FIIN 1 hydrochloride

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Cat.No. 4002 - FIIN 1 hydrochloride | C32H39Cl2N7O4 | CAS No. 1256152-35-8
Description: Potent, irreversible FGFR inhibitor
Chemical Name: N-(3-((3-(2,6-dichloro-3,5-dimethoxyphenyl)-7-(4-(diethylamino)butylamino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)methyl)phenyl)acrylamide
Purity: ≥96% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent, irreversible FGFR inhibitor (Kd values are 2.8, 5.4, 6.9 and 120 nM for FGFR1, FGFR3, FGFR2 and FGFR4 respectively); acts at the ATP binding site. Also irreversibly inhibits Flt-1, Flt-4 and VEGFR-2 (Kd values are 32, 120 and 210 nM respectively); displays limited activity (Kd >500 nM) at other kinases. Exhibits antiproliferative activity in FGFR3- and FGFR1-transformed Ba/F3 cells (EC50 values are 10 and 14 nM respectively). Derived from the reversible FGFR inhibitor, PD 173074 (Cat. No. 3044).

Technical Data

M. Wt 693.06
Formula C32H39Cl2N7O4
Storage Store at -20°C
Purity ≥96% (HPLC)
CAS Number 1256152-35-8
PubChem ID 90488902
InChI Key IQLGDXNKTDKSMY-UHFFFAOYSA-N
Smiles CCN(CC)CCCCNC1=NC=C2C(N(CC3=CC=CC(NC(C=C)=O)=C3)C(N(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C2)=O)=N1.Cl

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 69.31 100
ethanol 69.31 100

Preparing Stock Solutions

The following data is based on the product molecular weight 693.06. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.44 mL 7.21 mL 14.43 mL
5 mM 0.29 mL 1.44 mL 2.89 mL
10 mM 0.14 mL 0.72 mL 1.44 mL
50 mM 0.03 mL 0.14 mL 0.29 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Zhou (2010) A structure-guided approach to creating covalent FGFR inhibitors. Chem.Biol. 17 285 PMID: 20338520


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View all FGFR Inhibitors

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Citations for FIIN 1 hydrochloride

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Literature in this Area

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Cancer Research Product Guide

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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Stem Cells

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

Pathways for FIIN 1 hydrochloride

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