BIBU 1361 dihydrochloride

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Cat.No. 2417 - BIBU 1361 dihydrochloride | C22H27ClFN7.2HCl | CAS No. 793726-84-8
Description: Selective inhibitor of EGFR-kinase
Chemical Name: N-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]-pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride
Purity: ≥97% (HPLC)
Datasheet
Citations
Literature

Biological Activity

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.

Compound Libraries

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Technical Data

M. Wt 516.87
Formula C22H27ClFN7.2HCl
Storage Desiccate at +4°C
Purity ≥97% (HPLC)
CAS Number 793726-84-8
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 12.92 25
ethanol 2.58 5
water 51.69 100

Preparing Stock Solutions

The following data is based on the product molecular weight 516.87. 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.

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Solca et al (2004) Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J.Pharmacol.Exp.Ther. 311 502 PMID: 15199094


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View all EGFR Inhibitors

Keywords: BIBU 1361 dihydrochloride, supplier, Selective, inhibitors, inhibits, EGFR-kinases, Epidermal, Growth, Factors, Receptors, ErbB, Her, Receptor, Tyrosine, Kinases, RTKs, BIBU1361, dihydrochloride, EGFR, EGFR, Tocris Bioscience

Citations for BIBU 1361 dihydrochloride

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