ABT-737

ABT-737は一種のBH3模倣の阻害剤で、無細胞試験でBcl-xL、Bcl-2とBcl-wに作用する時のEC50値が78.7 nM、30.3 nMと197.8 nMにそれぞれ分かれることですが、Mcl-1、Bcl-BとBfl-1を抑制する作用がありません。臨床2期。

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ABT-737 化学構造
分子量: 813.43

高品質保証

文献中の引用(90)

カスタマーフィードバック(16)

MSDS

製品説明

  • Compare Bcl-2 Inhibitors
    Bcl-2製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • ABT-737のメカニズム

製品の説明

生物活性

製品説明 ABT-737は一種のBH3模倣の阻害剤で、無細胞試験でBcl-xL、Bcl-2とBcl-wに作用する時のEC50値が78.7 nM、30.3 nMと197.8 nMにそれぞれ分かれることですが、Mcl-1、Bcl-BとBfl-1を抑制する作用がありません。臨床2期。
ターゲット

Bcl-xL

Bcl-2

Bcl-w

IC50

78.7 nM (EC50)

30.3 nM (EC50)

197.8 nM (EC50) [1]

In vitro試験 ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. ABT-737 is sensitive to HL60, KG1 and NB4 cells with IC50 of 50 nM, 80 nM and 80 nM, respectively. ABT-737 induces apoptosis in HL60 cells, which due to decreased Bcl-2/Bax heterodimerization and has no effect on cell cycle distribution. ABT-737 also induces cytochrome c release from purified mitochondria and promotes conformational changes in Bax that are associated with apoptosis. [1] Resistant cells (Hela and MCF-7) can be sensitized to ABT-737 by approaches that down-regulate, destabilize, or inactivate Mcl-1. ABT-737 also causes Bax/BAK-dependent cytochrome c release only when Mcl-1 has been neutralized. [2] ABT-737 displaces Bim from Bcl2's BH3-binding pocket, allowing Bim to activate Bax, induce mitochondrial permeabilization, and rapidly commit the primary chronic lymphocytic leukemia (CLL) cells to death. [3] Knockdown of Mcl-1 with siRNA sensitizes two resistant SCLC cell lines H196 and DMS114 to ABT-737 by enhancing the induction of apoptosis. Likewise, up-regulation of Noxa sensitizes H196 cells to ABT-737. ABT-737 inhibits proliferation and induces apoptosis in many SCLC cell lines including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 and etc. Bcl-2 and Noxa may contribute mechanistically to the cellular response to ABT-737 in NCI-H146 cells. [4] A recent study shows that ABT-737 significantly induces apoptosis in HTLV-1 infected T-cell lines as well as in fresh ATLL cells. [5]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
OCI-Ly1  NVOxcFU1S2WubDDWbYFjcWyrdImgRZN{[Xl? NH\QfFMzPTBibl5CpC=> MlPnO|IhcA>? M4T6R2ROW09? NXS3eZFL[2G3c3XkJFk4LSCub4PzJI9nKH[rYXLpcIl1gSCrbjDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEKFTE[gd4lTVkF? NXO4fXYxOjZ4NUeyPFg>
KG1a NU\yTZlIS2WubDDWbYFjcWyrdImgRZN{[Xl? M{PldFAuOTBizszN NWPDVVJ3OjRiaB?= M4DjT2ROW09? M2fCc2lEPTB;Nz62PEDPxE1uIHTlZ5Jm[XOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NH\jT|YzPjV3MkexNi=>
Kasumi-1 NUezTFlXS2WubDDWbYFjcWyrdImgRZN{[Xl? NXvxR2NEOC1zMDFOwG0> M1TzXlI1KGh? MVvEUXNQ Ml\yTWM2OD12Lki3JO69VSxiZHXjdoVie2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUSyOlU2OjdzMh?=
KG1a M1HKdWFxd3C2b4Ppd{BCe3OjeR?= MXuwMVExKM7:TR?= NVzWOGJSOjRiaB?= NGC0VFZFVVOR MlzEbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3:5NlI3PTV{N{Gy
Kasumi-1 NGO1bWpCeG:ydH;zbZMhSXO|YYm= NEPISVQxNTFyIN88US=> M4[1SFI1KGh? NF3tfldFVVOR M{K4OYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MUGyOlU2OjdzMh?=
MC-3  NX\Ue5RYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPafnFKPS9zMD:yNEDPxE1? MUCyOEBp MoX1SG1UVw>? MoS5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MnPwNlY1PDd4MUW=
HN22  NVj4RYw3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jDRlIvPS95LkWvNlIvPSEQvF2= M2HGc|I1KGh? MYTEUXNQ M{XnbYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MlG5NlY1PDd4MUW=
MC-3  MnvDRZBweHSxc3nzJGF{e2G7 M2rHbVUwOTBxMkCg{txO MlLCNlQhcA>? NXP3Z|ZWTE2VTx?= MWDpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| M372eVI3PDR5NkG1
HN22  MUjBdI9xfG:|aYOgRZN{[Xl? M1r6TVIvPS95LkWvNlIvPSEQvF2= M1jCRlI1KGh? NUnS[WtCTE2VTx?= MUTpcoR2[2W|IHPhd5Bie2VvbXXkbYF1\WRiYYDvdJRwe2m| NHnGe2YzPjR2N{[xOS=>
MOLT-4 NXjIdGh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;YR2ZYOTBvNUCwNEBvVQ>? MmrlO|IhcA>? NYHXNFBRTE2VTx?= MXzJR|UxRTBwMUm4JO69VQ>? M1TiZVI3Ozl{M{Oy
RS4;11 NIflcllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnn2NVAuPTByMDDuUS=> NWrXXmEyPzJiaB?= NF3XUIRFVVOR MUnJR|UxRTBwMECyJO69VQ>? MlPmNlY{QTJ|M{K=
JURKAT MoDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUexNE02ODByIH7N MV:3NkBp NVPOclF2TE2VTx?= NULMSHIxUUN3ME22OkDPxE1? M4\Ie|I3Ozl{M{Oy
CEM R M4LlWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVH3VGdbOTBvNUCwNEBvVQ>? NFPCWVI4OiCq NWf4VIxPTE2VTx?= MXzJR|UxRTVwNDFOwG0> MnHqNlY{QTJ|M{K=
CEM S NH\ucVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\yV|RwOTBvNUCwNEBvVQ>? NVPMXIVYPzJiaB?= NX6wO2RXTE2VTx?= MWfJR|UxRTF{LkGg{txO NWj2Oo5JOjZ|OUKzN|I>
MOLT-4 NWLH[nFmSXCxcITvd4l{KEG|c3H5 MWCxNE0yODByIH7N NIrRSZkzPCCq NE\zUGNFVVOR MV\jZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= NUXtNmI6OjZ|OUKzN|I>
CEM S Moj4RZBweHSxc3nzJGF{e2G7 MYexNE0yODByIH7N Mn7KNlQhcA>? MnzhSG1UVw>? MX7jZZV{\XNidHjlJINt\WG4YXflJI9nKEKlbD2yJIFv\CC2aHWg[I94dnKnZ4XsZZRqd25ib3[gRoNtNXiOIHHu[EBO[2xvMR?= MlLDNlY{QTJ|M{K=
JURKAT MoLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzWNVAxNTFyMECgcm0> MYq0PEBp MWjEUXNQ NH;ESIlKSzVyPUm1OeKyQS5|IH7N MYSyOlE4OjJ4OR?=
LOUCY NEXmPW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLQdXcyODBvMUCwNEBvVQ>? Mn3sOFghcA>? NGntSI9FVVOR NHi3SW5KSzVyPUOyMljDuTFyLkmgcm0> M{HvXVI3OTd{Mk[5
WM-115 Mkj1R4VtdCCYaXHibYxqfHliQYPzZZk> NEnzb5QyODEEoH7N MmLtO|IhcA>? MXjlcohidmOnczDjeZJkfW2rbj3pcoR2[2WmIHHueIkue3W{dnn2ZYzDqA>? NXXjc5E6OjZzMU[3O|Y>
B16 M3H1V2NmdGxiVnnhZoltcXS7IFHzd4F6 M4jBfVExOMLibl2= NFfLNXA4OiCq M4jPe4VvcGGwY3XzJIN2emO3bXnuMYlv\HWlZXSgZY51cS2|dYL2bZZidMLi NHe5[nIzPjFzNke3Oi=>
HL-60  NGDzZnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXKyVXNLPzJiaB?= MoXWTWM2OMLiPTCxNE44KG6P NF7Xe3YzPjB2NU[wPS=>
MOLM-13  M{\4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{G1ZVczKGh? MoPwTWM2OMLiPTCyO{46KG6P MkS1NlYxPDV4MEm=
OCI-AML3 M1\qcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO3NkBp MkGzTWM2OMLiPTCxPVUxKG6P NGHmd5gzPjB2NU[wPS=>
BCWM.1 M3:yfmFxd3C2b4Ppd{BCe3OjeR?= MnzTNE0yNjZizszN NYTqSWxZOjRiaB?= MWnpcoR2[2W|IHPlcIwh[XCxcITvd4l{ MV2yOVg6OzJ7MB?=
MWCL-1 M3nFeWFxd3C2b4Ppd{BCe3OjeR?= M4HwU|AuOS54IN88US=> NYLSRVFTOjRiaB?= M2\4OIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M2H6ZVI2QDl|Mkmw
MM.1s MoT3RZBweHSxc3nzJGF{e2G7 MlnsNE0yNjZizszN MYeyOEBp NXLBWlROcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MlTmNlU5QTN{OUC=
HCT116 Mn7rSpVv[3Srb36gRZN{[Xl? MVuzM|ExKM7:TR?= NWXudGVtOTMEoHlCpC=> M1zKZWROW09? MU\pcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gUGM{Si2LSTDjc453\XK|aX;uJIFv\CCVUWPUUVEh\GWpcnHkZZRqd25? NYjObVhMOjV5MUWwNlg>
HCT116 BAX BAK1 DKO NIDI[mlHfW6ldHnvckBCe3OjeR?= MkPoN{8yOCEQvF2= MkjXNVLDqGkEoB?= NI\2cmtFVVOR M3fLN4lv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBNSzOELVnJJINwdn[ncoPpc44h[W6mIGPRV3ROOSCmZXfyZYRifGmxbh?= MUSyOVcyPTB{OB?=
HCT116 NXXk[VEyTnWwY4Tpc44hSXO|YYm= Mmr6NVAh|ryP M{PlUFEzyqCqwrC= MlzkSG1UVw>? M2[zc4lv[3KnYYPld{BITlBvTFOzRkBxfW6ldHG= NGXUe2gzPTdzNUCyPC=>
HCT116 BAX BAK1 DKO MojGSpVv[3Srb36gRZN{[Xl? M3TmdlExKM7:TR?= M1f5W|EzyqCqwrC= NYn6b5RXTE2VTx?= NGrhNIxqdmO{ZXHz[ZMhT0[SLVzDN2IheHWwY4Th NG\mZoMzPTdzNUCyPC=>
HCT116 MmizRZV1d3CqYXf5JGF{e2G7 MnjvNVAh|ryP M4DxXFEzyqCqwrC= MkizSG1UVw>? MXHpcoR2[2W|IHGgZ49ueGyndHWgZZV1d3CqYXfpZ{Bz\XOyb37z[S=> NIPkU2gzPTdzNUCyPC=>
HCT116 BAX BAK1 DKO NIDWeopCfXSxcHjh[5khSXO|YYm= NFLhcIoyOCEQvF2= MYmxNuKhcMLi NF\VOFRFVVOR MmX1bY5lfWOnczDhJINwdXCuZYTlJIF2fG:yaHHnbYMhemW|cH;ud4U> M2m4[lI2PzF3MEK4
U937 Ml\FRZBweHSxc3nzJGF{e2G7 NG\DeGMxNjF{NT2yJO69VQ>? MYiyOEBp NGLmeGRmdmijbnPld{BFUEFxWD2xNU1qdmS3Y3XkJIFxd3C2b4Ppdy=> M{S4T|I2PzF2MEK0
U937  NIjvWXdCeG:ydH;zbZMhSXO|YYm= NFezZ5MxNjVizszN Mor3NlQhcA>? MUjlcohidmOnczDjcIVifmGpZTDv[kBRSVKSIHHu[EBk[XOyYYPlMVMh[XNid3XscEBieyCQb4jhJIxmfmWu NX3kTGNzOjV5MUSwNlQ>
HL-60 AAA-Bcl-2 NU\Gd3FKSXCxcITvd4l{KEG|c3H5 M{nSUVAuPSEQvF2= NEGyeIY1QCCq MnqyTWM2OD1yLki3JO69de,:jHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Moj3NlU4OTF2NkC=
HL-60 EEE-Bcl-2 M1ruT2Fxd3C2b4Ppd{BCe3OjeR?= NEfCZ5gxNTVizszN M3O1ZlQ5KGh? NEfwZ|BKSzVyPUWg{txu97zOIHnu[JVk\XNiY3XscEBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NH7uXGEzPTdzMUS2NC=>
U87 M325PGZ2dmO2aX;uJGF{e2G7 NHfUbIs2OCEQvF2= MmiyNlQhcA>? NYLtPFYxemWmdXPld{B1cGVibWLORUBmgHC{ZYPzbY9vKGyndnXsd{Bw\iCPTWCtNkwhVU2SLUG0JIFv\CCEY3ytNi=> NU\NR5o5OjV4Nke2OlM>
K562 NEnD[I5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHL5R5UyNTFyIN88US=> M2S0fFQ5KGh? NHjvRXRFVVOR NUTv[3dWUUN3ME2yOk44KM7:TR?= Mor2NlU2QTZ3NkG=
K562/Mcl -1-IRESBim MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzFTWM2OD17LkOg{txO MWiyOVU{PTlyMB?=
K562/Bcl- 2-IRESBim M3LOb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37qUWlEPTB;MD6zOUDPxE1? M2P0dlI2PTN3OUCw
Jurkat M{Twemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTRTWM2OD1yLk[2JO69VQ>? NF7IUYIzPTV|NUmwNC=>
JurkatΔBak Ml\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDzcGZ[UUN3ME61NEDPxE1? NVPMVoV{OjV3M{W5NFA>
HL60/VCR MnrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fEbGlEPTB-MUCwJO69VQ>? NViwe5lPOjV3M{W5NFA>
Kasumi-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwMEGg{txO MYiyOVU{PTlyMB?=
Kasumi-1/ABT NFq1NWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHSbnVKSzVyPUCuOVEh|ryP NHmyNmozPTV|NUmwNC=>
THP-1 Mk[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTFUZR6UUN3ME2xMlI4KM7:TR?= MWmyOVU{PTlyMB?=
U937 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jOR2lEPTB;NT6yPUDPxE1? MU[yOVU{PTlyMB?=
C1498 NGqyPIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3K4UGlEPTB;Nj6xN{DPxE1? M4jpWFI2PTN3OUCw
RPMI 8226 M33QUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\PTWM2OD1yLkK1JO69VQ>? MVmyOVU{PTlyMB?=
MM.1S MnnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[0TWM2OD1yLkSwJO69VQ>? Mnn6NlU2OzV7MEC=
NCI-H929 NHzFSolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvWOGd7UUN3ME2xOU4zOSEQvF2= NX3yWWJGOjV3M{W5NFA>
U266 MoTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nIO2lEPTB;MD62PEDPxE1? NXXmcpZNOjV3M{W5NFA>
MCF-7 M3j2R2NmdGxiVnnhZoltcXS7IFHzd4F6 NWjJU|ZpPSEQvF2= NFT4UGU1QCCq NWnEdW5ZTE2VTx?= MULlcohidmOnczD0bIUhe2Wwc3n0bZZqfHlidH:gc5IhemGmaXH0bY9v Moe5NlU1ODlzMkS=
MCF-7 NH;yXo5CeG:ydH;zbZMhSXO|YYm= Mke5OUDPxE1? MYi0M|I1NzR6IHi= NHTwe2lFVVOR NV;jfWo6cW6lcnXhd4V{KHSqZTDjcIVifmWmIGDBVnA> NHvvPHkzPTRyOUGyOC=>
MCF-7 MXrGeY5kfGmxbjDBd5NigQ>? NY\DfXFlPSEQvF2= MnzMNlQhcA>? NWnLRY5{TE2VTx?= M2facoVvcGGwY3XzJJRp\WyndnXsJI9nKE2lbD2xJIV5eHKnc4Ppc47DqA>? NXHCWZl{OjV2MEmxNlQ>
MDA-MB 231  MoXCSpVv[3Srb36gRZN{[Xl? MUO1JO69VQ>? NXfVZYFCOjRiaB?= NFfyb45FVVOR MUPlcohidmOnczD0bIVt\X[nbDDv[kBO[2xvMTDlfJBz\XO|aX;uxsA> M3y2UFI2PDB7MUK0
ZR-75-1  NVX4UXBRTnWwY4Tpc44hSXO|YYm= M1LU[FUh|ryP M3SyPFI1KGh? NVn5V3BrTE2VTx?= NUXyWVFp\W6qYX7j[ZMhfGinbHX2[Ywhd2ZiTXPsMVEh\XiycnXzd4lwdsLi M3O4N|I2PDB7MUK0
A549 M17FUWNmdGxiVnnhZoltcXS7IFHzd4F6 M2P6UFAuOjBizszN M3TCVlczKGh? Mo\GSG1UVw>? NXy3V2R{\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NYmyN3I{OjV|OEi3OlI>
H1299 NHnGOIVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlW3NE0zOCEQvF2= M4\v[lczKGh? NVjKOWtUTE2VTx?= M3\5WYRm[3KnYYPld{B1cGViY3XscEB{fXK4aY\hcEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldkBkd22kaX7l[EB4cXSqIHHzdIlzcW5? MWqyOVM5QDd4Mh?=
HO-8910 MnjnR4VtdCCYaXHibYxqfHliQYPzZZk> MUOwMVIxKM7:TR?= NXvsOllnPzJiaB?= MUTEUXNQ NWXTR4li\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= NFfQRlkzPTN6OEe2Ni=>
HT-29 NWfJZYlVS2WubDDWbYFjcWyrdImgRZN{[Xl? NICwSnkxNTJyIN88US=> MnS2O|IhcA>? M4[yZWROW09? MUjk[YNz\WG|ZYOgeIhmKGOnbHygd5Vzfmm4YXygbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYKgZ49u[mmwZXSge4l1cCCjc4Dpdolv NIC3NFczPTN6OEe2Ni=>
HCT-116 NIHzRXhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHjzcYQxNTJyIN88US=> MkXlO|IhcA>? M{fucmROW09? NVjyTHJM\GWlcnXhd4V{KHSqZTDj[YxtKHO3co\peoFtKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzKGOxbXLpcoVlKHerdHigZZNxcXKrbh?= M4fQWVI2Ozh6N{[y
A549 NYPmWHpHSXCxcITvd4l{KEG|c3H5 NUjVOJppOjBizszN NV\BcIU4PDhiaB?= MVTEUXNQ M2XjU4lv\HWlZYOgZZBweHSxc3nzJJNq\26rZnnjZY51dHliY3;tZolv\WRid3n0bEBie3Crcnnu NWfzT3ZQOjV|OEi3OlI>
H1299 NWnDUWg4SXCxcITvd4l{KEG|c3H5 NY\lcZVvOjBizszN MVK0PEBp MkHuSG1UVw>? NEGxemZqdmS3Y3XzJIFxd3C2b4Ppd{B{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIgh[XOyaYLpci=> NGrDXXAzPTN6OEe2Ni=>
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... Click to View More Cell Line Experimental Data

In vivo試験 In aggressive leukemia model, ABT-737 suppresses the leukemia burden by 53% at the 30 mg/kg, with significantly extended survival of mice. ABT-737 does not induce significantly abnormalities in blood cell counts or serum chemistries. [1] ABT-737 prolongs the survival of recipient mice transplanted with Bcl-2-transduced tumors. [2] ABT-737 shows great antitumor activity in an ATLL mouse model at a dose of 100 mg/kg. [5]
臨床試験 ABT-737, associated with Platinum, is currently under Phase II clinical trials in ovarian tumors.
特集 First-generation inhibitor of anti-apoptotic Bcl-2 proteins.

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

Fluorescence polarization assays Binding affinity of GST-Bcl-2 family proteins to the FITC-conjugated BH3 domain of Bim (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is determined. Briefly, 100 nM of GST-Bcl-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-Bim BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. Then IC50 are determined.

細胞アッセイ:

[4]

細胞株 SCLC cell lines NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114
濃度 0.001-10 μM
反応時間 48 hours
実験の流れ

SCLC cells are treated for 48 hours in 96-well tissue culture plates in a total volume of 100 μL tissue culture medium supplemented with 10% human serum. Viable cells are determined using the MTS assay.

動物実験:

[1]

動物モデル Scid mice injected with Luc-expressing FD/ΔRaf-1:ER cells
製剤 1 g/mL stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4−5; final concentration of DMSO ≤ 1%)
投薬量 20 and 30 mg/kg
投与方法 For intraperitoneal (i.p.) every day

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download ABT-737 SDF
分子量 813.43
化学式

C42H45ClN6O5S2

CAS No. 852808-04-9
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 100 mg/mL (122.93 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% Propylene glycol, 5% Tween 80, 65% D5W 30mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 Benzamide, 4-[4-[(4'-chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]-

文献中の引用 (90)

Frequently Asked Questions

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

    Answer: 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.

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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他の質問がある場合は、お気軽くお問合せください。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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