BKT140
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BKT140, also known as BL-8040 and TF 14016, is an orally bioavailable inhibitor of CXC Chemokine Receptor 4 (CXCR4) with potential antineoplastic activity [1].
The G protein-coupled receptor CXCR4 plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types. CXCR4 has been involved in promoting tumor progression. CXCR4 expression is a prognostic marker in various types of cancer, such as acute myelogenous leukemia or breast carcinoma. CXCR4 acts as an important molecule involved in the spread and progression of a variety of different tumors [2].
BKT140 reduced the colony-forming capacity of non-small cell lung cancer (NSCLC) cells. Subcutaneous administration of BKT140 significantly delayed the development of H460 xenografts and showed a similar trend for A549 xenografts [1]. Pre-clinical studies in animal models with BKT140 showed a robust mobilization of white blood cells (WBC) and hematopoietic stem cells (HSC). BKT140 showed a direct anti-tumor effect against human-derived multiple myeloma (MM), lymphoma and primary leukemia cells and cell lines in vitro and in vivo, causing significant apoptosis [2]. BKT140 was well tolerated and rapidly absorbed in patients with multiple myeloma. BKT140 administration significantly increased the number of peripheral blood neutrophils, monocytes, lymphocytes, and CD34+ cells in a dose-dependent manner [3].
References:
[1] Fahham D, Weiss I D, Abraham M, et al. In vitro and in vivo therapeutic efficacy of CXCR4 antagonist BKT140 against human non–small cell lung cancer[J]. The Journal of thoracic and cardiovascular surgery, 2012, 144(5): 1167-1175. e1.
[2] Burger J A, Kipps T J. CXCR4: a key receptor in the crosstalk between tumor cells and their microenvironment[J]. Blood, 2006, 107(5): 1761-1767.
[3] Nagler A, Shimoni A, Avivi I, et al. BKT140 is a novel CXCR4 antagonist with stem cell mobilization and antimyeloma effects: an open-label first human trial in patients with multiple myeloma undergoing stem cell mobilization for autologous transplantation[J]. Blood, 2010, 116(21): 2260-2260.
Storage | Store at -20°C |
M.Wt | 2159.52 |
Cas No. | 664334-36-5 |
Formula | C97H144FN33O19S2 |
Solubility | ≥216 mg/mL in DMSO; ≥2.61 mg/mL in EtOH with gentle warming and ultrasonic; ≥52.4 mg/mL in H2O |
Chemical Name | (3S,6S,9S,12R,17R,20S,23S,26S,29S,34aS)-N-((S)-1-amino-5-guanidino-1-oxopentan-2-yl)-26,29-bis(4-aminobutyl)-17-((S)-2-((S)-2-((S)-2-(4-fluorobenzamido)-5-guanidinopentanamido)-5-guanidinopentanamido)-3-(naphthalen-2-yl)propanamido)-6-(3-guanidinopropyl)- |
SDF | Download SDF |
Canonical SMILES | NCCCC[C@@H]1NC(=O)[C@H](CCCNC(=O)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCCNC(=O)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]4CCCN4C(=O)[C@H](CCCCN)NC1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N)NC(=O)[C@H](Cc5ccc6ccccc6c5)NC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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