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AdipoGen Life Sciences
Ibrutinib
100
CHF
CHF 100.00
In stock
AG-CR1-3620-M0055 mgCHF 100.00
AG-CR1-3620-M02525 mgCHF 400.00
| Product Details | |
|---|---|
| Synonyms | PCI-32765 |
| Product Type | Chemical |
| Properties | |
| Formula |
C25H24N6O2 |
| MW | 440.5 |
| CAS | 936563-96-1 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White solid. |
| Solubility | Soluble in DMSO. Slightly soluble in ethanol (1mg/ml). Insoluble in water. |
| InChi Key | XYFPWWZEPKGCCK-GOSISDBHSA-N |
| Smiles | NC1=C2C(=NC=N1)N(N=C2C1=CC=C(OC2=CC=CC=C2)C=C1)C1CCCN(C1)C(=O)C=C |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Potent and highly selective Bruton's tyrosine kinase (BTK) inhibitor. Orally bioavailable and irreversible inhibitor of BTK (IC50 = 0.5 nM) with antineoplastic activity.
- Binds to and irreversibly inhibits BTK activity, preventing B cell activation and B cell-mediated signaling. This leads to an inhibition of the growth of malignant B cells that overexpress BTK.
- Shown to inhibit autophosphorylation of BTK (IC50 = 11nM), phosphorylation of PLCγ (IC50 = 29nM), a substrate of BTK and phosphorylation of ERK (IC50 = 13nM).
Product References
- The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy: L.A. Honigberg, et al.; PNAS 107, 13075 (2010)
- BTK inhibitor ibrutinib is cytotoxic to myeloma and potently enhances bortezomib and lenalidomide activities through NF-κB: S.A. Rushworth, et al.; Cell Signal. 25, 106 (2013)
- In vitro, in vivo and ex vivo characterization of ibrutinib: a potent inhibitor of the efflux function of the transporter MRP1: H. Zhang, et al.; Br. J. Pharmacol. 171, 5845 (2014)
- Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase: M.S. Davids & J.R. Brown; Future Oncol. 10, 957 (2014) (Review)