99% High Purity PCI-32765 CAS 936563-96-1 Ibrutinib CAS NO.936563-96-1

Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.
 

Ibrutinib shows the potent and irreversible inhibitory effect and selectivity for Btk enzymatic activity. In BCR pathway-activated DOHH2 cell line, Ibrutinib inhibits autophosphorylation of Btk, phosphorylation of Btk's physiological substrate PLCγ, and phosphorylation of further downstream kinase, ERK with IC50 of 11 nM, 29 nM and 13 nM, respectively.  Ibrutinib exhibits a significant dose-dependent and time-dependent induction of cytotoxicity in chronic lymphocytic leukemia (CLL) cells. In addition, Ibrutinib induces cell death depending on caspase pathway activation and antagonizes the ability of CLL cells to proliferate after TLR signaling. A recent study shows that Ibrutinib inhibits BCR-activated primary B cell proliferation with IC50 of 8 nM and results in inhibition of TNFα, IL-1β and IL-6 production in primary monocytes with IC50 of 2.6 nM, 0.5 nM and 3.9 nM, respectively.
 

In a collagen-induced arthritis model, Ibrutinib significantly reduces clinical arthritis scores reflecting paw swelling and joint inflammation by inhibiting B-cell activation. In a MRL-Fas(lpr) lupus model, Ibrutinib reduces renal disease and autoantibody production.In an adoptive transfer TCL1 mouse model of CLL, Ibrutinib (25 mg/kg/day) causes a transient early lymphocytosis, and delays CLL disease progression. 

Ibrutinib is a highly selective Bruton's tyrosine kinase (Btk) irreversible inhibitor.PCI-32765 (Ibrutinib) is a selective and irreversible pyrrolopyrimidine-based inhibitor of BTK with IC50 of 0.5 nM. [1] PCI-32765 binds irreversibly to Cys-481 in BTK and thus is only active with other kinases with such a modifiable cysteine residue. In DOHH2 cells, in which the BCR pathway can be activated by anti-IgG, PCI-32765 inhibits autophosphorylation of BTK (IC50, 11 nM), BTK's physiological substrate, PLCg (IC50, 29 nm), and downstream ERK (IC50, 13 nm). 
PCI-32765 (Ibrutinib) may be an important new targeted treatment approach for CLL pts. In ex vivo assays with whole bold, PCI-32765 (Ibrutinib) prevents the activation of human BCR with an IC50 of about 0.2 μM, while not influencing the activation of T cell. Treatment of CD40 or BCR activated CLL cells with PCI-32765 (Ibrutinib) results in inhibition of BTK tyrosine phosphorylation and also effectively abrogates downstream survival pathways activated by this kinase including ERK1/2, PI3K, and NF-κB. In addition, PCI-32765 (Ibrutinib) prevents activation-induced proliferation of CLL cells in vitro, and effectively inhibits survival signals provided externally to CLL cells from the microenvironment including soluble factors (CD40L, BAFF, IL-6, IL-4, and TNF-α), fibronectin engagement, and stromal cell contact. PCI-32765 is originally developed by Pharmacyclics. And participants is been invited for the phase I clinical trials.

1. We has 11 years' exporting experience in pharmaceutical ingredient products.

Our professional and thoughtful after-sales service eliminates your worries.

2.We can provide you with ten thousands of products of different levels.

3. We offer convenient one-station purchasing service.

(1)Any inquiries will be replied within 12 hours.
(2)Dedication to quality, supply & service.
(3)Strictly on selecting raw materials.
(4)Reasonable & competitive price, fast lead time.

Wuhan Kanal Technology Co., Ltd. founded in 2010,it is a large manufacturer of fine Pharmaceutical& Chemical & Cosmetic materials that integrates R&D, production and sales together.  Our Kanal company is established under the support of the Wuhan city government, so Kanal has large advantages in enterprise credit, finance security, product quality control, and cargo export.Kanal locates in the national new materials industry park of Wuhan city and is awarded the title of high-tech corporation.

Wuhan Kanal has its own R&D and development laboratory. We Kanal set up a R&D team with rich experience and strong technical strength, most of the practitioners have more than ten years' experience and technology in organic synthesis development. It owns almost 15 acre and more than 280 workers.

An ISO 9001 & GMP qualified company, we are mainly specialized in producing high quality but low price Pharmaceutical intermediates, APIs and other fine chemicals & cosmetics products which related to human and animals medicines as well as additives in gas &oil field, almost half of the goods are for exporting. What's more, we provide the OEM (customize) manufactures, if you can't find materials from the world, then tell us, we will research and produce in our high-tech equipmented laboratory. We are dedicated to satisfying our customers with our products and services.


1. We has 11 years' exporting experience in active pharmaceutical ingredient products.
Our professional and thoughtful after-sales service eliminates your worries.

2.We can provide you with ten thousands of products of different levels.

3. We offer convenient one-station purchasing service.

(1)Any inquiries will be replied within 12 hours.
(2)Dedication to quality, supply & service.
(3)Strictly on selecting raw materials.
(4)Reasonable & competitive price, fast lead time.

Our company is based on the optical valley biological city,making full use of the park policy advantages, focusing on the research and development of biological medicine.

The pharmaceutical intermediates are mainly applied to anti-cancer, anti-depression, cardiovascular, diabetes and other new medicine. The chemical intermediates mainly refer to heterocyclics and OLED intermediates.Our factory produce new fine chemical materials which are mainly used in water treatment, bactericidal and anti-corrosion, dyes, electronic materials and other industry fields.
Wuhan Kanal has export & import license, and hazard chemical sales license. The products are exported to America, Brazil, South Korea, Japan, Taiwan, Malaysia, Thailand, Indonesia, Europe union and other countries or regions. 
Under rich experiences and excellent international reputation, the company becomes a quite influential enterprise in China's API field. Wuhan Kanal sincerely look forward to establishing long good cooperation with our customers from all over the world.