[CAS NO. 1022899-36-0] PCI-33380
PRODUCTS SPECIFICATIONS [1022899-36-0]
DESCRIPTION [1022899-36-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 855.78 |
| Molecular Formula | C46H52BF2N11O3 |
| SMILES | NC1=C(C(C2=CC=C(OC3=CC=CC=C3)C=C2)=NN4C(CCC5)CN5C(/C=C/CN6CCN(CCNC(CCC7=CC=C(C=C(C(C)=C8)[N]9=C8C)[N-]7[B+3]9([F-])[F-])=O)CC6)=O)C4=NC=N1 |
Summary
PCI-33380 is an irreversible and selective Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
In Vitro
PCI-33380 bound to Btk could be detected by denaturing gel electrophoresis and fluorescent gel scanning
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Immunofluorescence [2]
| Cell Line: | Human B cells. |
| Concentration: | 2 μM. |
| Incubation Time: | 1 h. |
| Result: | Found that 10 nM of PCI-32765 was sufficient to fully occupy the active site of Btk in primary B cells in culture by using the fluorescently tagged derivative PCI-33380. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 58.43 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.1685 mL | 5.8426 mL | 11.6852 mL |
| 5 mM | 0.2337 mL | 1.1685 mL | 2.3370 mL |
| 10 mM | 0.1169 mL | 0.5843 mL | 1.1685 mL |
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1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (2.92 mM); Clear solution
References
- [1] Zuo Y, et al. A novel 2,5-diaminopyrimidine-based affinity probe for Bruton's tyrosine kinase. Sci Rep. 2015 Nov 4;5:16136.
- [2] Honigberg LA, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80.
