Ibrutinib (PCI-32765) | BTK inhibitor | Probechem Biochemicals

Chemical Structure : Ibrutinib

CAS No.: 936563-96-1

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Ibrutinib (PCI-32765, PCI32765, PCI 32765)

货号: PC-42772Not For Human Use, Lab Use Only.

Ibrutinib (PCI-32765, PCI32765) is a potent and highly selective, covalent BTK inhibitor with IC50 of 0.5 nM.

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10 mg	￥780	In stock
25 mg	￥1280	In stock
50 mg	￥1980	In stock
100 mg	￥2980	In stock
250 mg		Get quote

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生物&药学活性

Ibrutinib (PCI-32765, PCI32765) is a potent and highly selective, covalent BTK inhibitor with IC50 of 0.5 nM.

Ibrutinib modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

Ibrutinib (PCI-32765) selectively inhibits B-cell signaling and activation. It inhibits autophosphorylation of Btk (IC50=11 nM), phosphorylation of Btk's physiological substrate PLCγ (IC50=29 nM).

Ibrutinib (PCI-32765) inhibits BCR-activated primary B cell proliferation (IC50=8 nM).

Following FcγR stimulation, Ibrutinib (PCI-32765) inhibits TNFα, IL-1β and IL-6 production in primary monocytes (IC50=2.6, 0.5, 3.9 nM, respectively).

Ibrutinib (PCI-32765) (3.125-50 mg/kg, p.o.) reduces the level of circulating autoantibodies and completely suppresses disease in mice with collagen-induced arthritis.

Ibrutinib (PCI-32765) (0.1 μM) inhibits activation-induced proliferation of CLL cells, induces selective cytotoxicity in B cells compared with T cells, but alters activation induced T-cell cytokine production.

物理化学性质&存储条件

分子量	440.4971
分子式	C25H24N6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	DMSO: ≥ 52 mg/mL
Chemical Name/SMILES	2-Propen-1-one, 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-

参考文献

1. Honigberg LA, et al. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80.

2. Herman SE, et al. Blood. 2014 May 22;123(21):3286-95.

3. Kohrt HE, et al. Blood. 2014 Mar 20;123(12):1957-60.

Ibrutinib (PCI-32765, PCI32765, PCI 32765)

生物&药学活性

物理化学性质&存储条件

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Ibrutinib (PCI-32765, PCI32765, PCI 32765)

生物&药学活性

物理化学性质&存储条件

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