PCI-32765 (Ibrutinib)

Catalog No. A11020

PCI-32765 (Ibrutinib)是Bruton酪氨酸激酶（BTK）的口服生物利用小分子抑制剂，具有潜在的抗肿瘤活性。对Bmx，CSK，FGR，BRK及HCK适度有效，对EGFR，Yes，ErbB2，JAK3等作用效果较弱。

Product Citations

Simonowski A, .et al. Differential use of BTK and PLC in FcεRI- and KIT-mediated mast cell activation: A marginal role of BTK upon KIT activation, Biochim Biophys Acta Mol Cell Res, 2019, Dec 11;1867(4):118622 PMID: 31837347
Carolin N. Zorn, .et al. Stimulus strength determines the BTK-dependence of the SHIP1-deficient phenotype in IgE/antigen-triggered mast cells, Sci Rep, 2018, 8: 15467 PMID: 30341350
Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277

Technical details

Catalog Num	A11020
M. Wt	440.5
Formula	C25H24N6O2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	936563-96-1
Synonyms	Ibrutinib
SMILES	C=CC(=O)N1CCC[C@H](C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N

Biological Activity

Targets

Target	Value
BTK	IC50: 0.5nM
BLK	IC50: 0.5nM
Bmx	IC50: 0.8nM
CSK	IC50: 2.3nM
FGR	IC50: 2.3nM
BRK	IC50: 3.3nM
Hck	IC50: 3.7nM
EGFR	IC50: 5.6nM
YES	IC50: 6.5nM
ErbB2	IC50: 9.4nM
ITK	IC50: 10.7nM
JAK3	IC50: 16.1nM
FRK	IC50: 29.2nM
LCK	IC50: 33.2nM
RET	IC50: 36.5nM
FLT3	IC50: 73nM
TEC	IC50: 78nM
Abl	IC50: 86nM
Fyn	IC50: 96nM
RIPK2	IC50: 152nM
c-Src	IC50: 171nM
Lyn	IC50: 200nM
PDGFRα	IC50: 718nM
Fms	IC50: 5.545μM
FER	IC50: 8.07μM
JAK1	IC50: >10μM
JAK2	IC50: >10μM
NEK2	IC50: >10μM
p38	IC50: >10μM
PI3K	IC50: >10μM
PLK1	IC50: >10μM
RSK1	IC50: >10μM
Syk	IC50: >10μM

Solubility *

In vitro (25°C)	DMSO	81 mg/mL (183.88 mM)
	Water	Insoluble
	Ethanol	41 mg/mL (93.07 mM)
In vivo	5% DMSO+30% PEG 300+5% Tween 80+ddH2O	9 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq 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.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	22.7 mL	113.51 mL	227.01 mL
0.5 mM	4.54 mL	22.7 mL	45.4 mL
1 mM	2.27 mL	11.35 mL	22.7 mL
5 mM	0.45 mL	2.27 mL	4.54 mL

*The above data is based on the productmolecular weight 440.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.