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E7090 (succinate)

CAT: 0804-HY-101466A-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-101466A-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively[1].
CAS Number
1879965-80-6
UNSPSC
12352005
Target
FGFR
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/e7090-succinate.html
Purity
99.17
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(O)CCC(O)=O.O=C(N1C=CC2=C1C=C(OCCOC)C(OC3=CC(NC(C4=CC=C(C5CCN(CCO)CC5)C=C4)=O)=NC=C3)=C2)NC.[3/2]
Molecular Formula
C32H37N5O6.3/2C4H6O4
Molecular Weight
764.82
References & Citations
[1]Saori Watanabe Miyano, et al. E7090: A potent and selective FGFR inhibitor with activity in multiple FGFR-driven cancer models with distinct mechanisms of activation. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.|[2]Saori Watanabe Miyano, et al. E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models. Mol Cancer Ther. 2016 Nov;15 (11) :2630-2639.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Phase 2

Chemical Information

E7090 succinate

Tasurgratinib Succinate is the succinate salt form of tasurgratinib, an orally bioavailable inhibitor of the tyrosine kinase fibroblast growth factor receptor (FGFR) types 1, 2, and 3 (FGFR1/2/3), with potential antineoplastic activity. Upon oral administration, tasurgratinib targets, binds to and inhibits FGFR1/2/3, and is specifically active against certain FGFR2 fusions and rearrangements. This may result in the inhibition of FGFR1/2/3-related signal transduction pathways. This inhibits proliferation in FGFR1/2/3-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases (RTKs), is upregulated in many tumor cell types.

CAS Number1879965-80-6
PubChem CID129275025
IUPAC Namebutanedioic acid;5-[[2-[[4-[1-(2-hydroxyethyl)piperidin-4-yl]benzoyl]amino]-4-pyridinyl]oxy]-6-(2-methoxyethoxy)-N-methylindole-1-carboxamide
Molecular FormulaC36H43N5O10
Molecular Weight705.8
Topological Polar Surface Area202
Hydrogen Bond Donor Count5
Hydrogen Bond Acceptor Count12
Rotatable Bond Count14
Heavy Atom Count51
Formal Charge0
Complexity973
SMILES
CNC(=O)N1C=CC2=CC(=C(C=C21)OCCOC)OC3=CC(=NC=C3)NC(=O)C4=CC=C(C=C4)C5CCN(CC5)CCO.C(CC(=O)O)C(=O)O
InChI
InChI=1S/C32H37N5O6.C4H6O4/c1-33-32(40)37-14-10-25-19-29(28(21-27(25)37)42-18-17-41-2)43-26-7-11-34-30(20-26)35-31(39)24-5-3-22(4-6-24)23-8-12-36(13-9-23)15-16-38;5-3(6)1-2-4(7)8/h3-7,10-11,14,19-21,23,38H,8-9,12-13,15-18H2,1-2H3,(H,33,40)(H,34,35,39);1-2H2,(H,5,6)(H,7,8)
InChIKey
DLFIYSXIMACKCX-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of E7090 succinate
CAS: 1879965-80-6
CID: 129275025
Formula: C36H43N5O10
MW: 705.8
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight705.8
Hydrogen Bond Donor Count5
Hydrogen Bond Acceptor Count12
Rotatable Bond Count14
Exact Mass705.30099259
Monoisotopic Mass705.30099259
Topological Polar Surface Area202 Ų
Heavy Atom Count51
Formal Charge0
Complexity973
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count2
Compound Is CanonicalizedYes

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