GlpBio

BKT140

目录号: GC17526纯度: >99.50%同义词: BKT140 (4-fluorobenzoyl); BL-8040; TF14016
A CXCR4 antagonist
BKT140
Cas No.: 664334-36-5
规格价格库存数量操作
1mg¥777.00现货
1
5mg¥2,573.00现货
1
10mg¥3,633.00现货
1
25mg¥7,235.00现货
1
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产品描述 Description

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.

实验参考方法 Experimental Reference Method

Cell experiment:

Hematopoietic cancer cells are incubated with different concentrations of Motixafortide (BKT140) or AMD3100 for 24 hours. Motixafortide (BKT140) is treated with 1M hydrochloric acid (HCL) to achieve a pH of 2.7 to 3 at room temperature for 30 minutes and the pH is adjusted to 7 using concentrated NaOH. Proteinase K is added to Motixafortide (BKT140) at a final concentration of 100 mg/mL, incubated at 37°C for 1 hour, and inactivated by heat treatment (65°C for 30 minutes). After incubation, cells are stained with propidium iodide and the percent of viable PI-negative cells in culture is determined[2].

Animal experiment:

Mice: Severe combined immune-deficient (SCID)/beige mice (C.B-17/IcrHsd-SCID-bg) are used in the study. NB4 cells resuspended in PBS are injected subcutaneously into the flanks of the mice (200 mL per mouse containing 5×106 cells). Tumor growth is monitored daily, and mice are randomized to drug-treated or control PBS-treated groups (10 mice per group) when the tumor size (width×length) reaches 0.04 cm2. BKT140 is administered subcutaneously at a dose of 200 mg per mouse each day for 5 days[2].

References:

[1]. Peled A, et al. The high-affinity CXCR4 antagonist BKT140 is safe and induces a robust mobilization of human CD34+ cellsin patients with multiple myeloma. Clin Cancer Res. 2014 Jan 15;20(2):469-79.
[2]. Beider K, et al. CXCR4 antagonist 4F-benzoyl-TN14003 inhibits leukemia and multiple myeloma tumor growth. Exp Hematol. 2011 Mar;39(3):282-92.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
664334-36-5
同义词
BKT140 (4-fluorobenzoyl); BL-8040; TF14016
化学名
(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)-
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
分子式
C97H144FN33O19S2
分子量
2159.52 g/mol
溶解性
≥ 216mg/mL in DMSO
保存条件
Store at -20°C
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol