Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a KD of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor drug, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC)[1][2].
体外研究 (In Vitro)
Nimotuzumab (10 μg/mL; 24 hours) induces significant downregulation of CD16 on NK cells[1]. Nimotuzumab (10 μg/mL; 48 hours) induces the upregulation of PD-L1 molecule on DCs when co-cultured with the NK: DC: HNSCC cells[1]. The intrinsic properties of Nimotuzumab requires bivalent binding (i.e., binding with both antibody arms to two targets simultaneously) for stable attachment to cellular surface, which leads to Nimotuzumab selectively binding to cells that express moderate to high EGFR levels[2].
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.
Clinical Trial
CAS 号
780758-10-3
中文名称
尼妥珠单抗
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Zaima Mazorra, et al. Nimotuzumab Induces NK Cell Activation, Cytotoxicity, Dendritic Cell Maturation and Expansion of EGFR-Specific T Cells in Head and Neck Cancer Patients. Front Pharmacol. 2017 Jun 19;8:382.
[2]. Melarkode S Ramakrishnan, et al. Nimotuzumab, a promising therapeutic monoclonal for treatment of tumors of epithelial origin. MAbs. Jan-Feb 2009;1(1):41-8.
Trastuzumab is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
IC50 & Target[1]
HER2
体外研究 (In Vitro)
Treatment of HER2-overexpressing breast cancer cell lines with Trastuzumab results in induction of p27KIP1 and the Rb-related protein, p130, which in turn significantly reduces the number of cells undergoing S-phase. A number of other phenotypic changes are observed in vitro as a consequence of Trastuzumab binding to HER2-overexpressing cells. Interaction of Trastuzumab with the human immune system via its human immunoglobulin G1 Fc domain may potentiate its antitumor activities. in vitro studies demonstrate that Trastuzumab is very effective in mediating antibody-dependent cell-mediated cytotoxicity against HER2-overexpressing tumor targets[1]. Trastuzumab consists of two antigen-specific sites that bind to the juxtamembrane portion of the extracellular domain of the HER2 receptor and that prevent the activation of its intracellular tyrosine kinase. Trastuzumab recruits immune effector cells that are responsible for antibody-dependent cytotoxicity[2]. The presence of Trastuzumab IgG significantly increases killing of all breast cancer cell lines. The ADCC activity of PBMCs evoked by Trastuzumab is equally strong against Trastuzumab-sensitive (SKBR-3) or Trastuzumab-resistant (JIMT-1) breast cancer cells, with dose-dependent cell death reaching 50–60% killing at an effector/target ratio of 60:1[3].
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.
体内研究 (In Vivo)
Trastuzumab treatment of mouse xenograft models results in marked suppression of tumor growth. When given in combination with standard cytotoxic chemotherapeutic agents, Trastuzumab treatment generally results in statistically superior antitumor efficacy compared with either agent given alone[1]. Trastuzumab causes a significant growth inhibition of the outgrowth of macroscopic JIMT-1 xenograft tumors in both nude and SCID mice[3].
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.
Clinical Trial
分子量
145531.50
Formula
C6470H10012N1726O2013S42
CAS 号
180288-69-1
中文名称
曲妥珠单抗;曲妥单抗;群司珠单抗
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Sliwkowski MX, et al. Nonclinical studies addressing the mechanism of action of trastuzumab. Semin Oncol. 1999 Aug;26(4 Suppl 12):60-70.
[2]. Hudis CA, et al. Trastuzumab–mechanism of action and use in clinical practice. N Engl J Med. 2007 Jul 5;357(1):39-51.
[3]. Barok M, et al. Trastuzumab causes antibody-dependent cellular cytotoxicity-mediated growth inhibition of submacroscopic JIMT-1 breast cancer xenografts despite intrinsic drug resistance. Mol Cancer Ther. 2007 Jul;6(7):2065-72.
Cell Assay [3]
The effects of Trastuzumab and Trastuzumab-F(ab′)2 on the growth of JIMT-1, SKBR-3, and BT-474 cells are evaluated using the AlamarBlue method. Exponentially growing cells are harvested and plated in single wells of a 96-well flat-bottomed tissue culture plate at defined densities, ranging from 4,500-8,000 cells per well depending on the cell line. After overnight culture, the regular medium is exchanged to medium containing 0, 1, 10, or 100 μg/mL Trastuzumab or Trastuzumab-F(ab′) 2. Cell viability is tested after 72 h of treatment. Fluorescence is detected at an excitation of 544 nm, and emission is detected at 590 nm[3].
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 Administration [3]
Trastuzumab and Trastuzumab-F(ab′)2 are given at a dose of 5 and 25 μg/g, respectively, by weekly i.p. injection. The five times greater amount of administered F(ab′)2 is chosen based on the different half-lives of IgG and F(ab′) F(ab′)2. Control mice are treated with weekly i.p. injection of 100 μL physiologic saline (saline). Animals are euthanized by CO2 inhalation[3].
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.
参考文献
[1]. Sliwkowski MX, et al. Nonclinical studies addressing the mechanism of action of trastuzumab. Semin Oncol. 1999 Aug;26(4 Suppl 12):60-70.
[2]. Hudis CA, et al. Trastuzumab–mechanism of action and use in clinical practice. N Engl J Med. 2007 Jul 5;357(1):39-51.
[3]. Barok M, et al. Trastuzumab causes antibody-dependent cellular cytotoxicity-mediated growth inhibition of submacroscopic JIMT-1 breast cancer xenografts despite intrinsic drug resistance. Mol Cancer Ther. 2007 Jul;6(7):2065-72.
Cetuximab (C225) is a human IgG1 monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a Kd of 0.201 nM for EGFR by SPR. Cetuximab has potent antitumor activity[1].
IC50 & Target[1]
Soluble EGFR
0.201 nM (Kd)
EGFR
0.147 nM (Kd, Fixed A431 cells)
体外研究 (In Vitro)
Cetuximab (C225) is a monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a Kd of 0.201 nM for soluble EGFR by SPR. Cetuximab also exhibits a Kd of 0.147 nM for EGFR in fixed A431 cells by ELISA[1]. Cetuximab (C225; 30 nM) time-dependently inhibits the proliferation of SCC-1, SCC-11B, SCC-38, and SCC-13Y cells after treatment for 8 d. Cetuximab (30 nM) causes G0/G1 arrest, induces apoptosis, and reduces Rb, p27KIP1, Bcl-2, and Bax expression in SCC-13Y cells. Cetuximab (30 nM) also enhances radiosensitivity and increases radiation-induced apoptosis in SCC-13Y cells[3].
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.
体内研究 (In Vivo)
Cetuximab (1 mg/injection) has effect on the tumour volume but the effect is more pronounced on UT-SCC-14 xenografts. In UT-SCC-14 xenografts, Cetuximab treatment significantly reduces the expression of EGFR, pEGFR and Ki67. The MCT1 and GLUT1 expression is significantly decreased in the Cetuximab-treated groups of both cell lines but differences are more pronounced in UT-SCC-14 xenografts[2].
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.
Clinical Trial
分子量
145543.35
CAS 号
205923-56-4
中文名称
西妥昔单抗
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Goldstein NI, et al. Biological efficacy of a chimeric antibody to the epidermal growth factor receptor in a human tumor xenograft model. Clin Cancer Res. 1995 Nov;1(11):1311-8.
[2]. Gustafsson H, et al. EPR Oximetry of Cetuximab-Treated Head-and-Neck Tumours in a Mouse Model. Cell Biochem Biophys. 2017 Jul 29.
[3]. Huang SM, et al. Epidermal growth factor receptor blockade with C225 modulates proliferation, apoptosis, and radiosensitivity in squamous cell carcinomas of the head and neck. Cancer Res. 1999 Apr 15;59(8):1935-40.
Atezolizumab (MPDL3280A) is a selective humanized monoclonal IgG1 antibody against programmed death ligand 1 (PD-L1), used for cancer research.
体外研究 (In Vitro)
Atezolizumab (0, 2.5, 5, 10, 20, and 40 µg/ml; 24 hours; HOS and 143B cells) inhibits proliferation and induces immune-independent apoptosis of osteosarcoma cells[1]. Atezolizumab impairs the function of mitochondria to cause the imbalance between oxidants and antioxidants. Atezolizumab induces mitochondria-related apoptosis of osteosarcoma cells by activating JNK pathway. Atezolizumab (10 µg/ml; 24 hours; HOS and 143B cells) induces autophagy in osteosarcoma 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.
Clinical Trial
分子量
144590.50
CAS 号
1380723-44-3
中文名称
阿特珠单抗;阿替利珠单抗
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Cha E, et al. PD-L1 inhibition with MPDL3280A for solid tumors. Semin Oncol. 2015 Jun;42(3):484-7.
[2]. Liu Z, et al. Targeting autophagy enhances atezolizumab-induced mitochondria-related apoptosis in osteosarcoma. Cell Death Dis. 2021;12(2):164. Published 2021 Feb 8.
Rituximab(Synonyms: 利妥昔单抗; Anti-Human CD20 type I, Chimeric Antibody) 纯度: 98.42%
Rituximab 是一种抗 CD20 嵌合单克隆抗体,用于某些自身免疫疾病和癌症的研究。
Rituximab Chemical Structure
CAS No. : 174722-31-7
规格
价格
是否有货
数量
1 mg
¥2800
In-stock
5 mg
¥5600
In-stock
25 mg
询价
50 mg
询价
* Please select Quantity before adding items.
生物活性
Rituximab is an anti-CD20 chimeric monoclonal antibody used to treat certain autoimmune diseases and types of cancer.
体外研究 (In Vitro)
Rituximab inhibits the proliferation of stimulated human B cells, which is associated with a relative increase of B cells with an activated naive phenotype. Aside from this population shift, there are no major changes in phenotype or cytokine profile of the various B-cell subsets. B cells stimulated in the presence of rituximab induces stronger T-cell proliferation, compared to B cells stimulated in the absence of rituximab[1]. All lymphoma cells tested are equally sensitive to antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-mediated phagocytosis of tumor cells, and rituximab-induced apoptosis. Rituximab induces high CDC killing of follicular lymphoma cells[2].
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.
体内研究 (In Vivo)
A single injection of rituximab or the murine anti-CD20 Ab 1F5, given i.p. 1 day after the tumor, cures 100% of the animals. Depletion of either NK cells or neutrophils or both in tumor-injected animals does not affect the therapeutic activity of the drug. Similarly, rituximab is able to eradicate tumor cells in athymic nude mice, suggesting that its activity is T cell independent[3].
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.
Clinical Trial
分子量
144544.44
CAS 号
174722-31-7
中文名称
利妥昔单抗
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Kamburova EG, et al. In vitro effects of rituximab on the proliferation, activation and differentiation of human B cells. Am J Transplant. 2012 Feb;12(2):341-50.
[2]. Manches O, et al. In vitro mechanisms of action of rituximab on primary non-Hodgkin lymphomas. Blood. 2003 Feb 1;101(3):949-54.
[3]. Byrd JC, et al. The mechanism of tumor cell clearance by rituximab in vivo in patients with B-cell chronic lymphocytic leukemia: evidence of caspase activation and apoptosis induction. Blood. 2002 Feb 1;99(3):1038-43.
Cell Assay
A single injection of rituximab or the murine anti-CD20 Ab 1F5, given i.p. 1 day after the tumor, cures 100% of the animals. Depletion of either NK cells or neutrophils or both in tumor-injected animals does not affect the therapeutic activity of the drug. Similarly, rituximab is able to eradicate tumor cells in athymic nude mice, suggesting that its activity is T cell independent[3].
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 Administration [1]
C57BL/6 mice (8-10 wk of age) are inoculated 8×103 EL4-CD20+ cells in 200 μL of saline by tail vein injection. In parallel groups of mice, 150 g of rituximab, murine anti-CD20 IgG2a Ab 1F5, or control anti-human IL-2R Ab daclizumab in 300 μL of saline, or saline only is inoculated i.p. 24 h later[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.
参考文献
[1]. Kamburova EG, et al. In vitro effects of rituximab on the proliferation, activation and differentiation of human B cells. Am J Transplant. 2012 Feb;12(2):341-50.
[2]. Manches O, et al. In vitro mechanisms of action of rituximab on primary non-Hodgkin lymphomas. Blood. 2003 Feb 1;101(3):949-54.
[3]. Byrd JC, et al. The mechanism of tumor cell clearance by rituximab in vivo in patients with B-cell chronic lymphocytic leukemia: evidence of caspase activation and apoptosis induction. Blood. 2002 Feb 1;99(3):1038-43.
Nivolumab is a programmed death receptor-1 (PD-1) blocking human IgG4 antibody to treat advanced (metastatic) non-small cell lung cancer.
体外研究 (In Vitro)
Nivolumab binds to CHO cells expressing PD-1 with an EC50 of 1.66 nM, but does not bind to the parental CHO cell line. Nivolumab binds to PD-1 on activated T cells with an EC50 of 0.64 nM. Nivolumab also inhibits the interaction between PD-1 and its ligands, PD-L1 and PD-L2, with IC50 values of 2.52 and 2.59 nM, respectively. Nivolumab (1.5 ng/mL) can enhance T-cell reactivity in the presence of a T-cell receptor stimulus[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.
体内研究 (In Vivo)
Nivolumab (10 and 50 mg/kg, i.v.) is well tolerated in cynomolgus monkeys. Serum chemistry changes are limited to a reversible 28% decrease in T3 at week 13 in females treated with 50 mg/kg. T4 and TSH levels are unchanged. In males treated with 50 mg/kg, there are no changes in T3, T4, or TSH levels. Nivolumab exposure increases in an approximately dose-proportional manner between 10 and 50 mg/kg, with no substantial sex differences noted[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.
Clinical Trial
分子量
143599.09
CAS 号
946414-94-4
中文名称
纳武单抗;尼鲁单抗
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Wang C, et al. In vitro characterization of the anti-PD-1 antibody nivolumab, BMS-936558, and in vivo toxicology in non-human primates. Cancer Immunol Res. 2014 Sep;2(9):846-56.
Ipilimumab 是一种全人类单克隆抗体 IgG1κ,能够抗 CTLA-4(一种由活化的 T 细胞产生的免疫抑制分子)。
Ipilimumab Chemical Structure
CAS No. : 477202-00-9
规格
价格
是否有货
数量
1 mg
¥5500
In-stock
5 mg
询价
25 mg
询价
50 mg
询价
* Please select Quantity before adding items.
生物活性
Ipilimumab is a fully human monoclonal IgG1κ antibody against the cytotoxic T-lymphocyte antigen-4 (CTLA-4), an immune-inhibitory molecule expressed in activated T cells and in suppressor T regulatory cells.
体外研究 (In Vitro)
Ipilimumab inhibits CTLA-4, allowing the T cell immune response to be reactivated against tumor cells. Ipilimumab can promote antitumor activity as a single agent or in combination with cytokines, chemotherapy, or vaccines[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.
Clinical Trial
分子量
145313.36
CAS 号
477202-00-9
中文名称
易普利姆玛;伊匹单抗;伊匹木单抗
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Movva S, et al. The monoclonal antibody to cytotoxic T lymphocyte antigen 4, ipilimumab (MDX-010), a novel treatment strategy in cancer management. Expert Opin Biol Ther. 2009 Feb;9(2):231-41.
Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer[1][2].
体外研究 (In Vitro)
Trastuzumab emtansine (2 μg/mL; 3 d) significantly inhibits the proliferation of epithelial ovarian cancer (EOC) cells[2].
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.
体内研究 (In Vivo)
Trastuzumab emtansine (15 mg/kg; i.v. three to five times weekly for 3 weeks) exhibits significantly anti-tumor effect in mice[2].
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:
CB-17/SCID mice (6 weeks) were injected with OVA10 cells[2]
Dosage:
15 mg/kg
Administration:
I.v. three to five times weekly for 3 weeks
Result:
Showed remarkable inhibition of tumor growth in mice and was well tolerated.
Clinical Trial
CAS 号
1018448-65-1
中文名称
曲妥珠单抗-美坦新偶联物
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Verma S, et, al. Trastuzumab emtansine for HER2-positive advanced breast cancer. N Engl J Med. 2012 Nov 8;367(19):1783-91.
[2]. Menderes G, et, al. Superior in vitro and in vivo activity of trastuzumab-emtansine (T-DM1) in comparison to trastuzumab, pertuzumab and their combination in epithelial ovarian carcinoma with high HER2/neu expression. Gynecol Oncol. 2017 Oct;147(1):145-152.
Rovalpituzumab is a humanized monoclonal antibody against delta-like protein 3 (DLL3). Rovalpituzumab can be used in the synthesis of antibody-drug conjugate (ADC), Rovalpituzumab Tesirine[1]. Rovalpituzumab has activity against small cell lung cancer (SCLC)[1].
CAS 号
1613313-01-1
中文名称
洛伐妥珠单抗
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Bilal H Lashari, et al. Rovalpituzumab Tesirine: A Novel DLL3-Targeting Antibody-Drug Conjugate. Drugs R D. 2018 Dec;18(4):255-258.
Bemarituzumab is a first-in-class, humanized IgG1 monoclonal antibody against FGFR2b (a FGF receptor). Bemarituzumab blocks fibroblast growth factors from binding and activating FGFR2b. Bemarituzumab has the potential for cancer research[1].
CAS 号
1952272-74-0
中文名称
贝玛妥珠单抗
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Daniel Vt Catenacci, et al. Bemarituzumab with modified FOLFOX6 for advanced FGFR2-positive gastroesophageal cancer: FIGHT Phase III study design. Future Oncol. 2019 Jun;15(18):2073-2082.