Fosbretabulin disodium | 康普瑞汀A4磷酸二钠 | Combretastatin A4 disodium phosphate | Tubulin Destabilizing Agent

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Fosbretabulin disodium/康普瑞汀磷酸二钠 {[allProObj[0].p_purity_real_show]}

货号：A116116 同义名： 康普瑞汀A4磷酸二钠 / Combretastatin A4 disodium phosphate; CA 4P

Fosbretabulin disodium 是 Combretastatin A4（CA4）的水溶性前药，CA4 是一种微管靶向化合物，能够与 β-微管蛋白结合，Kd 为 0.4 μM（在无细胞实验中）。Fosbretabulin disodium 可抑制微管蛋白的聚合，IC50 为 2.4 μM，并破坏肿瘤血管结构。

Fosbretabulin disodium/康普瑞汀磷酸二钠化学结构
CAS号：168555-66-6

Fosbretabulin disodium/康普瑞汀磷酸二钠 3D分子结构
CAS号：168555-66-6

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Fosbretabulin disodium/康普瑞汀磷酸二钠纯度/质量文件产品仅供科研

货号：A116116 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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Fosbretabulin disodium/康普瑞汀磷酸二钠生物活性

描述	Fosbretabulin disodium (CA 4DP) is a tubulin destabilizing agent and is a proagent of Combretastatin A4, specifically targeting endothelial cells. It induces the regression of nascent tumor neovessels, diminishes tumor blood flow, and leads to central tumor necrosis^[1].^[3].
体内研究	Additionally, administration of Fosbretabulin disodium (100 mg/kg; intraperitoneally) has been shown to increase the mean arterial blood pressure (MABP) 1 and 6 hours post-administration and reduce tumor blood flow in rats^[3].
体外研究	Fosbretabulin disodium effectively inhibits the growth of various cancer cell lines including leukemia P-388, pancreas BXPC-3, neuroblastoma SK-N-SH, thyroid SW1736, lung-NSC NCI-H460, prostate DU-145, and pharynx FADU, displaying EC50 values ranging from 0.00025 to 0.23 μg/mL^[2].

Fosbretabulin disodium/康普瑞汀磷酸二钠细胞实验

Cell Line b3NULL endothelial cells b3HET endothelial cells b3WT endothelial cells	Concentration	Treated Time	Description	References
b3NULL endothelial cells	0.5 μM	15 h	Test the effect of Fosbretabulin on random migration of b3NULL endothelial cells, results showed b3NULL cells were sensitive to Fosbretabulin.	EMBO Rep. 2018 Jul;19(7):e44578.
b3HET endothelial cells	0.5 μM	15 h	Test the effect of Fosbretabulin on random migration of b3HET endothelial cells, results showed b3HET cells were sensitive to Fosbretabulin.	EMBO Rep. 2018 Jul;19(7):e44578.
b3WT endothelial cells	0.5 μM	15 h	Test the effect of Fosbretabulin on random migration of b3WT endothelial cells, results showed b3WT cells were insensitive to Fosbretabulin.	EMBO Rep. 2018 Jul;19(7):e44578.

Fosbretabulin disodium/康普瑞汀磷酸二钠动物实验

Species Nude mice Mice	Animal Model DLD-1 and HT29 xenograft tumor models Subcutaneous tumor model	Administration	Dosage	Frequency	Description	References
Nude mice	DLD-1 and HT29 xenograft tumor models	Intraperitoneal injection	250 mg/kg	Once weekly for 5 weeks	Evaluate the antitumor efficacy of Fosbretabulin on DLD-1 and HT29 xenograft tumors	Int J Mol Sci. 2021 Dec 3;22(23):13082
Mice	Subcutaneous tumor model	Intraperitoneal injection	50 mg/kg	Every 4 days for 21 days	Test the effect of Fosbretabulin on tumor growth and angiogenesis, results showed Fosbretabulin reduced tumor growth and vascular density in Cre-positive animals.	EMBO Rep. 2018 Jul;19(7):e44578.

Fosbretabulin disodium/康普瑞汀磷酸二钠动物研究

Dose	Mice: 150 mg/kg^[3] (i.p.) Rat: 3 mg/kg^[4] (i.p.),
Administration	i.p.

Fosbretabulin disodium/康普瑞汀磷酸二钠临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00507429	Anaplastic Thyroid Cancer	Phase 2 Phase 3	Terminated(Low rate of subject... 展开 >> accrual) 收起 <<	-	-
NCT00395434	Tumors	Phase 1	Completed	-	United Kingdom ... 展开 >> Mount Vernon Hospital Northwood, Middlesex, United Kingdom, HA6 2RN Royal Marsden Hospital Sutton, Surrey, United Kingdom, SM2 5PT 收起 <<
NCT00653939	Tumors	Phase 2	Completed	-	United States, California ... 展开 >> 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 收起 <<

Fosbretabulin disodium/康普瑞汀磷酸二钠参考文献

[1]Shen CH, et, al. Combretastatin A-4 inhibits cell growth and metastasis in bladder cancer cells and retards tumour growth in a murine orthotopic bladder tumour model. Br J Pharmacol. 2010 Aug;160(8):2008-27.

[2]Pettit GR, et, al. Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41. J Med Chem. 2005 Jun 16;48(12):4087-99.

[3]Tozer GM, et, al. Combretastatin A-4 phosphate as a tumor vascular-targeting agent: early effects in tumors and normal tissues. Cancer Res. 1999 Apr 1;59(7):1626-34.

Fosbretabulin disodium/康普瑞汀磷酸二钠实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.36mL

2.27mL

1.14mL

22.71mL

4.54mL

2.27mL

Fosbretabulin disodium/康普瑞汀磷酸二钠技术信息

CAS号	168555-66-6
分子式	C₁₈H₁₉Na₂O₈P
分子量	440.29
SMILES Code	O=P([O-])([O-])OC1=CC(/C=C\C2=CC(OC)=C(OC)C(OC)=C2)=CC=C1OC.[Na+].[Na+]
MDL No.	MFCD00943911

别名	康普瑞汀A4磷酸二钠 ;Combretastatin A4 disodium phosphate; CA 4P; CRC 87-09; Combrestatin A4; Combrestatin A4 3'-O-Phosphate (sodium salt); CA 4DP
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

H₂O: 4 mg/mL(9.08 mM)

动物实验：配制的工作液建议现用现配，短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00507429	Anaplastic Thyroid Cancer	Phase 2 Phase 3	Terminated(Low rate of subject... 展开 >> accrual) 收起 <<	-	-
NCT00395434	Tumors	Phase 1	Completed	-	United Kingdom ... 展开 >> Mount Vernon Hospital Northwood, Middlesex, United Kingdom, HA6 2RN Royal Marsden Hospital Sutton, Surrey, United Kingdom, SM2 5PT 收起 <<
NCT00653939	Tumors	Phase 2	Completed	-	United States, California ... 展开 >> 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 收起 <<
NCT00507429	-		Terminated(Low rate of subject... 展开 >> accrual) 收起 <<	-	-
NCT01052363	Central Nervous System Tumors	Phase 1	Withdrawn(No funding)	-	United States, West Virginia ... 展开 >> MBRCC, West Virginia University Morgantown, West Virginia, United States, 26506 收起 <<
NCT00077103	Head and Neck Cancer	Phase 1 Phase 2	Terminated(slow accrual)	-	United States, Michigan ... 展开 >> 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 收起 <<
NCT00003768	Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 <<	Phase 1	Completed	-	United States, Ohio ... 展开 >> Ireland Cancer Center Cleveland, Ohio, United States, 44106-5065 收起 <<
NCT00003698	Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 <<	Phase 1	Completed	-	United Kingdom ... 展开 >> Mount Vernon Hospital Northwood, England, United Kingdom, HA6 2RN 收起 <<
NCT02279602	Neuroendocrine Tumors	Phase 2	Completed	-	United States, California ... 展开 >> 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 收起 <<
NCT01305213	Recurrent Fallopian Tube Carci... 展开 >>noma Recurrent Ovarian Carcinoma Recurrent Primary Peritoneal Carcinoma 收起 <<	Phase 2	Completed	-	-
NCT02132468	-		Completed	-	-
NCT00653939	-		Completed	-	-
NCT02132468	Neuroendocrine Tumors	Phase 2	Completed	-	United States, California ... 展开 >> 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 收起 <<
NCT00113438	Cancer Tumor	Phase 2	Completed	-	United States, Utah ... 展开 >> Huntsman Cancer Institute Salt Lake City, Utah, United States, 84112 收起 <<
NCT01305213	-		Completed	-	-
NCT01701349	Anaplastic Thyroid Cancer	Phase 3	Withdrawn(Expected inability t... 展开 >>o recruit study participants in a reasonable amount of time.) 收起 <<	December 2017	-
NCT01423149	Choroidal Neovascularization ... 展开 >> Myopia, Degenerative 收起 <<	Phase 2	Completed	-	-
NCT00060242	Head and Neck Cancer	Phase 2	Completed	-	United States, Michigan ... 展开 >> 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 收起 <<
NCT02641639	Platinum Resistant Ovarian Can... 展开 >>cer 收起 <<	Phase 2 Phase 3	Terminated(Interim analysis fa... 展开 >>iled to show efficacy benefit) 收起 <<	-	-
NCT01023295	Polypoidal Choroidal Vasculopa... 展开 >>thy 收起 <<	Phase 2	Completed	-	United States, California ... 展开 >> 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 收起 <<
NCT01570790	Combretastatin A4 Phosphate ... 展开 >> Age-related Macular Degeneration AMD CNV Choroidal Neovascularization 收起 <<	Phase 1 Phase 2	Completed	-	United States, Maryland ... 展开 >> Wilmer Eye Institute Baltimore, Maryland, United States, 21287 收起 <<
NCT03014297	Neuroendocrine Tumors ... 展开 >> Everolimus 收起 <<	Phase 1	Active, not recruiting	June 30, 2019	United States, Kentucky ... 展开 >> University of Kentucky Markey Cancer Center Lexington, Kentucky, United States, 40502 收起 <<
NCT02055690	Ovarian Neoplasms ... 展开 >> Neoplasms, Ovarian Ovarian Cancer 收起 <<	Phase 1 Phase 2	Terminated(Safety)	-	United Kingdom ... 展开 >> 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 收起 <<

HeLa cells	Proliferation assay	Antiproliferative activity against human HeLa cells by sulforhodamine B assay, IC50=0.0047 μM	20973488
rat A10 cells	Function assay	Inhibition of microtubule depolymerization in rat A10 cells assessed as reorganization of interphase microtubule network by indirect immunofluorescence technique, EC50=0.007 μM	20973488
SKOV3 cells	Proliferation assay	Antiproliferative activity against human SKOV3 cells by sulforhodamine B assay, IC50=0.0045 μM	20973488

Fosbretabulin disodium/康普瑞汀磷酸二钠 {[allProObj[0].p_purity_real_show]}

Fosbretabulin disodium/康普瑞汀磷酸二钠纯度/质量文件产品仅供科研

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Fosbretabulin disodium/康普瑞汀磷酸二钠质控信息

Fosbretabulin disodium/康普瑞汀磷酸二钠生物活性

Fosbretabulin disodium/康普瑞汀磷酸二钠细胞实验

Fosbretabulin disodium/康普瑞汀磷酸二钠动物实验

Fosbretabulin disodium/康普瑞汀磷酸二钠动物研究

Fosbretabulin disodium/康普瑞汀磷酸二钠临床研究

Fosbretabulin disodium/康普瑞汀磷酸二钠参考文献

Fosbretabulin disodium/康普瑞汀磷酸二钠实验方案

Fosbretabulin disodium/康普瑞汀磷酸二钠技术信息

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Fosbretabulin disodium/康普瑞汀磷酸二钠 细胞实验

Fosbretabulin disodium/康普瑞汀磷酸二钠 动物实验

Fosbretabulin disodium/康普瑞汀磷酸二钠 动物研究

Fosbretabulin disodium/康普瑞汀磷酸二钠 临床研究

Fosbretabulin disodium/康普瑞汀磷酸二钠 参考文献

Fosbretabulin disodium/康普瑞汀磷酸二钠 实验方案

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Fosbretabulin disodium/康普瑞汀磷酸二钠纯度/质量文件产品仅供科研

Fosbretabulin disodium/康普瑞汀磷酸二钠质控信息

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Fosbretabulin disodium/康普瑞汀磷酸二钠细胞实验

Fosbretabulin disodium/康普瑞汀磷酸二钠动物实验

Fosbretabulin disodium/康普瑞汀磷酸二钠动物研究

Fosbretabulin disodium/康普瑞汀磷酸二钠临床研究

Fosbretabulin disodium/康普瑞汀磷酸二钠参考文献

Fosbretabulin disodium/康普瑞汀磷酸二钠实验方案

Fosbretabulin disodium/康普瑞汀磷酸二钠技术信息