ABT-737

目录号:S1002

仅限科研使用

ABT-737是一种BH3模拟抑制剂,作用于Bcl-xLBcl-2Bcl-w,无细胞试验中EC50分别为78.7 nM,30.3 nM和197.8 nM;但对Mcl-1, Bcl-B及Bfl-1没有抑制作用。ABT-737可诱导线粒体通路的凋亡和线粒体自噬。Phase 2。

ABT-737 Chemical Structure

CAS: 852808-04-9

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 3144.65 现货
RMB 972.14 现货
RMB 4659.22 现货
大包装 有超大折扣
大剂量询单有大折扣!

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的ABT-737发表文献334篇:

产品安全说明书

Bcl-2抑制剂选择性比较

相关Bcl-2产品

生物活性

产品描述 ABT-737是一种BH3模拟抑制剂,作用于Bcl-xLBcl-2Bcl-w,无细胞试验中EC50分别为78.7 nM,30.3 nM和197.8 nM;但对Mcl-1, Bcl-B及Bfl-1没有抑制作用。ABT-737可诱导线粒体通路的凋亡和线粒体自噬。Phase 2。
特性 ABT-737是第一代抗凋亡BCL-2家族蛋白小分子抑制剂。
靶点
Bcl-2 [1]
(Cell-free assay)
Bcl-xL [1]
(Cell-free assay)
Bcl-w [1]
(Cell-free assay)
Bcl-B [1]
(Cell-free assay)
30.3 nM(EC50) 78.7 nM(EC50) 197.8 nM(EC50) 1.82 μM(EC50)
体外研究

ABT-737降低BCL-2/BAX异质二聚体,而诱导HL60细胞凋亡,但是对细胞周期分布没有抑制效果。ABT-737也诱导细胞色素C从线粒体中释放,促进BAX构象改变,BAX与凋亡相关。在白血病模型中,ABT-737按30 mg/kg处理,阻断53%白血病负荷,且使鼠寿命明显延长。ABT-737不会导致血细胞数和血清组成发生异常。[1]通过使Mcl-1失活而使抵抗细胞(Hela和MCF-7)对ABT-737敏感。当Mcl-1无效时,ABT-737也导致BAX/BAK-依赖的细胞色素C释放。ABT-737延长携带BCL-2肿瘤的鼠寿命。[2]ABT-737从BCL2’s BH3结合袋取代BIM,使BIM激活BAX,诱导线粒体透化作用,快速致死慢性淋巴细胞性白血病(CLL)细胞。[3] Noxa正向调节增强H196细胞对ABT-737敏感性。ABT-737抑制多种SCLC细胞系,包括NCI-H889, NCI-H1963, NCI-H1417, NCI-H146等的增殖,并诱导细胞凋亡。最近研究显示,ABT-737作用于ATLL细胞,明显诱导HTLV-1感染的T细胞凋亡。ABT-737按100 mg/kg剂量作用于ATLL鼠模型显示出强抗癌活性。[5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
OCI-Ly1  MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnnGNlUxKG6PwrC= NFvKNJM4OiCq MYTEUXNQ NIPXdVBk[XW|ZXSgPVcmKGyxc4Ogc4YhfmmjYnnsbZR6KGmwIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSkOONjDzbXJPSQ>? M{PNO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkW3Nlg5Lz5{Nk[1O|I5QDxxYU6=
KG1a NEfQW5RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlvyNE0yOCEQvF2= NYXBXYVvOjRiaB?= NELZfJBFVVOR NH;CfnFKSzVyPUeuOlgh|ryPLDDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M2XNT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUWyO|EzLz5{NkW1NlcyOjxxYU6=
Kasumi-1 NFfHdYhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEXldJQxNTFyIN88US=> MVqyOEBp NYnZepZ6TE2VTx?= NG\nfVdKSzVyPUSuPFch|ryPLDDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NUK3NVIoRjJ4NUWyO|EzRC:jPh?=
KG1a M3zIPGFxd3C2b4Ppd{BCe3OjeR?= M2Ln[|AuOTBizszN NFzVSFczPCCq NWnBfJhxTE2VTx?= MYXpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWDPPHpuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OVI4OTJpPkK2OVUzPzF{PD;hQi=>
Kasumi-1 NIX4dXVCeG:ydH;zbZMhSXO|YYm= M2fh[VAuOTBizszN NGTxNIEzPCCq MWfEUXNQ MVTpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV3MkexNkc,OjZ3NUK3NVI9N2F-
MC-3  MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHaOU8yOC9{MDFOwG0> M4mzRlI1KGh? NIfCPXNFVVOR NWr0fGticW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR2N{[xOUc,OjZ2NEe2NVU9N2F-
HN22  NUH5V2ZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrZTFAzNjVxNz61M|IzNjVizszN MWeyOEBp NY\ud4xPTE2VTx?= NVq1R5pwcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYHvXWlXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0OFc3OTVpPkK2OFQ4PjF3PD;hQi=>
MC-3  NHXsV|ZCeG:ydH;zbZMhSXO|YYm= NYf5PHNoPS9zMD:yNEDPxE1? NFvlTFAzPCCq NFq3TIZFVVOR MWrpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| NXTQcYZ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0OFc3OTVpPkK2OFQ4PjF3PD;hQi=>
HN22  NF:5O5NCeG:ydH;zbZMhSXO|YYm= M{jW[|IvPS95LkWvNlIvPSEQvF2= M4PqSFI1KGh? MWXEUXNQ MV\pcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| NFSxNVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkS0O|YyPSd-Mk[0OFc3OTV:L3G+
MOLT-4 M37ibWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLyNVAuPTByMDDuUS=> MXW3NkBp NHLldXFFVVOR M4rDWWlEPTB;MD6xPVgh|ryP Ml;SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUKzN|IoRjJ4M{myN|MzRC:jPh?=
RS4;11 NHK3U2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDh[pp[OTBvNUCwNEBvVQ>? NUXuc41kPzJiaB?= NFH3[ldFVVOR MmnITWM2OD1yLkCwNkDPxE1? M4jV[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN|MzLz5{NkO5NlM{OjxxYU6=
JURKAT MlnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\zVHpMOTBvNUCwNEBvVQ>? NXnjZmxOPzJiaB?= M37GU2ROW09? NWXDeodLUUN3ME22OkDPxE1? M{f0TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN|MzLz5{NkO5NlM{OjxxYU6=
CEM R M3fmZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzWR4YyOC13MECwJI5O NHXLTHU4OiCq MofUSG1UVw>? NXvlOWM4UUN3ME21MlQh|ryP M1:3fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN|MzLz5{NkO5NlM{OjxxYU6=
CEM S NETNO3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn6UWVZOTBvNUCwNEBvVQ>? M2K2VVczKGh? MVfEUXNQ MXXJR|UxRTF{LkGg{txO Ml;JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUKzN|IoRjJ4M{myN|MzRC:jPh?=
MOLT-4 MVHBdI9xfG:|aYOgRZN{[Xl? NWrCO2dXOTBvMUCwNEBvVQ>? NEfjPHUzPCCq M4S1cGROW09? MkfMZ4F2e2W|IITo[UBkdGWjdnHn[UBw\iCEY3ytNkBidmRidHjlJIRwf26{ZXf1cIF1cW:wIH;mJGJkdC26TDDhcoQhVWOuLUG= NGL4OFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NlM{Oid-Mk[zPVI{OzJ:L3G+
CEM S MWLBdI9xfG:|aYOgRZN{[Xl? NYi3cWs2OTBvMUCwNEBvVQ>? M3nONVI1KGh? NYDKem1ETE2VTx?= NX\2XoJ5[2G3c3XzJJRp\SClbHXheoFo\SCxZjDCZ4wuOiCjbnSgeIhmKGSxd37y[Yd2dGG2aX;uJI9nKEKlbD34UEBidmRiTXPsMVE> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MkOzNkc,OjZ|OUKzN|I9N2F-
JURKAT NVHnNm1qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTjNVAxNTFyMECgcm0> NHXvVnA1QCCq NYfxWphqTE2VTx?= MoPJTWM2OD17NUZCtVkvOyCwTR?= Mnj5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzN{KyOlkoRjJ4MUeyNlY6RC:jPh?=
LOUCY NYfaUpRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\hSJEyODBvMUCwNEBvVQ>? MUK0PEBp NW\pcHozTE2VTx?= MXrJR|UxRTN{LklCtVExNjlibl2= M4jVclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUeyNlY6Lz5{NkG3NlI3QTxxYU6=
WM-115 MojsR4VtdCCYaXHibYxqfHliQYPzZZk> NYLpXnh5OTBywrDuUS=> M4r5eFczKGh? M4HNdoVvcGGwY3XzJIN2emO3bXnuMYlv\HWlZXSgZY51cS2|dYL2bZZidMLi MlTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[3O|YoRjJ4MUG2O|c3RC:jPh?=
B16 NHj2NoJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEKy[ogyODEEoH7N M4izS|czKGh? MVrlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? NX6xW2NURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVY4PzZpPkK2NVE3Pzd4PD;hQi=>
HL-60  MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIe1WG84OiCq NX[2VnpFUUN3MNMgQUAyOC55IH7N NV3qeGllRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOFU3ODlpPkK2NFQ2PjB7PD;hQi=>
MOLM-13  M4LScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13oSFczKGh? MmLZTWM2OMLiPTCyO{46KG6P MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB2NU[wPUc,OjZyNEW2NFk9N2F-
OCI-AML3 Mm\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\iVmU4OiCq NHnkOFRKSzVywrC9JFE6PTBibl2= NET1W5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0OVYxQSd-Mk[wOFU3ODl:L3G+
BCWM.1 MVfBdI9xfG:|aYOgRZN{[Xl? MoLTNE0yNjZizszN MXuyOEBp NGXZd2FqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MmDvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6OUOyPVAoRjJ3OEmzNlkxRC:jPh?=
MWCL-1 MWTBdI9xfG:|aYOgRZN{[Xl? MX6wMVEvPiEQvF2= NHrweVIzPCCq NUTz[2JmcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NX\yT|hmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4PVMzQTBpPkK1PFk{OjlyPD;hQi=>
MM.1s NE\ne5BCeG:ydH;zbZMhSXO|YYm= NIHJdo4xNTFwNjFOwG0> NULSe2NXOjRiaB?= MXjpcoR2[2W|IHPlcIwh[XCxcITvd4l{ M3nGOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEmzNlkxLz5{NUi5N|I6ODxxYU6=
HCT116 M4fyemZ2dmO2aX;uJGF{e2G7 M1;YT|MwOTBizszN NUDSNZU4OTMEoHlCpC=> NHHkO25FVVOR Mkn5bY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGxEO0JvSVmgZ49vfmW{c3nvckBidmRiU2HTWG0yKGSnZ4Lh[IF1cW:w NHrLTos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
HCT116 BAX BAK1 DKO MVHGeY5kfGmxbjDBd5NigQ>? M1GzeVMwOTBizszN NWDJdXF{OTMEoHlCpC=> MmXNSG1UVw>? MULpcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? NG\jd2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
HCT116 NV3yTZhVTnWwY4Tpc44hSXO|YYm= MkPrNVAh|ryP M2nI[lEzyqCqwrC= NIrGdIdFVVOR M13BXYlv[3KnYYPld{BITlBvTFOzRkBxfW6ldHG= Mmr4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUWwNlgoRjJ3N{G1NFI5RC:jPh?=
HCT116 BAX BAK1 DKO M3vhbmZ2dmO2aX;uJGF{e2G7 NXPVZmJTOTBizszN M3\iZVEzyqCqwrC= MljaSG1UVw>? NILidFlqdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th NXzZVVZrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVUxOjhpPkK1O|E2ODJ6PD;hQi=>
HCT116 MWHBeZRweGijZ4mgRZN{[Xl? NHPrfWsyOCEQvF2= NFnheYUyOsLiaNMg NHnWd4pFVVOR MkGzbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> MnLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUWwNlgoRjJ3N{G1NFI5RC:jPh?=
HCT116 BAX BAK1 DKO NYHpV4dkSXW2b4DoZYd6KEG|c3H5 M1r3e|ExKM7:TR?= NGXrNZAyOsLiaNMg M3jhO2ROW09? MoSybY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> Mn\lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUWwNlgoRjJ3N{G1NFI5RC:jPh?=
U937 Mnm3RZBweHSxc3nzJGF{e2G7 M3;veVAvOTJ3LUKg{txO NITqWpkzPCCq NYHlNXBN\W6qYX7j[ZMhTEiDL2itNVEucW6mdXPl[EBieG:ydH;zbZM> NYf3OHpmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVQxOjRpPkK1O|E1ODJ2PD;hQi=>
U937  M1iyTGFxd3C2b4Ppd{BCe3OjeR?= M2DKZ|AvPSEQvF2= M4TmTVI1KGh? NIHlPYNmdmijbnPld{BkdGWjdnHn[UBw\iCSQWLQJIFv\CClYYPwZZNmNTNiYYOge4VtdCCjczDOc5hiKGyndnXs MoPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUSwNlQoRjJ3N{G0NFI1RC:jPh?=
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TC32 M37Gc5FJXFNiYYPzZZk> NH;YUFJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBVSzN{IHPlcIx{ NF:4VW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 MnTjdWhVWyCjc4PhfS=> MW\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFE5KGOnbHzz NX;rVppbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 M3TXNZFJXFNiYYPzZZk> M4rrWJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNid3NvMjDj[Yxtew>? NFq4PJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Assay
Methods Test Index PMID
Western blot PARP / c-PARP / cleaved caspase 3 Hif-1a γ-H2AX / p-ATM 21393866 22006676 21084274
Immunofluorescence cytochrome C Bax Bim AIF p65 26447615 25034785 28846096
Growth inhibition assay Cell viability 22311987
ELISA IL-6 / IL-8 21084274
体内研究 ABT-737按30 mg/kg剂量作用于白血病模型,抑制白血病负担值达53% , 且明显延长鼠寿命。ABT-737不会引起血细胞数和血浆化学性质发生变话。[1] ABT-737延长移植BCL-2传感肿瘤的鼠寿命。[2] ABT-737按100 mg/kg剂量作用于ATLL鼠模型具有强抗癌活性。[5]

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]

  • 荧光偏振实验:

    测定GST-BCL-2蛋白家族与FITC-BIM BH3域结合的亲和力。100 nM GST-BCL-2家族融合蛋白和不同浓度 ABT-737在PBS温育2分钟。然后,加入20 nM FITC-BIM BH3 肽。进行荧光偏振,测定IC50值。

细胞实验:

[4]

  • Cell lines: SCLC细胞系,包括NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR,和DMS114
  • Concentrations: 0.001-10 μM
  • Incubation Time: 48小时
  • Method:

    SCLC细胞在含10%人血浆的 100 μL 组织培养基的96孔培养板上处理48小时,使用MTS测定存活细胞。

动物实验:

[1]

  • Animal Models: 注射ER细胞的Scid 鼠
  • Dosages: 20 mg/kg和30 mg/kg
  • Administration: 腹腔注射

溶解度(25°C)

体外

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):
2%DMSO+40%PEG300+5%Tween80+53%ddH2O

2mg/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 813.43
化学式

C42H45ClN6O5S2

CAS号 852808-04-9
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

技术支持

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操作手册

如果有其他问题,请给我们留言。

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常见问题及建议解决方法

问题 1:
What’s the recommended method about reconstitution of the compound for in vivo animal study?

回答:
For oral administration, we suggest the vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W, at up to 30mg/ml; For injection, ABT-737 can be dissolved in 2% DMSO/50% PEG 300/5% Tween 80/ddH2O at 2.5 mg/ml.