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PCI-32765 (Ibrutinib)

Catalog No.: A11020

Bruton tyrosine kinase inhibitor

PCI-32765 (Ibrutinib)

PCI-32765 (Ibrutinib) Chemical Structure

CAS NO. 936563-96-1

PCI-32765 is an orally bioavailable small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.

Availability: In stock

Package Price Qty
10 mg
$55.00
25 mg
$80.00
100 mg
$100.00
10mM * 1mL in DMSO
$50.00
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Warning Products are for laboratory research use only. Not for human use. We do not sell to patients.
  • 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
  • A

Biological Activity

PCI-32765 is an orally bioavailable small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.
Targets
Target Value
BTKIC50: 0.5nM
BLKIC50: 0.5nM
BmxIC50: 0.8nM
CSKIC50: 2.3nM
FGRIC50: 2.3nM
BRKIC50: 3.3nM
HckIC50: 3.7nM
EGFRIC50: 5.6nM
YESIC50: 6.5nM
ErbB2IC50: 9.4nM
ITKIC50: 10.7nM
JAK3IC50: 16.1nM
FRKIC50: 29.2nM
LCKIC50: 33.2nM
RETIC50: 36.5nM
FLT3IC50: 73nM
TECIC50: 78nM
AblIC50: 86nM
FynIC50: 96nM
RIPK2IC50: 152nM
c-SrcIC50: 171nM
LynIC50: 200nM
PDGFRαIC50: 718nM
FmsIC50: 5.545μM
FERIC50: 8.07μM
JAK1IC50: >10μM
JAK2IC50: >10μM
NEK2IC50: >10μM
p38IC50: >10μM
PI3KIC50: >10μM
PLK1IC50: >10μM
RSK1IC50: >10μM
SykIC50: >10μM
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.
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.

Catalog Num A11020
Actions Inhibitor
CAS No. 936563-96-1
Formula C25H24N6O2
M. Wt 440.5
Purity >98%
Synonyms Ibrutinib
SMILES C=CC(=O)N1CCC[[email protected]](C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N
Storage

Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for 36 months.
In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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