BKT140
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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
