CasNo.936563-96-1,Ibrutinib (PCI-32765),(936563-96-1) Suppliers

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Purity: >97%

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Ibrutinib PCI-32765 936563-96-1

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Biological Activity

Description

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 is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I.

Targets

BTK [1] (Cell-free assay)	BLK [1] (Cell-free assay)	Bmx [1] (Cell-free assay)	CSK [1] (Cell-free assay)	FGR [1] (Cell-free assay)	View More
0.5 nM	0.5 nM	0.8 nM	2.3 nM	2.3 nM	View More

In vitro

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. [1] 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. [2] 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. [3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human Rec1 cells	Function assay	2.5 μM	6 h	Inhibition of Lyn phosphorylation in human Rec1 cells at 2.5 uM incubated for 6 hrs by Western blotting method	25222877
human WSU-NHL cells	Cytotoxic assay		72 h	Cytotoxicity against human WSU-NHL cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=1.09 μM	24915291
human SU-DHL6 cells	Cytotoxic assay		72 h	Cytotoxicity against human SU-DHL6 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.58 μM.	24915291

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pEGFR(Tyr1068) / EGFR; pBTK / pPLCγ2 / pAKT / pERK / pJNK;	28061447 23940282
Immunofluorescence	CD11b; COX-2;	30231870
ELISA	hTNFα; IL-10;	26627823 27792904

In vivo

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. [1] In an adoptive transfer TCL1 mouse model of CLL, Ibrutinib (25 mg/kg/day) causes a transient early lymphocytosis, and delays CLL disease progression. [4]