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ABT-737

ABT-737是一種BH3模擬抑制劑，作用于Bcl-xL，Bcl-2和Bcl-w，無細(xì)胞試驗(yàn)中EC50分別為78.7 nM，30.3 nM和197.8 nM；但對Mcl-1， Bcl-B及Bfl-1沒有抑制作用。ABT-737可誘導(dǎo)線粒體通路的凋亡和線粒體自噬。Phase 2。

ABT-737 Chemical Structure

ABT-737 Chemical Structure

CAS: 852808-04-9

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1203.93 現(xiàn)貨
5mg 972.14 現(xiàn)貨
50mg 4659.22 現(xiàn)貨
100mg 7964.03 現(xiàn)貨
1g 23751 現(xiàn)貨
更大包裝 有超大折扣

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ABT-737相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Bcl-2 Signaling Pathways

Bcl-2信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
DMS53 Function assay 5 to 10 uM 12 hrs Inhibition of BCl-2/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method 26982372
DMS53 Apoptosis assay 5 to 10 uM 12 hrs Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as caspase-3 cleavage at 5 to 10 uM after 12 hrs by immunoblotting method 26982372
DMS53 Apoptosis assay 5 to 10 uM 12 hrs Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as PARP cleavage at 5 to 10 uM after 12 hrs by immunoblotting method 26982372
DMS53 Function assay 5 to 10 uM 12 hrs Inhibition of BCl-2/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method 26982372
DMS53 Apoptosis assay 5 to 10 uM 12 hrs Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as cytochrome c release at 5 to 10 uM after 12 hrs by immunoblotting method 26982372
RS4:11 Apoptosis assay 10 uM 24 hrs Induction of apoptosis in human RS4:11 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method 23047228
IM9 Apoptosis assay 10 uM 24 hrs Induction of apoptosis in human IM9 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method 23047228
BP3 Apoptosis assay 10 uM 24 hrs Induction of apoptosis in human BP3 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method 23047228
MDA-MB-231 Function assay 0.03 to 1 uM 1 hr Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced cytochrome c release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis 22747598
MDA-MB-231 Function assay 0.03 to 1 uM 1 hr Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced Smac protein release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis 22747598
HeLa Function assay 10 uM 16 hrs Inhibition of Rluc-Bax/eYFP-Bcl-xL interaction expressed in human HeLa cells at 10 uM after 16 hrs by BRET assay 22425031
HeLa Function assay 1 uM 12 hrs Induction of Bcl-xL-mediated apoptosis in doxycyclin-stimulated human HeLa cells overexpressing Noxa at 1 uM after 12 hrs by Hoechst staining 22386982
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 Y101H mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.38 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 F97V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.3 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.29 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.27 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 V141A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.19 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 R100E mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.16 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.073 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 delta136T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.06 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.058 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.021 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142Gdelta136T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.01 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 E96G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0058 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 E129H mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0045 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Wild type Bcl-2-like protein 1 expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0034 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 Y195F mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0015 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A93V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0014 μM. 21807512
BL21 Function assay 10 uM 3 hrs Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 G196A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.001 μM. 21807512
RS4;11 Function Assay 100 nM 1/3/6 h induces caspase-dependent Mcl-1 cleavage 24951472
OPM-2? Apoptosis Assay 125/250/500 nM 48h? induces cell apoptosis in a dose-dependent manner 25008202
COG-LL-319 Function Assay 100 nM 1/3/6 h induces caspase-dependent Mcl-1 cleavage 24951472
RPMI-8226? Apoptosis Assay 125/250/500 nM 48h? induces cell apoptosis in a dose-dependent manner 25008202
OPM-2? Cell Viability Assay 125/250/500 nM 48h? decreases cell viability in a dose-dependent manner 25008202
RPMI-8226? Cell Viability Assay 125/250/500 nM 48h? decreases cell viability in a dose-dependent manner 25008202
Caco2 Apoptosis Assay 1/5/10 μM 48 h causes cell death in a dose-dependent manner 25192188
Colo205 Apoptosis Assay 1/5/10 μM 48 h causes cell death in a dose-dependent manner 25192188
SW480 Apoptosis Assay 1/5/10 μM 48 h causes cell death in a dose-dependent manner 25192188
HT29 Apoptosis Assay 1/5/10 μM 48 h causes cell death in a dose-dependent manner 25192188
CX-1 Growth Inhibition Assay 0.2–60 μM 72 h IC50=1.8 μM 25208882
LS174T Growth Inhibition Assay 0.2–60 μM 72 h IC50=18.3 μM 25208882
Clone A Growth Inhibition Assay 0.2–60 μM 72 h IC50=7.5 μM 25208882
MM.1S Function Assay 500/750 nM 24/48 h downregulates Bim, principally the EL isoform 25208888
U266 Function Assay 500/750 nM 24/48 h downregulates Bim, principally the EL isoform 25208888
RPMI8226 Function Assay 500/750 nM 24/48 h downregulates Bim, principally the EL isoform 25208888
A5-RT3 Function Assay 5 μM 6 h induces the release of mitochondrial proteins and reduces clonogenic survival in a caspase-independent manner 25210795
HaCaT Function Assay 10?μM 24/48 h induces MMP and DNA fragmentation 25210795
A5-RT3 Function Assay 10?μM 24/48 h induces MMP and DNA fragmentation 25210795
HaCaT Cell Viability Assay 0.1/1/10 μM 24 h decreases cell viability in a dose-dependent manner 25210795
A5-RT3 Cell Viability Assay 0.1/1/10 μM 24 h decreases cell viability in a dose-dependent manner 25210795
HCT116 Cell Viability Assay 0-10 μM 24?h? IC50=20.49?μM 25304383
LS411N Cell Viability Assay 0-10 μM 24?h? IC50=11.47?μM 25304383
SW620 Cell Viability Assay 0-10 μM 24?h? IC50=12.24?μM 25304383
Caco-2 Cell Viability Assay 0-10 μM 24?h? IC50=19.7?μM 25304383
DLD1 Cell Viability Assay 0-10 μM 24?h? IC50=18.78?μM 25304383
RL? Cell Viability Assay 0.0001-1 μM 96 h decreases the cell viability in a dose-dependent manner 25373508
RKO Cell Viability Assay 0-10 μM 24?h? IC50>?25?μM 25304383
OcI-LY18 Cell Viability Assay 0.0001-1 μM 96 h decreases the cell viability in a dose-dependent manner 25373508
H1299 Apoptosis Assay 20 μM 48 h induces apoptosis significantly combined with aspirin 25388762
Sc-1 Cell Viability Assay 0.0001-1 μM 96 h decreases the cell viability in a dose-dependent manner 25373508
A549 Apoptosis Assay 20 μM 48 h induces apoptosis significantly combined with aspirin 25388762
HT-29 Cell Viability Assay 0-20 μM 72 h decreases the cell survival in a dose-dependent manner combined with aspirin 25388762
HCT-116 Cell Viability Assay 0-20 μM 72 h decreases the cell survival in a dose-dependent manner combined with aspirin 25388762
HO-8910 Cell Viability Assay 0-20 μM 72 h decreases the cell survival in a dose-dependent manner combined with aspirin 25388762
H1299 Cell Viability Assay 0-20 μM 72 h decreases the cell survival in a dose-dependent manner combined with aspirin 25388762
ZR-75-1? Function Assay 5 μM 24 h enhances thelevel of Mcl-1 expression? 25409124
A549 Cell Viability Assay 0-20 μM 72 h decreases the cell survival in a dose-dependent manner combined with aspirin 25388762
MCF-7 Function Assay 5 μM 24 h enhances thelevel of Mcl-1 expression? 25409124
MDA-MB 231? Function Assay 5 μM 24 h enhances thelevel of Mcl-1 expression? 25409124
MCF-7 Apoptosis Assay 5 μM 4/24/48 h increases the cleaved PARP 25409124
MCF-7 Cell Viability Assay 5 μM 48 h enhances the sensitivity to or radiation 25409124
K562 Cell Viability Assay 1-10 μM 48 h IC50=26.7 μM 25596561
U87 Function Assay 50 μM 24 h reduces the mRNA expression levels of MMP-2, MMP-14 and Bcl-2 25667663
HL-60?AAA-Bcl-2 Apoptosis Assay 0-5 μM 48 h IC50=0.87 μm，induces cell apoptosis in a dose-dependent manner 25711460
HL-60?EEE-Bcl-2 Apoptosis Assay 0-5 μM 48 h IC50=5 μm， induces cell apoptosis in a dose-dependent manner 25711460
U937? Apoptosis Assay 0.5 μM 24 h enhances cleavage of PARP and caspase-3 as well as Noxa level 25714024
U937 Apoptosis Assay 0.125-2 μM 24 h enhances DHA/X-11-induced apoptosis 25714024
HCT116?BAX BAK1?DKO Autophagy Assay 10 μM 12?h? induces a complete autophagic response 25715028
HCT116?BAX BAK1?DKO Function Assay 10 μM 12?h? increases GFP-LC3B puncta 25715028
HCT116 Autophagy Assay 10 μM 12?h? induces a complete autophagic response 25715028
HCT116 Function Assay 10 μM 12?h? increases GFP-LC3B puncta 25715028
HCT116?BAX BAK1?DKO Function Assay 3/10 μM 12?h? induces a dose-dependent increase in LC3B-II conversion and SQSTM1 degradation 25715028
HCT116 Function Assay 3/10 μM 12?h? induces a dose-dependent increase in LC3B-II conversion and SQSTM1 degradation 25715028
MM.1s Apoptosis Assay 0-1.6 μM 24 h induces cell apoptosis 25893290
MWCL-1 Apoptosis Assay 0-1.6 μM 24 h induces cell apoptosis 25893290
BCWM.1 Apoptosis Assay 0-1.6 μM 24 h induces cell apoptosis 25893290
B16 Cell Viability Assay 100?nM 72 h enhances curcumin-induced anti-survival? 26116776
WM-115 Cell Viability Assay 100?nM 72 h enhances curcumin-induced anti-survival? 26116776
LOUCY Growth Inhibition Assay 100-1000 nM 48 h IC50=32.8±10.9 nM 26172269
JURKAT Growth Inhibition Assay 100-1000 nM 48 h IC50=955±9.3 nM 26172269
CEM S Apoptosis Assay 10-1000 nM 24 h causes the cleavage of Bcl-2 and the downregulation of Bcl-xL and Mcl-1 26392332
MOLT-4 Apoptosis Assay 10-1000 nM 24 h causes the cleavage of Bcl-2 and the downregulation of Bcl-xL and Mcl-1 26392332
CEM S Growth Inhibition Assay 10-5000 nM 72 h IC50=12.1 μM 26392332
CEM R Growth Inhibition Assay 10-5000 nM 72 h IC50=5.4 μM 26392332
JURKAT Growth Inhibition Assay 10-5000 nM 72 h IC50=66 μM 26392332
RS4;11 Growth Inhibition Assay 10-5000 nM 72 h IC50=0.002 μM 26392332
MOLT-4 Growth Inhibition Assay 10-5000 nM 72 h IC50=0.198 μM 26392332
MC-3? Apoptosis Assay 5/10/20 μM 24 h induces caspase-mediated apoptosis 26447615
HN22? Apoptosis Assay 2.5/7.5/22.5 μM 24 h induces caspase-mediated apoptosis 26447615
HN22? Growth Inhibition Assay 2.5/7.5/22.5 μM 24 h inhibits cell growth in a dose-dependent manner 26447615
MC-3? Growth Inhibition Assay 5/10/20 μM 24 h inhibits cell growth in a dose-dependent manner 26447615
Kasumi-1 Apoptosis Assay 0-10 μM 24 h induces cell apoptosis in a dose-dependent manner 26552712
KG1a Apoptosis Assay 0-10 μM 24 h induces cell apoptosis in a dose-dependent manner 26552712
Kasumi-1 Cell Viability Assay 0-10 μM 24 h IC50=4.87 μM, decreases cell viability in a dose-dependent manner 26552712
KG1a Cell Viability Assay 0-10 μM 24 h IC50=7.68 μM, decreases cell viability in a dose-dependent manner 26552712
OCI-Ly1? Cell Viability Assay 250 nM? 72 h caused 97% loss of viability in cells transfected with BCL6 siRNA 26657288
Eu-Myc Apoptosis assay 1 uM Induction of apoptosis in mouse Eu-Myc cells overexpressing BCL2 assessed as inhibition of colony formation at 1 uM 18040043
KB Cytotoxicity assay 0.5 uM Cytotoxicity in human siRNA-mediated-MCL1-kncok down KB cells overexpressing BCL2 at 0.5 uM 18040043
HCT116 Apoptosis assay 48 hrs Induction of apoptosis in human HCT116 p53+/+ cells after 48 hrs by Annexin V-FITC staining-based flow cytometric method 26982372
BL21 (DE3) Function assay 2 hrs Binding affinity to N-terminus 8X His-tagged human Bcl-xL expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, Ki = 0.001 μM. 22448988
BL21 (DE3) Function assay 2 hrs Binding affinity to N-terminus 6X His-tagged human Bcl2 expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, Ki = 0.0006 μM. 22448988
Remb1 Cytotoxicity assay 24 hrs Cytotoxicity against human Remb1 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50 = 1.4 μM. 29453135
RS4:11 Cytotoxicity assay 24 hrs Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50 = 0.33 μM. 29453135
SKOV3 Growth inhibition assay 72 hrs Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay, IC50 = 46.59 μM. 27712939
U266 Growth inhibition assay 72 hrs Growth inhibition of human U266 cells after 72 hrs by MTT assay, IC50 = 27.35 μM. 27712939
MCF7 Growth inhibition assay 72 hrs Growth inhibition of human MCF7 cells after 72 hrs by MTT assay, IC50 = 25.33 μM. 27712939
HL60 Growth inhibition assay 72 hrs Growth inhibition of human HL60 cells after 72 hrs by MTT assay, IC50 = 0.97 μM. 27712939
NCI-H1417 Cytotoxicity assay 4 days Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.1734 μM. 23448298
NCI-H187 Cytotoxicity assay 4 days Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.1377 μM. 23448298
NCI-H1963 Cytotoxicity assay 4 days Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.054 μM. 23448298
K562 Apoptosis assay 48 hrs Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry, IC50 = 16.4 μM. 23314054
RS4:11 Apoptosis assay 48 hrs Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry, IC50 = 0.27 μM. 23314054
NCI-H1417 Antiproliferative assay 4 days Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay, IC50 = 0.412 μM. 22747598
NCI-H1963 Antiproliferative assay 4 days Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay, IC50 = 0.059 μM. 22747598
NCI-H146 Antiproliferative assay 4 days Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay, IC50 = 0.037 μM. 22747598
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 34.7 μM. 22582991
HL60 Cytotoxicity assay 48 hrs Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 0.76 μM. 22582991
CCRF-CEM Cytotoxicity assay 48 hrs Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 0.74 μM. 22582991
NCI-H1417 Growth inhibition assay 4 days Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay, IC50 = 0.13 μM. 22448988
NCI-H146 Growth inhibition assay 4 days Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay, IC50 = 0.097 μM. 22448988
BL21 (DE3) Function assay 2 hrs Binding affinity to N-terminus 8X His-tagged human Bcl-xL expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, IC50 = 0.006 μM. 22448988
BL21 (DE3) Function assay 2 hrs Binding affinity to N-terminus 6X His-tagged human Bcl2 expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, IC50 = 0.002 μM. 22448988
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay, IC50 = 47.7 μM. 22172701
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay, IC50 = 27.6 μM. 19743858
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay, IC50 = 21.26 μM. 19743858
Hepa-1c1c7 Cytotoxicity assay 48 hrs Cytotoxicity against mouse Hepa-1c1c7 cells after 48 hrs by cell titer-blue assay, IC50 = 8.68 μM. 19743858
H460 Cytotoxicity assay 48 hrs Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay, IC50 = 8.03 μM. 19743858
SU-8686 Cytotoxicity assay 48 hrs Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay, IC50 = 4.24 μM. 19743858
HCT116 Cytotoxicity assay 48 hrs Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay, IC50 = 4.06 μM. 19743858
Jurkat Cytotoxicity assay 48 hrs Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay, IC50 = 1.38 μM. 19743858
MEF Cytotoxicity assay 24 hrs Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum, EC50 = 0.051 μM. 21366295
MEF Cytotoxicity assay 24 hrs Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum, EC50 = 0.051 μM. 21366295
MEF Cytotoxicity assay 24 hrs Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum, EC50 = 0.00203 μM. 21366295
NCI-H146 Cytotoxicity assay 48 hrs Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum, EC50 = 0.087 μM. 18841882
FL5.12 Cytotoxicity assay 24 hrs Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum, EC50 = 0.03 μM. 18841882
FL5.12 Cytotoxicity assay 24 hrs Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum, EC50 = 0.0077 μM. 18841882
UPCI:SCC90 Growth Inhibition Assay 72 h GI50=6.6 ± 1.5 μM 25139387
UD-SCC2 Growth Inhibition Assay 72 h GI50=28 ± 2.9 μM 25139387
93-VU-147T Growth Inhibition Assay 72 h GI50=4.3 ± 3.5 μM 25139387
UM-SCC47 Growth Inhibition Assay 72 h GI50=19 ± 12.3 μM 25139387
UM-SCC22B Growth Inhibition Assay 72 h GI50=19 ± 2.9 μM 25139387
PCI-15B Growth Inhibition Assay 72 h GI50=11 ± 4.5 μM 25139387
PCI-13 Growth Inhibition Assay 72 h GI50=15 ± 1.8 μM 25139387
OCI-AML3 Growth Inhibition Assay 72 h IC50?= 1950 nM 26045609
MOLM-13? Growth Inhibition Assay 72 h IC50?= 27.9 nM 26045609
HL-60? Growth Inhibition Assay 72 h IC50?= 10.7 nM 26045609
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Toledo Apoptosis assay Induction of apoptosis in human Toledo cells, LD50 = 0.06 μM. 24900652
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
MOLT4 Antiproliferative assay Antiproliferative activity against human MOLT4 cells in presence of 10% human serum, EC50 = 0.622 μM. 28926247
RS4:11 Antiproliferative assay Antiproliferative activity against human RS4:11 cells in presence of 10% human serum, EC50 = 0.024 μM. 28926247
CLL Apoptosis assay Induction of apoptosis in human CLL cells, EC50 = 0.0045 μM. 20925433
SUDHL4 Growth inhibition assay Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.85 μM. 17256834
FL5.12 Function assay Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of 3% FBS, EC50 = 0.22 μM. 17256834
SUDHL4 Growth inhibition assay Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.22 μM. 17256834
RS11380 Growth inhibition assay Inhibition of cell growth in human RS11380 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.15 μM. 17256834
DoHH2 Growth inhibition assay Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.13 μM. 17256834
FL5.12 Function assay Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of 3% FBS, EC50 = 0.05 μM. 17256834
FL5.12 Function assay Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of bovine gelatin, EC50 = 0.03 μM. 17256834
DoHH2 Growth inhibition assay Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.0083 μM. 17256834
RS11380 Growth inhibition assay Inhibition of cell growth in human RS11380 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.014 μM. 17256834
FL5.12 Function assay Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of bovine gelatin, EC50 = 0.008 μM. 17256834
U266 Growth Inhibition Assay IC50=0.68 μM 25535900
NCI-H929 Growth Inhibition Assay IC50=15.21 μM 25535900
MM.1S Growth Inhibition Assay IC50=0.40 μM 25535900
RPMI 8226 Growth Inhibition Assay IC50=0.25 μM 25535900
U937 Growth Inhibition Assay IC50=5.29 μM 25535900
C1498 Growth Inhibition Assay IC50=6.13 μM 25535900
THP-1 Growth Inhibition Assay IC50=1.27 μM 25535900
Kasumi-1 Growth Inhibition Assay IC50=0.01 μM 25535900
Kasumi-1/ABT Growth Inhibition Assay IC50=0.51 μM 25535900
JurkatΔBak Growth Inhibition Assay IC50>50 μM 25535900
HL60/VCR Growth Inhibition Assay IC50>100 μM 25535900
K562/Bcl- 2-IRESBim Growth Inhibition Assay IC50=0.35 μM 25535900
Jurkat Growth Inhibition Assay IC50=0.66 μM 25535900
K562/Mcl -1-IRESBim Growth Inhibition Assay IC50=9.3 μM 25535900
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
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生物活性

產(chǎn)品描述 ABT-737是一種BH3模擬抑制劑，作用于Bcl-xL，Bcl-2和Bcl-w，無細(xì)胞試驗(yàn)中EC50分別為78.7 nM，30.3 nM和197.8 nM；但對Mcl-1， Bcl-B及Bfl-1沒有抑制作用。ABT-737可誘導(dǎo)線粒體通路的凋亡和線粒體自噬。Phase 2。
特性 ABT-737是第一代抗凋亡BCL-2家族蛋白小分子抑制劑。
靶點(diǎn)
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)
體外研究(In Vitro)
體外研究活性 ABT-737降低BCL-2/BAX異質(zhì)二聚體,而誘導(dǎo)HL60細(xì)胞凋亡,但是對細(xì)胞周期分布沒有抑制效果。ABT-737也誘導(dǎo)細(xì)胞色素C從線粒體中釋放，促進(jìn)BAX構(gòu)象改變，BAX與凋亡相關(guān)。在白血病模型中，ABT-737按30 mg/kg處理，阻斷53%白血病負(fù)荷，且使鼠壽命明顯延長。ABT-737不會(huì)導(dǎo)致血細(xì)胞數(shù)和血清組成發(fā)生異常。[1]通過使Mcl-1失活而使抵抗細(xì)胞（Hela和MCF-7）對ABT-737敏感。當(dāng)Mcl-1無效時(shí)，ABT-737也導(dǎo)致BAX/BAK-依賴的細(xì)胞色素C釋放。ABT-737延長攜帶BCL-2腫瘤的鼠壽命。[2]ABT-737從BCL2’s BH3結(jié)合袋取代BIM,使BIM激活BAX,誘導(dǎo)線粒體透化作用,快速致死慢性淋巴細(xì)胞性白血病(CLL)細(xì)胞。[3] Noxa正向調(diào)節(jié)增強(qiáng)H196細(xì)胞對ABT-737敏感性。ABT-737抑制多種SCLC細(xì)胞系，包括NCI-H889, NCI-H1963, NCI-H1417, NCI-H146等的增殖，并誘導(dǎo)細(xì)胞凋亡。最近研究顯示，ABT-737作用于ATLL細(xì)胞，明顯誘導(dǎo)HTLV-1感染的T細(xì)胞凋亡。ABT-737按100 mg/kg劑量作用于ATLL鼠模型顯示出強(qiáng)抗癌活性。[5]
激酶實(shí)驗(yàn) 熒光偏振實(shí)驗(yàn)
測定GST-BCL-2蛋白家族與FITC-BIM BH3域結(jié)合的親和力。100 nM GST-BCL-2家族融合蛋白和不同濃度 ABT-737在PBS溫育2分鐘。然后，加入20 nM FITC-BIM BH3 肽。進(jìn)行熒光偏振，測定IC50值。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 SCLC細(xì)胞系，包括NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR,和DMS114
濃度 0.001-10 μM
孵育時(shí)間 48小時(shí)
方法

SCLC細(xì)胞在含10%人血漿的 100 μL 組織培養(yǎng)基的96孔培養(yǎng)板上處理48小時(shí)，使用MTS測定存活細(xì)胞。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot PARP / c-PARP / cleaved caspase 3 Hif-1a γ-H2AX / p-ATM 21393866
Immunofluorescence cytochrome C Bax Bim AIF p65 26447615
Growth inhibition assay Cell viability 22311987
ELISA IL-6 / IL-8 21084274
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 ABT-737按30 mg/kg劑量作用于白血病模型，抑制白血病負(fù)擔(dān)值達(dá)53% , 且明顯延長鼠壽命。ABT-737不會(huì)引起血細(xì)胞數(shù)和血漿化學(xué)性質(zhì)發(fā)生變話。[1] ABT-737延長移植BCL-2傳感腫瘤的鼠壽命。[2] ABT-737按100 mg/kg劑量作用于ATLL鼠模型具有強(qiáng)抗癌活性。[5]
動(dòng)物實(shí)驗(yàn) Animal Models 注射ER細(xì)胞的Scid 鼠
Dosages 20 mg/kg和30 mg/kg
Administration 腹腔注射

化學(xué)信息&溶解度

分子量 813.43 分子式

C42H45ClN6O5S2
CAS號(hào) 852808-04-9 SDF Download ABT-737 SDF
Smiles CN(C)CCC(CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-]
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (122.93 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 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.

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