?= M2C3Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
leukemia MVXTVmIh[XO|YYm= M1vLfFQ5KGh? M1q3NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
renal cancer MonmV3JDKGG|c3H5 MnPtOFghcA>? Ml3BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
non-small cell lung cancer MVXTVmIh[XO|YYm= NIT6eow1QCCq M{DmXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
breast cancer M1mxb3NTSiCjc4PhfS=> MX:0PEBp NXLubnhXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
colon cancer M3PDfnNTSiCjc4PhfS=> NGfsZm41QCCq NFH4bWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc3OSd-Mke5PVQ4PjF:L3G+
ovarian cancer MWrTVmIh[XO|YYm= NEXzV|U1QCCq MmjaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
CNS cancer MX7TVmIh[XO|YYm= NXfBZ5ZyPDhiaB?= Mmq0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
prostate cancer NGjwXZRUWkJiYYPzZZk> MVu0PEBp MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
Remb1 M{e3VG1VXCCjc4PhfS=> NGrNNmIzPCCq MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR3M{GzOUc,Ojl2NUOxN|U9N2F-

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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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