Ibrutinib
| Code | Size | Price |
|---|
| AG-CR1-3620-M005 | 5 mg | £80.00 |
Quantity:
| AG-CR1-3620-M025 | 25 mg | £290.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Storage:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
PCI-32765
Appearance:
White solid.
CAS:
936563-96-1
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS08
Handling Advice:
Keep cool and dry.
Hazards:
H360, H373
InChi:
InChI=1S/C25H24N6O2/c1-2-21(32)30-14-6-7-18(15-30)31-25-22(24(26)27-16-28-25)23(29-31)17-10-12-20(13-11-17)33-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m1/s1
InChiKey:
XYFPWWZEPKGCCK-GOSISDBHSA-N
Long Description:
Chemical. CAS: 936563-96-1. Formula: C25H24N6O2. MW: 440.5. 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 PLCgamma (IC50 = 29nM), a substrate of BTK and phosphorylation of ERK (IC50 = 13nM).
MDL:
MFCD20261150
Molecular Formula:
C25H24N6O2
Molecular Weight:
440.5
Package Type:
Vial
Precautions:
P260, P280, P308, P313, P314
Product 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 PLCgamma (IC50 = 29nM), a substrate of BTK and phosphorylation of ERK (IC50 = 13nM).
Purity:
>98% (HPLC)
Signal word:
Danger
SMILES:
NC1=C2C(=NC=N1)N(N=C2C1=CC=C(OC2=CC=CC=C2)C=C1)C1CCCN(C1)C(=O)C=C
Solubility Chemicals:
Soluble in DMSO. Slightly soluble in ethanol (1mg/ml). Insoluble in water.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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-kappaB: 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)