Venetoclax (ABT-199)

For research use only. Not for use in humans.

目录号:S8048 别名: GDC-0199

Venetoclax (ABT-199) Chemical Structure

CAS No. 1257044-40-8

Venetoclax (ABT-199, GDC-0199)是一种Bcl-2选择性抑制剂,无细胞试验中Ki为<0.01 nM,比作用于Bcl-xL和Bcl-w选择性高4800倍以上,对Mcl-1没有抑制活性。有研究证明 Venetoclax 在三阴性乳腺癌 MDA-MB-231 细胞中诱导细胞生长抑制,凋亡,细胞周期停滞和自噬。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 5561.46 现货
RMB 2196.04 现货
RMB 7942.49 现货
RMB 24488.39 现货
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客户使用Selleck生产的Venetoclax (ABT-199)发表文献439篇:

产品安全说明书

Bcl-2抑制剂选择性比较

生物活性

产品描述 Venetoclax (ABT-199, GDC-0199)是一种Bcl-2选择性抑制剂,无细胞试验中Ki为<0.01 nM,比作用于Bcl-xL和Bcl-w选择性高4800倍以上,对Mcl-1没有抑制活性。有研究证明 Venetoclax 在三阴性乳腺癌 MDA-MB-231 细胞中诱导细胞生长抑制,凋亡,细胞周期停滞和自噬。Phase 3。
特性 ABT-263 (Navitoclax)的重组
靶点
Bcl-2 [1]
(Cell-free assay)
<0.01 nM(Ki)
体外研究

ABT-199 对Bcl-xL, Mcl-1 和Bcl-w具有低的敏感性,Ki分别为48 nM, >444 nM 和 245 nM。ABT-199 有效抑制FL5.12-Bcl-2 细胞, RS4;11细胞, EC50分别为4 nM 和 8 nM,作用于 FL5.12-Bcl-xL细胞具有低活性,EC50为261 nM。ABT-199 诱导RS4;11 细胞快速凋亡,细胞色素c释放,caspase激活,磷脂酰丝氨酸外化,及sub-G0/G1 DNA积累。定量免疫印迹表明,ABT-199对包括NHL,DLBCL,MCL,AML和ALL细胞系的灵敏度,与Bcl-2的表达强烈相关。ABT-199也诱导 CLL 凋亡,平均EC50 为3.0 nM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CS-THL1 MkLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrFTIMzOCCwTR?= MlfMO|IhcA>? MWXEUXNQ MUTJcohq[mm2czDj[YxtKGe{b4f0bEBie3Onc4Pl[EBjgSClZXzsJJZq[WKrbHn0fS=> NULqT3hLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5NVY3QThpPkK1PVE3Pjl6PD;hQi=>
CS-THL1 M{O0eWFxd3C2b4TpZ{BCe3OjeR?= MW[yOUBvVQ>? M1X2fWROW09? NHLZV4dKdmS3Y3XzJIFxd3C2b4Ppdy=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTlzNk[5PEc,OjV7MU[2PVg9N2F-
DoGKiT NGHme2tCeG:ydH;0bYMhSXO|YYm= NYfKSFNjPTBibl2= NWTxNIJQTE2VTx?= NH\vXGZKdmS3Y3XzJIFxd3C2b4Ppdy=> NXKySlduRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5NVY3QThpPkK1PVE3Pjl6PD;hQi=>
RS4-11 M1ew[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jZRVczKGh? NWHPTplQUUN3ME2wMlA1ODJizszN M4[xdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkS5O|Y5Lz5{NU[0PVc3QDxxYU6=
NALM-6 MnLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXBSZR[PzJiaB?= MXzJR|UxRjNizszN MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ2OUe2PEc,OjV4NEm3Olg9N2F-
SU-DHL-6 NYHTb5BTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\FN|AvQCEQvF2= NG\J[G9KdmirYnn0d{Bk\WyuIHfyc5d1cCCjc4Pld5Nm\CCkeTDj[YxtKH[rYXLpcIl1gQ>? MoraQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUC4NFMoRjJ3NUmwPFA{RC:jPh?=
OCI-Ly19 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjC[XB2OSEQvF2= M1fqPWlvcGmkaYTzJINmdGxiZ4Lve5RpKGG|c3Xzd4VlKGK7IHPlcIwhfmmjYnnsbZR6 NHfCWmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW5NFgxOyd-MkW1PVA5ODN:L3G+
SU-DHL-6 MVPGeY5kfGmxbjDBd5NigQ>? M4nQUlAvPzVizszN NEPKV5AyQCCq MXnJcoNz\WG|ZYOgdJJwNXO3co\peoFtKHC{b4TlbY4hVUOOLUGg[ZhxemW|c3nvci=> MoLXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUC4NFMoRjJ3NUmwPFA{RC:jPh?=
KCL22 M3Wwb2Z2dmO2aX;uJGF{e2G7 NV\vR4RrOiEQvF2= NX;ROnQyPDhiaB?= MXLEUXNQ M3\4dGlv[3KnYYPld{BFVkFiZoLh[4Fu\W62YYTpc44> MlrLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{OyOVIoRjJ3M{OzNlUzRC:jPh?=
LOUCY NHXFOYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrRNVAh|ryP MoXOOFghcA>? MYHEUXNQ MorJTWM2OD1yLkCxN|kh|ryP MlLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
ALL-SIL NIPzclJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljPNVAh|ryP NXezcIFMPDhiaB?= MW\EUXNQ NIGySotKSzVyPUCuNVgxOyEQvF2= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
CUTLL1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\YNVAh|ryP NGfPeZU1QCCq NXr3SpVrTE2VTx?= M2D1SWlEPTB;MD6zPFI{KM7:TR?= NF;SUZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
KOPTK1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zNXFExKM7:TR?= MoKxOFghcA>? MlLTSG1UVw>? MoH2TWM2OD1yLk[0N|Ih|ryP MknuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEG3NFQoRjJ3M{CxO|A1RC:jPh?=
DND-41 NEjy[XhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSxNEDPxE1? NV;JcppHPDhiaB?= NUXKUI9KTE2VTx?= M1zEWGlEPTB;MT65Olk2KM7:TR?= NYHDVVFiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNFE4ODRpPkK1N|AyPzB2PD;hQi=>
PF-382 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPVNVAh|ryP NVLLOYQ2PDhiaB?= MXvEUXNQ Ml2yTWM2OD1{LkG4NlQh|ryP NFLvdnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwNVcxPCd-MkWzNFE4ODR:L3G+
KARPAS-45 NFjLdmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HrVFExKM7:TR?= MVm0PEBp NWPhWHk1TE2VTx?= NHO5[G1KSzVyPUOuNlIzPSEQvF2= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyMUewOEc,OjV|MEG3NFQ9N2F-
PEER NWDQZllYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUeyVYJ{OTBizszN NYfUXYsxPDhiaB?= NXfqbGM5TE2VTx?= NHnQN|RKSzVyPUSuOlQxOyEQvF2= M{PZcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{CxO|A1Lz5{NUOwNVcxPDxxYU6=
CX-1 NV;xcGF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;BfHpuOTByIN88US=> NHO0ZnQ4OiCq MUfJR|UxRTZwNzFOwG0> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJyOEi4Nkc,OjV{MEi4PFI9N2F-
LS147T NEiyN21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\aXWx3OTByIN88US=> NUnmZ5RqPzJiaB?= NVnRUZBvUUN3ME2yPU42KM7:TR?= NY[2dmg5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNFg5QDJpPkK1NlA5QDh{PD;hQi=>
HL-60 NVTL[nB3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYKyUGEzPDhiaB?= MY\JR|UxRDFizszN NFyzfXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
MOLM-13 MoXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHkS4ZkPDhiaB?= NIj6UnRKSzVyPEGg{txO MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NkGxOkc,OjR|NE[xNVY9N2F-
OCI-AML2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWm0PEBp NVrLdFM6UUN3MEyxJO69VQ>? NHK2dXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
Kasumi-1 NGPxfXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzLZnA{PDhiaB?= MWnJR|UxRDFizszN Mne0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NE[xNVYoRjJ2M{S2NVE3RC:jPh?=
KG-1 NHPFR5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfEZmVxPDhiaB?= NHfufYJKSzVyPEGg{txO NWrVVHJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFYyOTZpPkK0N|Q3OTF4PD;hQi=>
THP-1 NXjW[2RHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHf5Vos1QCCq MlP3TWM2ODxzIN88US=> NGjhTHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0OlEyPid-MkSzOFYyOTZ:L3G+
MOLM-14 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHMOFghcA>? MXjJR|UxRDFizszN M4raWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
MOLM-13 MojSRZBweHSxdHnjJGF{e2G7 MlfmOVAhdk1? MYiyOEBp MUDBdI9xfG:|aYOgbY5lfWO2aX;u M3rQdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S2NVE3Lz5{NEO0OlEyPjxxYU6=
HSB NH;seXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LGelExKM7:TR?= MoWzOFghcA>? NYnhSZNVTE2VTx?= NFzIbIVKSzVyPUSuOFQ5KM7:TR?= MkH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEK5OFgoRjJ2M{SyPVQ5RC:jPh?=
MOLT4 M32xO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:0PVUyOCEQvF2= MVK0PEBp MVPEUXNQ MWfJR|UxRTRwMUW0JO69VQ>? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2Mkm0PEc,OjR|NEK5OFg9N2F-
SKW-3/KE-37 NV\2eVlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnaXpJjOTBizszN M4joZVQ5KGh? NIjEVWFFVVOR NWG0UYJyUUN3ME2wMlcyOiEQvF2= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2Mkm0PEc,OjR|NEK5OFg9N2F-
SUPT-11 NHj6TZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYOxNEDPxE1? M1L3bFQ5KGh? Ml\xSG1UVw>? NUTaNFZoUUN3ME20MlQ4OyEQvF2= NHHMOpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0Nlk1QCd-MkSzOFI6PDh:L3G+
JURKAT NHXLT2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TDOVExKM7:TR?= NXfQe5lOPDhiaB?= MX;EUXNQ MXHJR|UxRTRwOEmzJO69VQ>? NXTm[mVtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFI6PDhpPkK0N|QzQTR6PD;hQi=>
CCRF-CEM M4HCd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfCPGgyOCEQvF2= MVi0PEBp NITCXnNFVVOR NInFcohKSzVyPUGuN|YxKM7:TR?= M1rhVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
LOUCY NX;GV3hKSXCxcITveIlkKEG|c3H5 M1nJWFIh|ryP MmrLOFghcA>? MVrEUXNQ MUnBdI9xfG:|aYOgbY5lfWO2aX;u M2HCRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SyPVQ5Lz5{NEO0Nlk1QDxxYU6=
RS4:11 NIHDSVJEgXSxdH;4bYNqfHliYYPzZZk> M{HiNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEC3PVc{Lz5{OUSwO|k4OzxxYU6=
RS4:11 NGLlSJNOXFNiYYPzZZk> NVrGPYM3PzJiaB?= NFrFVW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK3PFM{Oyd-M{CyO|g{OzN:L3G+
RS4:11 NXXB[VRlVVSVIHHzd4F6 NITHdmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEmyOlI1Pyd-Mki5NlYzPDd:L3G+
Toledo M162UW1VWyCjc4PhfS=> MmfWO|IhcA>? NV7DUWhMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyO|g{OzNpPkOwNlc5OzN|PD;hQi=>
NCI60 MWLTVmIh[XO|YYm= MkXnOFghcA>? MmL6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
RS4:11 MWDNWHQh[XO|YYm= MVWyOEBp NHm4OWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS1N|E{PSd-Mkm0OVMyOzV:L3G+
melanoma MnHNV3JDKGG|c3H5 NXLUOYNmPDhiaB?= M4KwelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
leukemia MmnnV3JDKGG|c3H5 MUe0PEBp MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
renal cancer NVXwZ4FEW1KEIHHzd4F6 M3\We|Q5KGh? NVm1SpVpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
non-small cell lung cancer NYHhWG1RW1KEIHHzd4F6 M3;zOlQ5KGh? M2TDflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|YyLz5{N{m5OFc3OTxxYU6=
breast cancer MV3TVmIh[XO|YYm= MljvOFghcA>? MmHxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
colon cancer NEHIPG1UWkJiYYPzZZk> NWLTXHlZPDhiaB?= MknOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
ovarian cancer NWj1eZlsW1KEIHHzd4F6 MUm0PEBp MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEe2NUc,Ojd7OUS3OlE9N2F-
CNS cancer M2DvZnNTSiCjc4PhfS=> MV[0PEBp NY\Ib4NsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4PjFpPkK3PVk1PzZzPD;hQi=>
prostate cancer MVPTVmIh[XO|YYm= NIGwfpc1QCCq MkT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OlEoRjJ5OUm0O|YyRC:jPh?=
Remb1 MmfmUXRVKGG|c3H5 NXjtbpNuOjRiaB?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR3M{GzOUc,Ojl2NUOxN|U9N2F-

... 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
体内研究 ABT-199 (100 mg/kg)处理RS4;11 移植瘤,产生的最大肿瘤生长抑制率为95%,肿瘤生长延迟152%。ABT-199单独处理或与SDX-105及其他药剂联用处理DoHH2和Granta-519移植瘤,也抑制肿瘤生长。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

亲和力分析:

竞争性荧光偏振检测测定ABT-199对Bcl-2家族的不同亚型的亲和力(Ki 或 IC50)。使用如下肽探针/蛋白对:f-bad (1 nM) 与Bcl-xL (6 nM), f-Bax (1 nM) 与 Bcl-2 (10 nM),f-Bax(1 nM) 与Bcl-w (40 nM), f-Noxa(2 nM) 与Mcl-1 (40 nM), 及 f-Bax (1 nM)与Bcl-2-A1(15 nM)。使用时间分辨荧光共振能量转移检测测定对Bcl-xL的亲和力。Bcl-xL (1 nM, His标记的 ) 与200 nM f-Bak, 1 nM Tb标记的anti-His抗体, 及 ABT-199,在室温下混合30分钟。在Envision酶标仪上,使用340/35 nm 激发滤光片及520/525 (f-Bak) 和495/510 nm (Tb标记的anti-His抗体) 发射滤光片,测量荧光值。
细胞实验:[1]
- 合并
  • Cell lines: NHL, DLBCL, MCL, AML 和 ALL 细胞系
  • Concentrations: ~1 μM
  • Incubation Time: 48 小时
  • Method: RS4;11 细胞按每孔5×104个接种在96孔板中,使用初始1 μM-0.05 nM。在半对数期稀释的ABT-199 处理细胞。白血病和淋巴瘤细胞系按每孔1.5-2×104个接种在合适的培养基中,与ABT-199温育48小时。使用Cell TiterGlo 试剂测定对细胞增殖的影响。通过对浓度-反应数据非线性回归分析测定EC50值。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 雌性 C.B-17 SCID 小鼠(携带DoHH2 和Granta-519 移植瘤) 和雌性 C.B-17 SCID-beige 小鼠 (携带RS4;11和 Toledo 移植瘤)
  • Dosages: ~100 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (115.14 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+50% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 868.44
化学式

C45H50ClN7O7S

CAS号 1257044-40-8
储存条件 粉状
溶于溶剂
别名 GDC-0199

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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.

  • 问题 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.

Bcl-2 Signaling Pathway Map

Bcl-2 Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID