Toxins for Antibody-Drug Conjugate Research Library
生物活性
Eribulin (E7389) is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
体外研究 (In Vitro)
Eribulin (1-100 nM; 72 h) inhibits cells proliferation, with IC50s of 22.8 and 21.5 nM for LM8 and Dunn cells, respectively[1]. Eribulin (10-50 nM; 12-72 h) increases early apoptosis significantly after 24 h treatment at the dose of 50 nM in LM8 cells[1]. Eribulin (10-50 nM; 12-72 h) induces G2/M arrest by 12 h treatment with at the dose of 50 nM, but not by long-term treatment (72 h) with 10 nM in LM8 cells[1]. Eribulin (1-50 nM; 12 h) does not induce senescence in LM8 cells[1]. Eribulin (1-10 nM; 16 h) induces morphological change and suppresses cell migration in a low concentration in LM8 cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
Cell Line:
LM8 cells and Dunn cells
Concentration:
0, 1, 10, 100 nM
Incubation Time:
72 hours
Result:
Inhibited cells proliferation in a dose-dependent manner.
Apoptosis Analysis[1]
Cell Line:
LM8 cells
Concentration:
0, 10, 50 nM
Incubation Time:
12, 24, 48, 72 hours
Result:
Induced early apoptosis after 12 h at the concentration of 50 nM. Not detected apoptosis at the concentration of 10 nM.
Cell Cycle Analysis[1]
Cell Line:
LM8 cells
Concentration:
0, 10, 50 nM
Incubation Time:
12, 24, 48, 72 hours
Result:
Induced G2/M arrest by 12 h treatment with 50 nM. No G2/M arrest was induced by10 nM treatment.
体内研究 (In Vivo)
Eribulin (1 mg/kg; i.v. once a week for 2 weeks) reduces primary tumor growth and lung metastasis of osteosarcoma in mice[1]. Eribulin (1 mg/kg; once i.v.) suppresses circulating tumor cells (CTC) appearance in the low-concentration phase[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
C3H/HeN mice (4-week-old) are injected LM8 cells[1]
Dosage:
1 mg/kg
Administration:
I.v. once a week for 2 weeks
Result:
Suppressed primary tumor growth and induced apoptosis in tumor cells. Reduced lung metastasis. Decreased the body weights.
Clinical Trial
分子量
729.90
Formula
C40H59NO11
CAS 号
253128-41-5
中文名称
艾日布林
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[1]. Watanabe K, et, al. Low-dose eribulin reduces lung metastasis of osteosarcoma in vitro and in vivo. Oncotarget. 2019 Jan 4; 10(2): 161-174.
[2]. Okouneva, T., et al., Inhibition of centromere dynamics by eribulin (E7389) during mitotic metaphase. Mol Cancer Ther, 2008. 7(7): p. 2003-11.
[3]. Smith, J.A., et al., Eribulin binds at microtubule ends to a single site on tubulin to suppress dynamic instability. Biochemistry, 2010. 49(6): p. 1331-7.
[4]. Towle, M.J., et al., Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions. Cancer Res, 2011. 71(2): p. 496-505.
Eribulin-d3 mesylate is a deuterium labeled Eribulin mesylate. Eribulin mesylate is a microtubule targeting agent that is used for the research of cancer[1][2].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
829.02
Formula
C41H60D3NO14S
中文名称
甲磺酸艾日布林 d3 (甲磺酸盐)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et, al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
[2]. Watanabe K, et, al. Low-dose eribulin reduces lung metastasis of osteosarcoma in vitro and in vivo. Oncotarget. 2019 Jan 4;10(2):161-174.
Eribulin-d3 mesylate is a deuterium labeled Eribulin mesylate. Eribulin mesylate is a microtubule targeting agent that is used for the research of cancer[1][2].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
829.02
Formula
C41H60D3NO14S
中文名称
甲磺酸艾日布林 d3 (甲磺酸盐)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et, al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
[2]. Watanabe K, et, al. Low-dose eribulin reduces lung metastasis of osteosarcoma in vitro and in vivo. Oncotarget. 2019 Jan 4;10(2):161-174.
Eribulin-d3 mesylate is a deuterium labeled Eribulin mesylate. Eribulin mesylate is a microtubule targeting agent that is used for the research of cancer[1][2].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
829.02
Formula
C41H60D3NO14S
中文名称
甲磺酸艾日布林 d3 (甲磺酸盐)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et, al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
[2]. Watanabe K, et, al. Low-dose eribulin reduces lung metastasis of osteosarcoma in vitro and in vivo. Oncotarget. 2019 Jan 4;10(2):161-174.
Eribulin mesylate (E7389 mesylate) is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin mesylate inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
体外研究 (In Vitro)
Eribulin (1-100 nM; 72 h) inhibits cells proliferation, with IC50s of 22.8 and 21.5 nM for LM8 and Dunn cells, respectively[1]. Eribulin (10-50 nM; 12-72 h) increases early apoptosis significantly after 24 h treatment at the dose of 50 nM in LM8 cells[1]. Eribulin (10-50 nM; 12-72 h) induces G2/M arrest by 12 h treatment with at the dose of 50 nM, but not by long-term treatment (72 h) with 10 nM in LM8 cells[1]. Eribulin (1-50 nM; 12 h) does not induce senescence in LM8 cells[1]. Eribulin (1-10 nM; 16 h) induces morphological change and suppresses cell migration in a low concentration in LM8 cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
Cell Line:
LM8 cells and Dunn cells
Concentration:
0, 1, 10, 100 nM
Incubation Time:
72 hours
Result:
Inhibited cells proliferation in a dose-dependent manner.
Apoptosis Analysis[1]
Cell Line:
LM8 cells
Concentration:
0, 10, 50 nM
Incubation Time:
12, 24, 48, 72 hour
Result:
Induced early apoptosis after 12 h at the concentration of 50 nM. Not detected apoptosis at the concentration of 10 nM.
Cell Cycle Analysis[1]
Cell Line:
LM8 cells
Concentration:
0, 10, 50 nM
Incubation Time:
12, 24, 48, 72 hour
Result:
Induced G2/M arrest by 12 h treatment with 50 nM. No G2/M arrest was induced by10 nM treatment.
体内研究 (In Vivo)
Eribulin (1 mg/kg; i.v. once a week for 2 weeks) reduces primary tumor growth and lung metastasis of osteosarcoma in mice[1]. Eribulin (1 mg/kg; once i.v.) suppresses circulating tumor cells (CTC) appearance in the low-concentration phase[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
C3H/HeN mice (4-week-old) are injected LM8 cells[1]
Dosage:
1 mg/kg
Administration:
I.v. once a week for 2 weeks
Result:
Suppressed primary tumor growth and induced apoptosis in tumor cells. Reduced lung metastasis.
Clinical Trial
分子量
826.00
Formula
C41H63NO14S
CAS 号
441045-17-6
中文名称
甲磺酸艾日布林
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:
DMSO : ≥ 100 mg/mL (121.07 mM)
Ethanol : ≥ 100 mg/mL (121.07 mM)
*“≥” means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.2107 mL
6.0533 mL
12.1065 mL
5 mM
0.2421 mL
1.2107 mL
2.4213 mL
10 mM
0.1211 mL
0.6053 mL
1.2107 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
[1]. Watanabe K, et, al. Low-dose eribulin reduces lung metastasis of osteosarcoma in vitro and in vivo. Oncotarget. 2019 Jan 4; 10(2): 161-174.
[2]. Smith, J.A., et al., Eribulin binds at microtubule ends to a single site on tubulin to suppress dynamic instability. Biochemistry, 2010. 49(6): p. 1331-7.
[3]. Okouneva, T., et al., Inhibition of centromere dynamics by eribulin (E7389) during mitotic metaphase. Mol Cancer Ther, 2008. 7(7): p. 2003-11.
[4]. Towle, M.J., et al., Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions. Cancer Res, 2011. 71(2): p. 496-505.
VCP-Eribulin consists the ADCs linker (VCP) and Eribulin[1]. Eribulin is a mechanistically unique microtubule inhibitor for cancer[2]. VCP-Eribulin is an Eribulin-based drug for antibody conjugates[1].
IC50 & Target
Traditional Cytotoxic Agents
分子量
1135.34
Formula
C59H86N6O16
CAS 号
2130869-17-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Earl F Albone, et al. Eribulin-based antibody-drug conjugates and methods of use. US20170252458A1.
[2]. Towle MJ, et al. Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions. Cancer Res. 2011 Jan 15;71(2):496-505.
Mal-PEG2-VCP-Eribulin consists the ADCs linker (Mal-PEG2-VCP) and Eribulin[1]. Eribulin is a mechanistically unique microtubule inhibitor for cancer[2]. Mal-PEG2-VCP-Eribulin is an Eribulin-based drug for antibody conjugates[1].
IC50 & Target
Traditional Cytotoxic Agents
分子量
1374.57
Formula
C70H99N7O21
CAS 号
2130869-18-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[1]. Earl F Albone, et al. Eribulin-based antibody-drug conjugates and methods of use. US20170252458A1.
[2]. Towle MJ, et al. Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions. Cancer Res. 2011 Jan 15;71(2):496-505.
