ABT-737

For research use only. Not for use in humans.

目录号:S1002

ABT-737 Chemical Structure

CAS No. 852808-04-9

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。

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
RMB 7964.03 现货
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客户使用Selleck生产的ABT-737发表文献299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 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  NUXONGhCS2WubDDWbYFjcWyrdImgRZN{[Xl? NUTWelVIOjVyIH7NxsA> NWL0N2poPzJiaB?= MUHEUXNQ NXe3epZL[2G3c3XkJFk4LSCub4PzJI9nKH[rYXLpcIl1gSCrbjDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEKFTE[gd4lTVkF? NXnHW2tZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVczQDhpPkK2OlU4Ojh6PD;hQi=>
KG1a MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkW5NE0yOCEQvF2= M1zOfVI1KGh? Ml\PSG1UVw>? M3XEbGlEPTB;Nz62PEDPxE1uIHTlZ5Jm[XOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3O3clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUWyO|EzLz5{NkW1NlcyOjxxYU6=
Kasumi-1 NHLxb5JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFrDbHoxNTFyIN88US=> MmfiNlQhcA>? MkDFSG1UVw>? NEjiRpBKSzVyPUSuPFch|ryPLDDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHvCbZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW1NlcyOid-Mk[1OVI4OTJ:L3G+
KG1a NGj2b2JCeG:ydH;zbZMhSXO|YYm= NWHKU3ZVOC1zMDFOwG0> NGTDfWwzPCCq MknmSG1UVw>? M2nGdYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NX;jeG5sRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OVI4OTJpPkK2OVUzPzF{PD;hQi=>
Kasumi-1 NHvNZXBCeG:ydH;zbZMhSXO|YYm= NEnQemExNTFyIN88US=> MoH4NlQhcA>? MVPEUXNQ NEe5ZY9qdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MofkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NUK3NVIoRjJ4NUWyO|EzRC:jPh?=
MC-3  M3[wfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LS[VUwOTBxMkCg{txO NEnyVIszPCCq M2nkVWROW09? MYPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYmwXIR[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0OFc3OTVpPkK2OFQ4PjF3PD;hQi=>
HN22  NFPvOplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVeyMlUwPy53L{KyMlUh|ryP M3f3cFI1KGh? M4[1[mROW09? MYDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mo\wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2NEe2NVUoRjJ4NES3OlE2RC:jPh?=
MC-3  M2\6O2Fxd3C2b4Ppd{BCe3OjeR?= M3rJWVUwOTBxMkCg{txO NUnPV4tzOjRiaB?= MnjISG1UVw>? M3j1ZYlv\HWlZYOgZ4F{eGG|ZT3t[YRq[XSnZDDhdI9xfG:|aYO= Ml3VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2NEe2NVUoRjJ4NES3OlE2RC:jPh?=
HN22  M{OwO2Fxd3C2b4Ppd{BCe3OjeR?= M2f2T|IvPS95LkWvNlIvPSEQvF2= NXrTU5lpOjRiaB?= NH75eIVFVVOR NX3BW5ZXcW6mdXPld{Bk[XOyYYPlMY1m\GmjdHXkJIFxd3C2b4Ppdy=> NHj0ZWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkS0O|YyPSd-Mk[0OFc3OTV:L3G+
MOLT-4 NVHWcoVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TUdVExNTVyMECgcm0> Mli2O|IhcA>? NX3WVFdtTE2VTx?= NVLnNlVRUUN3ME2wMlE6QCEQvF2= NH;0eWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NlM{Oid-Mk[zPVI{OzJ:L3G+
RS4;11 MmWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXIc2wyOC13MECwJI5O MmrUO|IhcA>? MoXuSG1UVw>? NVLvVFVrUUN3ME2wMlAxOiEQvF2= M1rlfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN|MzLz5{NkO5NlM{OjxxYU6=
JURKAT MlW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILESVgyOC13MECwJI5O Ml3kO|IhcA>? M2TLbWROW09? MnH4TWM2OD14NjFOwG0> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MkOzNkc,OjZ|OUKzN|I9N2F-
CEM R Ml;pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlT2NVAuPTByMDDuUS=> MlmwO|IhcA>? NFTOZnlFVVOR Ml7KTWM2OD13LkSg{txO MlLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUKzN|IoRjJ4M{myN|MzRC:jPh?=
CEM S MmPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmP6NVAuPTByMDDuUS=> M3z0R|czKGh? NGH2UHdFVVOR M3\VT2lEPTB;MUKuNUDPxE1? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MkOzNkc,OjZ|OUKzN|I9N2F-
MOLT-4 NFXYOFJCeG:ydH;zbZMhSXO|YYm= M2LTcFExNTFyMECgcm0> NGK3dm4zPCCq M1jNbWROW09? M4TGV4NifXOnczD0bIUh[2ynYY\h[4Uhd2ZiQnPsMVIh[W6mIITo[UBld3ewcnXneYxifGmxbjDv[kBD[2xveFygZY5lKE2lbD2x M2fkcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{myN|MzLz5{NkO5NlM{OjxxYU6=
CEM S MV;BdI9xfG:|aYOgRZN{[Xl? MXmxNE0yODByIH7N NIDU[nkzPCCq Mm\TSG1UVw>? NUHTSGNS[2G3c3XzJJRp\SClbHXheoFo\SCxZjDCZ4wuOiCjbnSgeIhmKGSxd37y[Yd2dGG2aX;uJI9nKEKlbD34UEBidmRiTXPsMVE> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MkOzNkc,OjZ|OUKzN|I9N2F-
JURKAT NGfTb|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTFNVAxNTFyMECgcm0> M3:yTlQ5KGh? MYHEUXNQ NY\vVlZVUUN3ME25OVXDuTlwMzDuUS=> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF5MkK2PUc,OjZzN{KyOlk9N2F-
LOUCY NXu5RlhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWexNFAuOTByMDDuUS=> MnHuOFghcA>? M2LmdGROW09? Mn3RTWM2OD1|Mj64xtEyOC57IH7N NFfMXIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG3NlI3QSd-Mk[xO|IzPjl:L3G+
WM-115 Ml3yR4VtdCCYaXHibYxqfHliQYPzZZk> M3u0c|ExOMLibl2= M1[wdlczKGh? NFf3cW5mdmijbnPld{BkfXKldX3pck1qdmS3Y3XkJIFvfGlvc4Xyeol3[W{EoB?= NGT1cHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlc4Pid-Mk[xNVY4PzZ:L3G+
B16 M2TzbWNmdGxiVnnhZoltcXS7IFHzd4F6 NGPxOlEyODEEoH7N MlPTO|IhcA>? M{WwdYVvcGGwY3XzJIN2emO3bXnuMYlv\HWlZXSgZY51cS2|dYL2bZZidMLi MoPQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[3O|YoRjJ4MUG2O|c3RC:jPh?=
HL-60  NX3jWnF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;lO|IhcA>? NGfIVIhKSzVywrC9JFExNjdibl2= MnnOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNEW2NFkoRjJ4MES1OlA6RC:jPh?=
MOLM-13  NVvJT|JPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LpeFczKGh? NXvBelBTUUN3MNMgQUAzPy57IH7N NV32TGt2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOFU3ODlpPkK2NFQ2PjB7PD;hQi=>
OCI-AML3 MonmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrCdZVtPzJiaB?= MW\JR|UxyqB;IEG5OVAhdk1? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB2NU[wPUc,OjZyNEW2NFk9N2F-
BCWM.1 MlXsRZBweHSxc3nzJGF{e2G7 NXzMPXRvOC1zLk[g{txO M1O1VFI1KGh? M1XI[Ilv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MoOzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6OUOyPVAoRjJ3OEmzNlkxRC:jPh?=
MWCL-1 MlTRRZBweHSxc3nzJGF{e2G7 MnfpNE0yNjZizszN MmOwNlQhcA>? NH3xXVhqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh7M{K5NEc,OjV6OUOyPVA9N2F-
MM.1s MX3BdI9xfG:|aYOgRZN{[Xl? NF\FWFIxNTFwNjFOwG0> MkHqNlQhcA>? NUL6fpp4cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NW\lb|BQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4PVMzQTBpPkK1PFk{OjlyPD;hQi=>
HCT116 NVvrRpF5TnWwY4Tpc44hSXO|YYm= NVvIWHYyOy9zMDFOwG0> MlOyNVLDqGkEoB?= NF[yOXhFVVOR NVfaVHR2cW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEyFM1KtTWkh[2:wdnXyd4lwdiCjbnSgV3FUXE1zIHTl[5Ji\GG2aX;u MnjLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUWwNlgoRjJ3N{G1NFI5RC:jPh?=
HCT116 BAX BAK1 DKO MXnGeY5kfGmxbjDBd5NigQ>? MnvpN{8yOCEQvF2= NUjadYlJOTMEoHlCpC=> MV3EUXNQ MV\pcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? M4jBSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{G1NFI5Lz5{NUexOVAzQDxxYU6=
HCT116 NYXqbW5VTnWwY4Tpc44hSXO|YYm= NF[0W|IyOCEQvF2= MVqxNuKhcMLi M4rkRWROW09? NW\EdmlUcW6lcnXhd4V{KEeIUD3MR|NDKHC3bnP0ZS=> NWL4OnBxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVUxOjhpPkK1O|E2ODJ6PD;hQi=>
HCT116 BAX BAK1 DKO M3PheGZ2dmO2aX;uJGF{e2G7 NUjZc4sxOTBizszN MkPJNVLDqGkEoB?= NIDvT29FVVOR NEnv[m9qdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th NF22UVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUexOVAzQCd-MkW3NVUxOjh:L3G+
HCT116 M4PtT2F2fG:yaHHnfUBCe3OjeR?= MnywNVAh|ryP NUXW[nVlOTMEoHlCpC=> MYnEUXNQ MWTpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{Bz\XOyb37z[S=> NXrVd2o1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVUxOjhpPkK1O|E2ODJ6PD;hQi=>
HCT116 BAX BAK1 DKO NEP1[|FCfXSxcHjh[5khSXO|YYm= MlvvNVAh|ryP M1XiclEzyqCqwrC= NV[xVGRYTE2VTx?= MorSbY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> NXPkVnAzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVUxOjhpPkK1O|E2ODJ6PD;hQi=>
U937 M1GwV2Fxd3C2b4Ppd{BCe3OjeR?= NIT5Zm8xNjF{NT2yJO69VQ>? MV2yOEBp NEXYcHRmdmijbnPld{BFUEFxWD2xNU1qdmS3Y3XkJIFxd3C2b4Ppdy=> Mn7qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5MUSwNlQoRjJ3N{G0NFI1RC:jPh?=
U937  NYfifZJFSXCxcITvd4l{KEG|c3H5 M2HnOVAvPSEQvF2= MoHQNlQhcA>? MYPlcohidmOnczDjcIVifmGpZTDv[kBRSVKSIHHu[EBk[XOyYYPlMVMh[XNid3XscEBieyCQb4jhJIxmfmWu NV\yeZNSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3NVQxOjRpPkK1O|E1ODJ2PD;hQi=>
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Rh41 NUn3e41ieUiWUzDhd5NigQ>? NF\GPWtyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDRzIHPlcIx{ NIGzNmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 Mo\sdWhVWyCjc4PhfS=> M2f2NZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz M{PWT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MoHodWhVWyCjc4PhfS=> NH;ON5VyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> NFnhO3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 NIfB[JlyUFSVIHHzd4F6 NED5Zm5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NE\seHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 MVPxTHRUKGG|c3H5 NXfIOYRseUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 NWq5[4tGeUiWUzDhd5NigQ>? M{THcZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy| MnH5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 M2n4T5FJXFNiYYPzZZk> NEDYeVFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBPSjF4NEOgZ4VtdHN? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC NWGzUldkeUiWUzDhd5NigQ>? MWrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNU2FIHPlcIx{ NXTSem5rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32 NH3jZYhyUFSVIHHzd4F6 MWDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz NIjpOo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 NIXoZ5ByUFSVIHHzd4F6 NFnYSnpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDF6IHPlcIx{ NY[2W2JKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NHfmXpJyUFSVIHHzd4F6 M2TP[5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNid3NvMjDj[Yxtew>? MoHkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PARP / c-PARP / cleaved caspase 3 ; 

PubMed: 21393866     


H146 cells were preincubated in normoxia or hypoxia (1% O2) for 18 hours prior to treatment with ABT-737 (89.1 nM ), after which cells were harvested for protein analysis by Western blot. 

Hif-1a; 

PubMed: 22006676     


Representative western blots for HIF-1α, PARP and cleaved caspase 3 in response to 24-72 hr exposure to ABT-737 in varying concentration in normoxia and hypoxia in 4 neuroblastoma cell lines. Actin is shown as a loading control. Blots are representative of 3 independent experiments.

γ-H2AX / p-ATM; 

PubMed: 21084274     


Induction of γ-H2AX and p-ATM by ABT-737. Cells were treated with 10 µmol/L ABT-737 for 24 hours and then maintained in fresh media for 1 or 2 more days prior to Western blot analysis.

21393866 22006676 21084274
Immunofluorescence
cytochrome C; 

PubMed: 26447615     


Immunocytochemistry revealed the release of mitochondrial cytochrome c (green) into the cytoplasm after ABT-737 exposure (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field.

Bax; 

PubMed: 26447615     


Immunocytochemistry revealed the mitochondrial translocation of Bax from the cytoplasm after ABT-737 treatment (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field C. To assess whether ABT-737 treatment has an effect on the dimerization of Bax, the levels of dimeric Bax were measured with or without ABT-737 treatment in MC-3 and HN22 cells.

Bim; 

PubMed: 26447615     


Immunocytochemistry revealed the mitochondrial translocation of Bim from the cytoplasm after ABT-737 treatment (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field.

AIF; 

PubMed: 25034785     


localization of apoptosis inducing factor (AIF) in LCSC pre-stained with Mitotracker Red and untreated or treated with 500 nM ABT-737 for 48 h. Magnification × 60, zoom × 3, bar 20 μm. 

p65 ; 

PubMed: 28846096     


BCL-xL dependent SVEC cells were treated with ABT-737 (10 μM) +/- Q-VD-Oph (30 μM) for 1 h, immunostained for p65 and analysed by confocal microscopy. TNF (20 ng/ml) was used as positive control for p65 nuclear translocation. Scale bar represents 30μM. Representative images from three independent experiments.

26447615 25034785 28846096
Growth inhibition assay
Cell viability; 

PubMed: 22311987     


Stably transfected K562 cells were treated with increasing concentrations of ABT-737, obatoclax, or maritoclax for 24 h. Cell viability was determined by measuring intracellular ATP levels with the CellTiter Glo assay.

22311987
ELISA
IL-6 / IL-8; 

PubMed: 21084274     


The secretion of IL-6 and IL-8 in PV-10 cells treated with DMSO, ABT-737 or enantiomer for 24 hours was determined by ELISA.

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]

- 合并

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]

- 合并
  • 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。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 注射ER细胞的Scid 鼠
  • Dosages: 20 mg/kg和30 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (122.93 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):
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 粉状
溶于溶剂
别名 N/A

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、MSDS / 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、MSDS / 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

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:

    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.

Bcl-2 Signaling Pathway Map

Bcl-2 Inhibitors with Unique Features

相关Bcl-2产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID