Ibrutinib (PCI-32765)

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Chemical Information

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Customer Reviews (3)

Kinase Assay:

^[1]

Cell Assay:

^[2]

Animal Study:

^[1]

References

Name: Ibrutinib (PCI-32765)
Brand: Selleckchem
SKU: S2680

貨號 Cat. No.: S2680
規格 Size: 5~200mg
品牌 Brand: Selleckchem

Ibrutinib (PCI-32765)

Catalog No.S2680

3 Reviews 8 Product Citations

Ibrutinib is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

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Quantity

10mM/1mLIn DMSO	USD 342	In stock	0 1 2 3 4 5 6 7 8 9 10
5mg	USD 214	In stock	0 1 2 3 4 5 6 7 8 9 10
10mg	USD 403	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 1222	In stock	0 1 2 3 4 5 6 7 8 9 10
200mg	USD 3112	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Kinase Assays	In vitro kinase IC50 values are measured using ³³P filtration binding assay after 1 hour incubation of kinase,³³P-ATP, Ibrutinib, and substrate [0.2 mg/mL poly(EY)(4:1]. Assays are performed at Reaction Biology.

Cell lines	Chronic lymphocytic leukemia (CLL) cells
Concentrations	0.01-100 μM
Incubation Time	48 hours
Method	MTT (3’[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide) assays are performed to determine cytotoxicity. Briefly, cells (CLL B cells or healthy volunteer T cells or NK cells) are incubated for 48 hours with different concentrations of Ibrutinib, or vehicle control. MTT reagent is then added, and plates are incubated for an additional 20 hours before washing with protamine sulfate in phosphate-buffered saline. Dimethyl sulfoxide is added, and absorbance is measured by spectrophotometry at 540 nm in a Labsystems plate reader. Cell viability is also measured at various time points with the use of annexin/PI flow cytometry. Data are analyzed with Expo-ADC32 software package. Results are expressed as the percentage of total positive cells over untreated control. Experiments examining caspase-dependent apoptosis includes the addition of 100μM Z-VAD.

Animal Models	MRL-Fas(lpr) lupus model and collagen-induced arthritis model.
Dosages	≤50 mg/kg
Administration	Administered via p.o.
Solubility	1% DMSO/30% polyethylene glycol/1% Tween 80, 12 mg/mL

Download Ibrutinib (PCI-32765) SDF

Molecular Weight (MW)	440.5
Formula	C₂₅H₂₄N₆O₂
CAS No.	936563-96-1

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	88 mg/mL (199 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	1% DMSO/30% polyethylene glycol/1% Tween 80,	12 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	(R)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one

Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.4405	4.405	8.81	13.215

Molarity Calculator Dilution Calculator Molecular Weight Calculator

Description

Ibrutinib is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

0.5 nM ^[1]

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]

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]

Click to enlarge	Rating
	Source	Cell Signal, 2013, 25(1), 106-12.. Ibrutinib (PCI-32765) purchased from Selleck
	Method	Western blotting/Proliferation/death assays
	Cell Lines	MM cell lines
	Concentrations	1/10 μM
	Incubation Time	48 h
	Results	Ibrutinib induces signifi cant cell death (7–46%) in MM cells at 10 μM(Fig. C) as measured by the Cell Titer GLO assay. We also observed a similar effect with ibrutinib in MM cell lines ( Fig. D).