HER2-IN-7 is a potent inhibitor of HER2. Deregulation of ErbB family signalling modulates proliferation, invasion, metastasis, angiogenesis, and tumour cell survival. HER2-IN-7 has the potential for the research of diseases associated ErbBs (especially HER2), including cancer (extracted from patent WO2019214634A1, compound 23)[1].
分子量
565.55
Formula
C28H26F3N7O3
CAS 号
2387574-01-6
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]. Zhengtao LI, et al. Erbb receptor inhibitors. Patent WO2019214634A1.
HER2-IN-7 is a potent inhibitor of HER2. Deregulation of ErbB family signalling modulates proliferation, invasion, metastasis, angiogenesis, and tumour cell survival. HER2-IN-7 has the potential for the research of diseases associated ErbBs (especially HER2), including cancer (extracted from patent WO2019214634A1, compound 23)[1].
分子量
565.55
Formula
C28H26F3N7O3
CAS 号
2387574-01-6
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]. Zhengtao LI, et al. Erbb receptor inhibitors. Patent WO2019214634A1.
HER2-IN-7 is a potent inhibitor of HER2. Deregulation of ErbB family signalling modulates proliferation, invasion, metastasis, angiogenesis, and tumour cell survival. HER2-IN-7 has the potential for the research of diseases associated ErbBs (especially HER2), including cancer (extracted from patent WO2019214634A1, compound 23)[1].
分子量
565.55
Formula
C28H26F3N7O3
CAS 号
2387574-01-6
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]. Zhengtao LI, et al. Erbb receptor inhibitors. Patent WO2019214634A1.
HER2-IN-8 is a HER-2 inhibitor extracted from patent WO2021179274A1 compound 107. HER2-IN-8 can be used for the research of cancer and inflammation[1].
IC50 & Target[1]
HER2
分子量
549.53
Formula
C26H25F2N9O3
CAS 号
2704630-49-7
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]. Zhou D, et, al. ErbB RECEPTOR INHIBITORS AS ANTI-TUMOR AGENTS. WO2021179274A1.
HER2-IN-8 is a HER-2 inhibitor extracted from patent WO2021179274A1 compound 107. HER2-IN-8 can be used for the research of cancer and inflammation[1].
IC50 & Target[1]
HER2
分子量
549.53
Formula
C26H25F2N9O3
CAS 号
2704630-49-7
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]. Zhou D, et, al. ErbB RECEPTOR INHIBITORS AS ANTI-TUMOR AGENTS. WO2021179274A1.
HER2-IN-8 is a HER-2 inhibitor extracted from patent WO2021179274A1 compound 107. HER2-IN-8 can be used for the research of cancer and inflammation[1].
IC50 & Target[1]
HER2
分子量
549.53
Formula
C26H25F2N9O3
CAS 号
2704630-49-7
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]. Zhou D, et, al. ErbB RECEPTOR INHIBITORS AS ANTI-TUMOR AGENTS. WO2021179274A1.
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.
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity[1].
IC50 & Target[1]
HER4
8.5 nM (IC50)
HER2
13 nM (IC50)
Human HER2
36 nM (IC50)
EGFR
65 nM (IC50)
BMX
4.9 nM (IC50)
BLK
31 nM (IC50)
JAK3
33 nM (IC50)
SLK
25 nM (IC50)
LOK
86 nM (IC50)
Clinical Trial
分子量
504.58
Formula
C26H32N8O3
CAS 号
2088323-16-2
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Irie H, et al. TAS0728, a covalent-binding, HER2-selective kinase inhibitor shows potent antitumor activity in preclinical models. Mol Cancer Ther. 2019 Feb 20.
TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling[1].
IC50 & Target[1]
ErbB3
23 nM (IC50)
体外研究 (In Vitro)
TX1-85-1 possesses an anti-proliferation EC50s of 9.9, 11.5, and 16.9 μM for Ovcar8, HCC827 GR6, and PC9 GR4 cells, respectively[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
580.68
Formula
C32H36N8O3
CAS 号
1603845-32-4
运输条件
Room temperature in continental US; may vary elsewhere.
HER2/neu (654-662) GP2 is a nine amino acid peptide derived from the human epidermal growth factor receptor 2 (HER2/nue, 654–662), induces HLA-A2-restricted cytotoxic T lymphocytes (CTL) reactive to various epithelial cancers[1][2].
分子量
884.11
Formula
C42H77N9O11
CAS 号
160790-21-6
Sequence
Ile-Ile-Ser-Ala-Val-Val-Gly-Ile-Leu
Sequence Shortening
IISAVVGIL
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]. Sun Y, et al. Observing the temperature dependent transition of the GP2 peptide using terahertz spectroscopy. PLoS One. 2012;7(11):e50306.
[2]. Tanaka Y, et al. Modification of the HER2/NEU-derived tumor antigen GP2 improves induction of GP2-reactive cytotoxic T lymphocytes. Int J Cancer. 2001 Nov;94(4):540-4.
HER2-IN-6 is a potent inhibitor of HER2. HER2-IN-6 has the potential for the research of wild and/or mutant EGFR and/or HER2 kinase mediated tumor (extracted from patent WO2021164697A1, compound 11)[1].
分子量
504.58
Formula
C26H32N8O3
CAS 号
2691891-38-8
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]. Yihan Wang, et al. Substituted amide derivative and composition thereof and use thereof. Patent WO2021164697A1.
EGFR/HER2-IN-2 (Compound ZINC35560729) is a dual inhibitor of EGFR and HER2 with IC50 values of 5.02 µM and 0.83 µM against EGFR and HER2, respectively[1].
IC50 & Target
EGFR
5.02 μM (IC50)
HER2
0.83 μM (IC50)
分子量
453.49
Formula
C26H23N5O3
CAS 号
1215571-02-0
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]. Sangande, et al. 2-substituted 4-aminoquinazoline derivatives as potential dual inhibitors of EGFR and HER2: an in silico and in vitro study. Medicinal Chemistry Research 31.5 (2022): 762-771.
EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual inhibitor of EGFR and HER2[1].
IC50 & Target
EGFR
HER2
分子量
453.49
Formula
C26H23N5O3
CAS 号
1031620-09-3
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]. Sangande, et al. 2-substituted 4-aminoquinazoline derivatives as potential dual inhibitors of EGFR and HER2: an in silico and in vitro study. Medicinal Chemistry Research 31.5 (2022): 762-771.
pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFRT790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities[1].
IC50 & Target
EGFR
0.72 nM (IC50)
EGFR (L858R/T790M)
8.2 nM (IC50)
HER2
75.1 nM (IC50)
HER4
2.0 nM (IC50)
分子量
444.71
Formula
C19H15BrClN5O
CAS 号
1639040-95-1
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]. Tang Q, et al. Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. Eur J Med Chem. 2022 Apr 5;233:114249.