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BL-8040

BL-8040 structure

CAS No.: 664334-36-5

Chemical Name:: BL-8040

Synonyms: Motixafortide;BKT140;TF14016;BL-8040;BKT140, >99%;BKT140 (BL-8040);4F-Benzoyl-TN14003;Motixafortide(TFA);Motixafortide(BKT140);BKT140 4-fluorobenzoyl

CBNumber:: CB03152184

Molecular Formula:: C97H144FN33O19S2

Molecular Weight:: 2159.52

MDL Number:

MOL File:: 664334-36-5.mol

Last updated:2024-07-02 08:54:57

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BL-8040 Properties

Density	1.52±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	≥216 mg/mL in DMSO; ≥2.61 mg/mL in EtOH with gentle warming and ultrasonic; ≥52.4 mg/mL in H2O
form	A crystalline solid
color	White to off-white
FDA UNII	DA9G065962

BL-8040 price

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
TRC	B591900	BKT140	664334-36-5	2.5mg	$605	2021-12-16	Buy
ChemScene	CS-6173	Motixafortide 98.27%	664334-36-5	25mg	$1200	2021-12-16	Buy
ChemScene	CS-6173	Motixafortide 98.27%	664334-36-5	1mg	$132	2021-12-16	Buy
ChemScene	CS-6173	Motixafortide 98.27%	664334-36-5	5mg	$396	2021-12-16	Buy
ApexBio Technology	B7833	BKT140	664334-36-5	10mg	$500	2021-12-16	Buy

Product number	Packaging	Price	Buy
B591900	2.5mg	$605	Buy
CS-6173	25mg	$1200	Buy
CS-6173	1mg	$132	Buy
CS-6173	5mg	$396	Buy
B7833	10mg	$500	Buy

BL-8040 Chemical Properties,Uses,Production

Uses

BKT140 is a CXCR4 inhibitor with potential antineoplastic activity. BKT140 is also a safe and efficient stem cell mobilizer for engraftment.

Definition

ChEBI: Motixafortide is a heterodetic cyclic peptide that has antineoplastic activity. It is a CXC chemokine receptor 4 (CXCR4) antagonist with an IC50 value of 0.8 nM and is currently under clinical investigation for the treatment of hematological malignancies, solid tumors, and stem cell mobilization. It was granted orphan drug designation by the FDA for the treatment of pancreatic cancer in 2019. It has a role as an apoptosis inducer, an antineoplastic agent and a C-X-C chemokine receptor type 4 antagonist.

Biological Activity

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].

Enzyme inhibitor

This orally bioavailable, disulfide cross-linked, polyphemusin-II-derived peptide antagonist (sequence shown above, with Nal = naphthylamine, Cit = citrulline, D-Lys = D-Lysine, and Cys = half-cystine), also known as 4-Fbenzoyl-TN14003 and BL-8040, targets CXC Chemokine Receptor-4 (CXCR4), a G-protein-coupled receptor that is directly involved in tumor progression, tumor angiogenesis, metastasis, and cancer cell survival. Primary Mode of Inhibitory Action: CXCR4 is over-expressed in more than 70% of human cancers and its expression often correlates with disease severity. BKT140 exhibits high affinity (Ki = 0.8nM) and a low rate of dissociation from its receptor. BKT140 prevents the binding of stromal derived factor-1 (SDF-1 or CXCL12) to CXCR4 activation, resulting in decreased tumor cell proliferation and migration. In addition, inhibition of CXCR4 may mobilize hematopoietic cell egress from the bone marrow and into blood. BKT140 significantly and preferentially stimulates multiple myeloma apoptotic cell death, as indicated by induced morphological changes, phosphatidylserine externalization, decreased mitochondrial membrane potential, caspase-3 activation, sub-G1 cell-cycle arrest, as well as DNA double-stranded breaks.

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.

BL-8040 Preparation Products And Raw materials

Raw materials

Preparation Products

BL-8040 Suppliers

Global( 63)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32957	60
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Shanghai Longyu Biotechnology Co., Ltd.	+8619521488211	info@longyupharma.com	China	2529	58
career henan chemical co	+86-0371-86658258 +8613203830695	factory@coreychem.com	China	29811	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32165	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10473	58
LEAP CHEM CO., LTD.	+86-852-30606658	market18@leapchem.com	China	24727	58
Hebei Miaoyin Technology Co.,Ltd	+86-17367732028 +86-17367732028	kathy@hbyinsheng.com	China	3512	58
Nanjing TGpeptide	+86-13347807150 +86-13347807150	support@tgpeptide.com	China	3279	58
Zhejiang Hangyu API Co., Ltd	+8617531972939	anna@api-made.com	China	2943	58

Supplier	Advantage
ATK CHEMICAL COMPANY LIMITED	60
BOC Sciences	58
Shanghai Longyu Biotechnology Co., Ltd.	58
career henan chemical co	58
TargetMol Chemicals Inc.	58
Zhejiang J&C Biological Technology Co.,Limited	58
LEAP CHEM CO., LTD.	58
Hebei Miaoyin Technology Co.,Ltd	58
Nanjing TGpeptide	58
Zhejiang Hangyu API Co., Ltd	58

View Lastest Price from BL-8040 manufacturers

Image	Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
	2020-02-19	BL-8040 664334-36-5	US $7.00 / KG	1KG	99%	100kg	Career Henan Chemical Co

BL-8040
664334-36-5
US $7.00 / KG
99%
Career Henan Chemical Co

BL-8040 Spectrum

BL-8040(664334-36-5)MS

BL-8040 BKT140 BKT140CXCR4 antagonist BKT140 (BL-8040) BKT140 4-fluorobenzoyl MOTIXAFORTIDE;BL-8040;TF14016 4F-Benzoyl-TN14003 BL-8040; TF14016; 4F-BENZOYL-TN14003 TF14016 BKT140, >99% BKT140,BL-8040,TF14016,4F-Benzoyl-TN14003, >99% L-Argininamide, N2-(4-fluorobenzoyl)-L-arginyl-L-arginyl-3-(2-naphthalenyl)-L-alanyl-L-cysteinyl-L-tyrosyl-N5-(aminocarbonyl)-L-ornithyl-L-lysyl-D-lysyl-L-prolyl-L-tyrosyl-L-arginyl-N5-(aminocarbonyl)-L-ornithyl-L-cysteinyl-, cyclic (4→13)-disulfide Motixafortide Motixafortide(TFA) (3S,6S,9S,12R,17R,20S,23S,26S,29R,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)-3,20-bis(4-hydroxybenzyl)-1,4,7,10,18,21,24,27,30-nonaoxo-9,23-bis(3-ureidopropyl)dotriacontahydropyrrolo[2,1-p][1,2,5,8,11,14,17,20,23,26,29]dithianonaazacyclodotriacontine-12-carboxamide Motixafortide(BKT140) {4-Fluorobenzoyl}-Arg-Arg-{2-Naph-Ala}-Cys-Tyr-{Cit}-Lys-{d-Lys}-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2 (Disulfide bridge: Cys4-Cys13) (3S,6S,9S,12R,17R,20S,23S,26S,29R,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)-3,20-bis(4-hydroxybenzyl)-1,4,7,10,18,21,24,27,30-nonaoxo-9,23-bis(3-ureidopropyl)triacontahydro-1H,16H-pyrrolo[2,1-p][1,2]dithia[5,8,11,14,17,20,23,26,29]nonaazacyclodotriacontine-12-carboxamide 664334-36-5 C97H144FN33O19S2