BIBU 1361 dihydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 2417
Selective inhibitor of EGFR-kinase
Discontinued Product
2417 has been discontinued.
View all EGF Receptor Inhibitors products.
Key Product Details
Description
Selective inhibitor of EGFR-kinase
Product Description
BIBU 1361 dihydrochloride is a potent inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM). Displays ~ 100-fold lower potency against ErbB2 (IC50 = 290 nM) and is selective over a range of other related tyrosine kinases (IC50 > 10 μM). Blocks downstream EGFR signaling events such as MAPKK/MAPK activation. Oral administration inhibits growth of established human xenografts in athymic mice.Product Specifications
Molecular Weight
516.87
Formula
C22H27ClFN7.2HCl
Storage
Desiccate at +4°C
Purity
≥97% (HPLC)
Chemical Name
N-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]-pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride
CAS Number
1643609-75-9
PubChem ID
46861539
InChI Key
ZNNWCQCQUKAMGL-UHFFFAOYSA-N
SMILES
Cl.Cl.CCN(CC)CC1CCN(CC1)C1=NC=C2N=CN=C(NC3=CC(Cl)=C(F)C=C3)C2=N1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 51.69 | 100 | |
| DMSO | 12.92 | 25 |
Preparing Stock Solutions
for BIBU 1361 dihydrochloride
The following data is based on the product molecular weight 516.87
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.93 mL | 9.67 mL | 19.35 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.87 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.93 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Solca Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J.Pharmacol.Exp.Ther. 2004 PMID: 15199094
Product Specific Notices for BIBU 1361 dihydrochloride
For research use only
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