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CAS No.: 117048-59-6
Synonyms: CRC 87-09;CA-4;Combrestatin A4
Combretastatin A4 is a tubulin polymerization inhibitor with Kd value of 0.4 μM for binding to β-tubulin.
生物活性
靶点 | β-tubulin Kd:0.4μM |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|---|---|---|---|---|
NCT00395434 | Tumors | Phase 1 | Completed | - | United Kingdom ... more >> Mount Vernon Hospital Northwood, Middlesex, United Kingdom, HA6 2RN Royal Marsden Hospital Sutton, Surrey, United Kingdom, SM2 5PT Collapse << |
NCT00507429 | Anaplastic Thyroid Cancer | Phase 2 Phase 3 | Terminated(Low rate of subject... more >> accrual) Collapse << | - | - |
NCT00003698 | Unspecified Adult Solid Tumor,... more >> Protocol Specific Collapse << | Phase 1 | Completed | - | United Kingdom ... more >> Mount Vernon Hospital Northwood, England, United Kingdom, HA6 2RN Collapse << |
实验方案
技术信息
CAS号 | 117048-59-6 | 储存条件 |
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分子式 | C18H20O5 | 运输 | 蓝冰 | |||||||
分子量 | 316.35 | 别名 | CRC 87-09;CA-4;Combrestatin A4;康普瑞汀 | |||||||
溶解度 |
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动物实验配方 |
Cell Lines | Concentration | Assay Type | Time | Activity Description | Data Sources |
---|
A10 cells | - | Growth inhibition assay | 48 h | Growth inhibition of rat A10 cells after 48 hrs by MTT assay, IC50=0.001 μM | 22044164 |
A-549 | - | Growth inhibition assay | - | Cytotoxic concentration required to inhibit 50% cell growth in A-549 lung carcinoma cell lines, ED50=1.20E-06 μM | 1875350 |
ACHN cell | - | Proliferation assay | - | Antiproliferative activity against drug resistant ACHN cell line expressing MDR1 by Alamar Blue assay, IC50=0.0016 μM | 17286393 |
BNL 1ME A.7R.1 cells | - | Cytotoxicity assay | - | Cytotoxicity against mouse BNL 1ME A.7R.1 cells, IC50=0.0009 μM | 25785605 |
Calu6 | - | Proliferation assay | 48 h | Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry, IC50=0.00094 μM | 21774499 |
CEM cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human CEM cells after 72 hrs by MTT assay, IC50=0.001 μM | 22676247 |
DU145 cells | - | Cytotoxicity assay | - | Cytotoxicity against human DU145 cells by SRB assay, GI50=0.00054 μM | 24016002 |
DU145 cells | - | Growth inhibition assay | - | Growth inhibition of human DU145 cells by sulforhodamine B assay, GI50=0.00054 μM | 23772309 |
DU145 cells | - | Cytotoxicity assay | 48 h | Cytotoxicity against human DU145 cells after 48 hrs by SRB assay, GI50=0.0008 μM | 18303849 |
DU145 cells | - | Cytotoxicity assay | - | Cytotoxicity against human DU145 cells by SRB assay, GI50=0.001 μM | 20496923 |
DU145 cells | - | Growth inhibition assay | 48 h | Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 |
H460 | - | Cytotoxicity assay | - | Cytotoxicity against human H460 cells by sulforhodamine B test, IC50=0.0012 μM | 18783207 |
H460 | - | Proliferation assay | - | Antiproliferative activity against human H460 cells, IC50=0.00124 μM | 16722633 |
HaCaT cells | - | Proliferation assay | - | Antiproliferative activity against human HaCaT cells assessed as cell viability by MTT assay, IC50=0.001 μM | 23063401 |
HCT 116 | - | Growth inhibition assay | - | Concentration which produces 50% inhibition of growth of human colon tumor HCT 116, IC50=0.0009 μM | 11714613 |
HCT116 cell | - | Cytotoxicity assay | - | Cytotoxicity against HCT116 cell line, IC50=0.00035 μM | 17249649 |
HCT116 cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human HCT116 cells assessed as reduction of [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50=0.00074 μM | 21955454 |
HCT116 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50=0.001 μM | 21112130 |
HCT116 cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.001 μM | 22676247 |
HCT15 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human HCT15 cells after 72 hrs by MTS assay, IC50=0.001 μM | 21112130 |
HeLa cell | - | Cytotoxicity assay | - | Cytotoxicity against HeLa cell line, IC50=0.0003 μM | 17249649 |
HeLa cells | - | Cytotoxicity assay | - | Cytotoxicity against human HeLa cells by MTT assay, IC50=0.00051 μM | 19879758 |
HeLa cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human HeLa cells after 72 hrs by resazurin based fluorescence assay, IC50=0.0009 μM | 24669888 |
HepG2 cells | - | Cytotoxicity assay | - | Cytotoxicity against human HepG2 cells, IC50=0.00014 μM | 17127061 |
HL60 cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.0001 μM | 20731355 |
HL60 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.001 μM | 21663319 |
HL60 cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | 22136312 |
HL60 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.001 μM | 22578111 |
HL60 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | 23117171 |
HL60 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test, IC50=0.001 μM | 25785605 |
HL60 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | 20420439 |
HL60 cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | 23445496 |
Hs578T cells | - | Growth inhibition assay | 48 h | Growth inhibition of human Hs578T cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 |
HT-29 | - | Growth inhibition assay | - | Cytotoxic concentration required to inhibit 50% cell growth in HT-29 colon adenocarcinoma cell lines, ED50=1.20E-06 μM | 1875350 |
HT-29 | - | Growth inhibition assay | - | Growth inhibition of human HT-29 cells by MTT assay, IC50=0.001 μM | 25689111 |
Human SH-SY5Y neuroblastoma cells | - | Function assay | - | Inhibitory concentration against Human SH-SY5Y neuroblastoma cells, IC50=0.0015 μM | 15963722 |
HuTu 80 cells | - | Proliferation assay | 72 h | Antiproliferative activity in human HuTu 80 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00137 μM | 22329561 |
HUVEC | - | Proliferation assay | - | Antiproliferative activity against human HUVEC, IC50=0.0015 μM | 16722633 |
HUVEC cells | - | Growth inhibition assay | 48 h | Growth inhibition of HUVEC cells after 48 hrs by MTT assay, IC50=0.001 μM | 22044164 |
K562 cells | - | Cytotoxicity assay | - | Cytotoxicity against human K562 cells, IC50=0.0014 μM | 19837594 |
KB cell | - | Proliferation assay | - | Antiproliferative activity against human KB cell line by methylene blue dye assay, IC50=0.0015 μM | 17034147 |
KBV1 cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human vinblastine-resistant KBV1 cells after 72 hrs by MTT assay, IC50=0.0004 μM | 20731355 |
KB-VIN10 cell | - | Proliferation assay | - | Antiproliferative activity against human KB-VIN10 cell line by methylene blue dye assay, IC50=0.0015 μM | 17034147 |
KB-VIN10 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human KB-VIN10 cells over-expressing P-gp 170/MDR1 after 72 hrs by methylene blue assay, IC50=0.0007 μM | 21641700 |
M14 | - | Cytotoxicity assay | - | In vitro cytotoxic activity was tested against human melanoma cancer (M14) cell line, GI50=0.0001 μM | 12729640 |
MCF-7 | - | Growth inhibition assay | - | Cytotoxic concentration required to inhibit 50% cell growth in MCF-7 breast carcinoma cell lines, ED50=3.80E-06 μM | 1875350 |
MCF7 cells | - | Proliferation assay | 72 h | Antiproliferative activity in human MCF7 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00111 μM | 22329561 |
MDA-MB-231 cells | - | Growth inhibition assay | 48 h | Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 |
MDA-MB-435 cells | - | Growth inhibition assay | 48 h | Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 |
MDA-MB-435 cells | - | Cytotoxicity assay | 72 h | Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50=0.001 μM | 22676247 |
MDA-MB-468 cells | - | Cytotoxicity assay | 4 days | Cytotoxicity against human MDA-MB-468 cells assessed as cell viability after 4 days by MTS assay, IC50=0.0011 μM | 24210503 |
melanoma B16 cell | - | Growth inhibition assay | - | Concentration which produces 50% inhibition of growth of murine melanoma B16 cell line, IC50=0.001 μM | 11714613 |
MLM melanoma cell | - | Growth inhibition assay | - | Cytotoxic concentration required to inhibit 50% cell growth in MLM melanoma cell lines, ED50=1.40E-06 μM | 1875350 |
Molt4/C8 cells | - | Proliferation assay | - | Antiproliferative activity against human Molt4/C8 cells, IC50=0.0016 μM | 17034150 |
Molt4/C8 cells | - | Proliferation assay | 3 days | Antiproliferative effect against human Molt4/C8 cells after 3 days, IC50=0.0016 μM | 17419607 |
NCI/ADR (MDR) cells | - | Function assay | - | Cell cycle arrest in NCI/ADR (MDR) cells by accumulation at G2/M phase, IC50=0.0015 μM | 16377187 |
NCI/ADR-RES cells | - | Growth inhibition assay | 48 h | Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 |
NCI/ADR-RES cells | - | Cytotoxicity assay | - | Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM | 23214452 |
NCI/ADR-RES cells | - | Cytotoxicity assay | 96 h | Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy, IC50=0.0013 μM | 25025991 |
NCIH460 cells | - | Cytotoxicity assay | 48 h | Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay, GI50=0.0006 μM | 18303849 |
NCI-H460 cells | - | Cytotoxicity assay | 72 h | Cytotoxic activity against human NCI-H460 cells after 72 hrs by sulforhodamine B test, IC50=0.0013 μM | 18396857 |
NCI-H522 cells | - | Growth inhibition assay | 48 h | Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 |
OVCAR3 | - | Growth inhibition assay | 48 h | Growth inhibition of human OVCAR3 cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 |
OVCAR8 cells | - | Growth inhibition assay | 96 h | Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs, IC50=0.0013 μM | 22044164 |
OVCAR8 cells | - | Cytotoxicity assay | 96 h | Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy, IC50=0.0013 μM | 25025991 |
OVCAR8 cells | - | Cytotoxicity assay | - | Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM | 23214452 |
PC3 cells | - | Growth inhibition assay | 48 h | Growth inhibition of human PC3 cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 |
RS4:11 cells | - | Proliferation assay | 72 h | Antiproliferative activity against human RS4:11 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test, IC50=0.0008 μM | 25785605 |
SKMEL-5 | - | Growth inhibition assay | - | Cytotoxic concentration required to inhibit 50% cell growth in SKMEL-5 melanoma cell lines, ED50=3.00E-08 μM | 1875350 |
SK-N-BE | - | Proliferation assay | 72 h | Antiproliferative activity in human SK-N-BE cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00058 μM | 22329561 |
SKOV3 | - | Cytotoxicity assay | - | Cytotoxicity against human SKOV3 cells by SRB assay, GI50=0.00042 μM | 24016002 |
SK-OV3 | - | Cytotoxicity assay | - | In vitro cytotoxic activity tested against human ovarian cancer (SK-OV3) cell line, GI50=0.0001 μM | 12729640 |
SK-OV-3 | - | Growth inhibition assay | 48 h | Growth inhibition of human SK-OV-3 after 48 hrs by SRB assay, GI50=0.00013 μM | 18722127 |
SKOV3 cells | - | Growth inhibition assay | - | Growth inhibition of human SKOV3 cells by sulforhodamine B assay, GI50=0.00042 μM | 23772309 |
SKOV3 cells | - | Growth inhibition assay | - | Growth inhibition of human SKOV3 cells by MTT assay, IC50=0.001 μM | 25689111 |
SW620 cells | - | Proliferation assay | 72 h | Antiproliferative activity in human SW620 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00152 μM | 22329561 |
ZR-75-1 | - | Cytotoxicity assay | - | Cytotoxicity against ZR-75-1 cell line, IC50=0.00024 μM | 17249649 |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|
NCT00395434 | Tumors | Phase 1 | Completed | - | United Kingdom ... more >> Mount Vernon Hospital Northwood, Middlesex, United Kingdom, HA6 2RN Royal Marsden Hospital Sutton, Surrey, United Kingdom, SM2 5PT Collapse << |
NCT00507429 | Anaplastic Thyroid Cancer | Phase 2 Phase 3 | Terminated(Low rate of subject... more >> accrual) Collapse << | - | - |
NCT00003698 | Unspecified Adult Solid Tumor,... more >> Protocol Specific Collapse << | Phase 1 | Completed | - | United Kingdom ... more >> Mount Vernon Hospital Northwood, England, United Kingdom, HA6 2RN Collapse << |
NCT00507429 | - | - | Terminated(Low rate of subject... more >> accrual) Collapse << | - | - |
NCT00003768 | Unspecified Adult Solid Tumor,... more >> Protocol Specific Collapse << | Phase 1 | Completed | - | United States, Ohio ... more >> Ireland Cancer Center Cleveland, Ohio, United States, 44106-5065 Collapse << |
NCT01305213 | - | - | Completed | - | - |
NCT00653939 | Tumors | Phase 2 | Completed | - | United States, California ... more >> Southbay Oncology Hematology Campbell, California, United States, 95008 Pacific Coast Hematology and Oncology Medical Group Fountain Valley, California, United States, 92708 UCLA Division of Hematology and Oncology Los Angeles, California, United States, 90095 Bay Area Cancer Research Group, LLC Pleasant Hill, California, United States, 94523 United States, Florida Boca Raton Comprehensive Cancer Center Boca Raton, Florida, United States, 21020 United States, Kentucky Kentuckiana Cancer Institute Louisville, Kentucky, United States, 40202 United States, Massachusetts Lahey Clinic Medical Center Burlington, Massachusetts, United States, 01805 United States, New Jersey The Center for Cancer and Hematologic Disease Cherry Hill, New Jersey, United States, 08003 United States, New Mexico San Juan Oncology Associates Farmington, New Mexico, United States, 87401 United States, Ohio Gabrail Cancer Center Canton, Ohio, United States, 44718 The Mark H. Zangmeister Center Columbus, Ohio, United States, 43219 Signal Point Clinical Research Middletown, Ohio, United States, 45042 United States, Virginia Blueridge Cancer Care Salem, Virginia, United States, 24153 United States, Washington Northwest Medical Specialties Tacoma, Washington, United States, 98405 United States, West Virginia Mary Babb Randolph Cancer Center-Clinical Trials Unit Morgantown, West Virginia, United States, 26506 Collapse << |
NCT01305213 | Recurrent Fallopian Tube Carci... more >>noma Recurrent Ovarian Carcinoma Recurrent Primary Peritoneal Carcinoma Collapse << | Phase 2 | Completed | - | - |
NCT01052363 | Central Nervous System Tumors | Phase 1 | Withdrawn(No funding) | - | United States, West Virginia ... more >> MBRCC, West Virginia University Morgantown, West Virginia, United States, 26506 Collapse << |
NCT01023295 | Polypoidal Choroidal Vasculopa... more >>thy Collapse << | Phase 2 | Completed | - | United States, California ... more >> OXiGENE Investigational Site Los Angeles, California, United States Hong Kong OXiGENE Investigational Site Hong Kong, Hong Kong Korea, Republic of OXiGENE Investigational Site Seoul, Korea, Republic of Singapore OXiGENE Investigational Site Singapore, Singapore Taiwan OXiGENE Investigational Site Changhua, Taiwan Collapse << |
NCT00077103 | Head and Neck Cancer | Phase 1 Phase 2 | Terminated(slow accrual) | - | United States, Michigan ... more >> Josephine Ford Cancer Center at Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, Ohio Ireland Cancer Center at University Hosptials Case Medical Center, Case Comprehensive Cancer Center Cleveland, Ohio, United States, 44106-5065 United States, Pennsylvania Hillman Cancer Center at University of Pittsburgh Cancer Institute Pittsburgh, Pennsylvania, United States, 15232 Collapse << |
NCT00653939 | - | - | Completed | - | - |
NCT02132468 | Neuroendocrine Tumors | Phase 2 | Completed | - | United States, California ... more >> Stanford University School of Medicine Stanford, California, United States, 94305 United States, Kentucky Markey Cancer Center, Clinical Research Office Lexington, Kentucky, United States, 40356 United States, New York Montefiore Bronx, New York, United States, 10467 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Wisconsin Froedtert Hospital, Medicial College of Wisconsin Milwaukee, Wisconsin, United States, 53226 Collapse << |
NCT02132468 | - | - | Completed | - | - |
NCT03014297 | Neuroendocrine Tumors ... more >> Everolimus Collapse << | Phase 1 | Active, not recruiting | June 30, 2019 | United States, Kentucky ... more >> University of Kentucky Markey Cancer Center Lexington, Kentucky, United States, 40502 Collapse << |
NCT00060242 | Head and Neck Cancer | Phase 2 | Completed | - | United States, Michigan ... more >> Josephine Ford Cancer Center at Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, Ohio Ireland Cancer Center at University Hosptials Case Medical Center, Case Comprehensive Cancer Center Cleveland, Ohio, United States, 44106-5065 United States, Pennsylvania Hillman Cancer Center at University of Pittsburgh Cancer Institute Pittsburgh, Pennsylvania, United States, 15232 Collapse << |
NCT02055690 | Ovarian Neoplasms ... more >> Neoplasms, Ovarian Ovarian Cancer Collapse << | Phase 1 Phase 2 | Terminated(Safety) | - | United Kingdom ... more >> Royal United Hospital Bath NHS Trust Bath, United Kingdom, BA1 3NG City Hospital Birmingham, United Kingdom, B18 7GH University Hospitals Bristol NHS Foundation Trust Bristol, United Kingdom, BS1 3NU University Collage London Hospitals NHS Foundation Trust London, United Kingdom, NW1 2PG The Royal Marsden NHS Foundation Trust London, United Kingdom, SM2 5PT The Christie NHS Foundation Trust Manchester, United Kingdom, M20 4BX Clatterbridge Centre for Oncology NHS Foundation Trust Merseyside, United Kingdom, CH63 4JY Mount Vernon Cancer Centre (East and North Herts NHS Trust) Middlesex, United Kingdom, HA6 2RN Freeman Hospital (Newcastle-upon-Tyne Hospitals NHS Foundation Trust) Newcastle-upon-Tyne And Wear, United Kingdom, NE7 7DN Oxford Radcliffe Hospitals NHS Trust Oxford, United Kingdom, OX3 9DU Collapse << |
NCT00113438 | Cancer Tumor | Phase 2 | Completed | - | United States, Utah ... more >> Huntsman Cancer Institute Salt Lake City, Utah, United States, 84112 Collapse << |
NCT01701349 | Anaplastic Thyroid Cancer | Phase 3 | Withdrawn(Expected inability t... more >>o recruit study participants in a reasonable amount of time.) Collapse << | December 2017 | - |
NCT01570790 | Combretastatin A4 Phosphate ... more >> Age-related Macular Degeneration AMD CNV Choroidal Neovascularization Collapse << | Phase 1 Phase 2 | Completed | - | United States, Maryland ... more >> Wilmer Eye Institute Baltimore, Maryland, United States, 21287 Collapse << |
NCT02279602 | Neuroendocrine Tumors | Phase 2 | Completed | - | United States, California ... more >> Stanford University School of Medicine Stanford, California, United States, 94305 United States, Kentucky Markey Cancer Center, Clinical Research Office Lexington, Kentucky, United States, 40356 United States, New York Montefiore Bronx, New York, United States, 10467 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Wisconsin Froedtert Hospital, Medicial College of Wisconsin Milwaukee, Wisconsin, United States, 53226 Collapse << |
NCT01423149 | Choroidal Neovascularization ... more >> Myopia, Degenerative Collapse << | Phase 2 | Completed | - | - |
NCT02641639 | Platinum Resistant Ovarian Can... more >>cer Collapse << | Phase 2 Phase 3 | Terminated(Interim analysis fa... more >>iled to show efficacy benefit) Collapse << | - | - |
靶点 | Description | IC50 |
---|---|---|
β-tubulin | Kd:0.4μM |
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