GLPBio

BKT140

Catalog No.: GC17526Purity:>99.50%Synonyms: 4F-benzoyl-TN14003, BL-8040, Motixafortide, TF 14016
COASDSData Sheet
BKT140(BKT140 4-fluorobenzoyl)은 ~1 nM의 IC50 vakue를 갖는 새로운 CXCR4 길항제입니다.

제품은 연구용으로만 사용됩니다. 인체에 사용할 수 없으며 환자에게 판매하지 않습니다.

BKT140
Cas No.: 664334-36-5
1mgIn Stock
$76.00
1
5mgIn Stock
$252.00
1
10mgIn Stock
$356.00
1
25mgIn Stock
$710.00
1
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제품 설명 (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.

실험 프로토콜 (Protocol)

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.

제품 문서 (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

화학적 특성 (Chemical Properties)

CAS 번호
664334-36-5
동의어
4F-benzoyl-TN14003, BL-8040, Motixafortide, TF 14016
화학명
(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
분자식
C97H144FN33O19S2
분자량
2159.52
용해도
≥ 216mg/mL in DMSO
보관
Store at -20°C
일반 주의사항
제품의 용해도 데이터에 따라 적절한 용매를 선택하십시오. 조제 후에는 반복적인 동결·해동을 피할 수 있도록 저장 용액을 소분하십시오.
저장 용액은 -80°C 보관 시 6개월 이내, -20°C 보관 시 1개월 이내에 사용하십시오.
용해도를 높이려면 튜브를 37°C로 데운 뒤 적절한 시간 동안 초음파 처리하십시오.
배송 조건
평가용 샘플은 아이스팩과 함께 배송됩니다. 그 외 용량은 실온 배송되며, 요청 시 아이스팩과 함께 배송할 수 있습니다.

계산 도구 (Calculators)몰 농도 / 희석 / 분자량 / 단위 변환 / 생체 내 제형 / 용해도

g/mol

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