Ibrutinib (PCI-32765)

Ibrutinib (PCI-32765)は一種の有効で、高度選択性的なBTK( Brutons tyrosine kinase)阻害剤で、無細胞試験でIC50値が0.5 nMですが、Bmx、CSK、FGR、BRK及びHCKに適度に作用して、EGFR、Yes、ErbB2とJAK3等に作用する効果が弱いです。

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Ibrutinib (PCI-32765) 化学構造
分子量: 440.5






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製品説明 Ibrutinib (PCI-32765)は一種の有効で、高度選択性的なBTK( Brutons tyrosine kinase)阻害剤で、無細胞試験でIC50値が0.5 nMですが、Bmx、CSK、FGR、BRK及びHCKに適度に作用して、EGFR、Yes、ErbB2とJAK3等に作用する効果が弱いです。



0.5 nM [1]

In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Sf9 cells MkHlSpVv[3Srb36gZZN{[Xl? M2q5RlEhcA>? NX7zZ4J6UW6qaXLpeIlwdiCxZjDoeY1idiCodXzsMYxmdme2aDDCWGsh\XiycnXzd4VlKGmwIGPmPUBk\WyuczD1d4lv\yCIQV2tV5JkfGmmZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBi\nSncjC2NEBucW6|IHL5JHRTNU[URWSgRZN{[XoxvJygTWM2OD1yLkWgcm0v NU\vV2J5OjF7NUi1OFc>
human Pfeiffer cells MlPwSpVv[3Srb36gZZN{[Xl? MWO3NkBp MYTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQ[oVq\m[ncjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{IH7NMi=> NXjkR4x4OjR7MUWyPVE>
human Ramos cells MUDGeY5kfGmxbjDhd5NigQ>? M1fwWVEhcA>? MmXnTY5pcWKrdHnvckBw\iCEdHugbY4hcHWvYX6gVoFud3NiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBRVENvZ3HtcYEzKHCqb4PwbI9zgWyjdHnvckBifCCWeYKxNlE4KGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVE1KG6PLh?= M2P2cFI1QTF3Mkmx
Sf9 cells MX3GeY5kfGmxbjDhd5NigQ>? NHeyeI4yKGh? M3HqTWlvcGmkaYTpc44hd2ZiTGnOMWEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDh[pRmeiB4MDDtbY5{KGK7IGTSMWZTTVRiQYPzZZktKEmFNUC9NE4zKM7:TT6= MVSyNVk2QDV2Nx?=
human DOHH2 cells MWnDfZRwfG:6aXRCpIF{e2G7 NIfi[5I4OiCq NXrkcmRiS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTE:KSEKgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60NUDPxE1w Mn\uNlQ6OTV{OUG=
human SU-DHL6 cells NVfzTnpmS3m2b4TvfIlkyqCjc4PhfS=> MkDPO|IhcA>? NV7rd3Y2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW1VvRFjMOkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU5KM7:TT6= MV2yOFkyPTJ7MR?=
human WSU-NHL cells NHnafmREgXSxdH;4bYPDqGG|c3H5 MV:3NkBp M3jUPWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHdUXS2QSFygZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wPUDPxE1? NIn0cm0zPDlzNUK5NS=>
human Rec1 cells MV;GeY5kfGmxbjDhd5NigQ>? M1fBPVIvPSEQvF2= MWG2JIg> MWLJcohq[mm2aX;uJI9nKEy7bjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iUnXjNUBk\WyuczDheEAzNjVidV2gbY5kfWKjdHXkJIZweiB4IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKG2ndHjv[C=> MX:yOVIzOjh5Nx?=

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 Ibrutinib is currently in Phase II clinical trials in patients with Chronic Lymphocytic Leukemia (CLL) or Small Lymphocytic Lymphoma (SLL). Combination of Ibrutinib and Rituximab is currently in Phase II clinical trials in patients with High-Risk Chronic

プロトコル (参考用のみ)



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.



細胞株 Chronic lymphocytic leukemia (CLL) cells
濃度 0.01-100 μM
反応時間 48 hours

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.



動物モデル MRL-Fas(lpr) lupus model and collagen-induced arthritis model.
製剤 Ibrutinib is dissolved in DMSO.
投薬量 ≤50 mg/kg
投与方法 Administered via p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download Ibrutinib (PCI-32765) SDF
分子量 440.5


CAS No. 936563-96-1
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 88 mg/mL (199.77 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+Castor oil 10mg/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.
化学名 (R)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID