TASURGRATINIB

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NCATS

Details

Stereochemistry	ACHIRAL
Molecular Formula	C32H37N5O6
Molecular Weight	587.6661
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of TASURGRATINIB

Structure Search

SMILES

CNC(=O)N1C=CC2=CC(OC3=CC=NC(NC(=O)C4=CC=C(C=C4)C5CCN(CCO)CC5)=C3)=C(OCCOC)C=C12

InChI

InChIKey=IBHOLSBDZMIPPT-UHFFFAOYSA-N

InChI=1S/C32H37N5O6/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/h3-7,10-11,14,19-21,23,38H,8-9,12-13,15-18H2,1-2H3,(H,33,40)(H,34,35,39)

HIDE SMILES / InChI

Molecular Formula	C32H37N5O6
Molecular Weight	587.6661
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Approval Year

Substance Class	Chemical Created by `admin` on `Sat Dec 16 18:16:33 UTC 2023` Edited by `admin` on `Sat Dec 16 18:16:33 UTC 2023`
Record UNII	TN7CUD1NGA
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TASURGRATINIB

Official Name

English

FGF/FGFR PATHWAY INHIBITOR E7090

Common Name

English

E7090

Code

English

1H-INDOLE-1-CARBOXAMIDE, 5-((2-((4-(1-(2-HYDROXYETHYL)-4-PIPERIDINYL)BENZOYL)AMINO)-4-PYRIDINYL)OXY)-6-(2-METHOXYETHOXY)-N-METHYL-

Systematic Name

English

1-(2-HYDROXYETHYL)-7-(2-METHOXYETHOXY)-N-METHYL-3- OXO-7H-6-OXA-4-AZA-7(5)-INDOLA-5(2,4)-PYRIDINA-1(4)-PIPERIDINA-2(1,4)-BENZENAHEPTAPHANE-7-CARBOXAMIDE

Systematic Name

English

5-((2-(((4-(1-(2-HYDROXYETHYL)PIPERIDIN-4-YL)PHENYL)CARBONYL)AMINO)PYRIDIN-4-YL)OXY)-6-(2-METHOXYETHOXY)-N-METHYL-1H-INDOLE-1-CARBOXAMIDE

Common Name

English

E 7090 [WHO-DD]

Common Name

English

tasurgratinib [INN]

Common Name

English

E-7090

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C1967

Created by admin on Sat Dec 16 18:16:33 UTC 2023 , Edited by admin on Sat Dec 16 18:16:33 UTC 2023

NCI_THESAURUS

C129825

Created by admin on Sat Dec 16 18:16:33 UTC 2023 , Edited by admin on Sat Dec 16 18:16:33 UTC 2023

Code System Code Type Description

CAS

1622204-21-0

Created by admin on Sat Dec 16 18:16:33 UTC 2023 , Edited by admin on Sat Dec 16 18:16:33 UTC 2023

PRIMARY

SMS_ID

300000022204

Created by admin on Sat Dec 16 18:16:33 UTC 2023 , Edited by admin on Sat Dec 16 18:16:33 UTC 2023

PRIMARY

NCI_THESAURUS

C118672

Created by admin on Sat Dec 16 18:16:33 UTC 2023 , Edited by admin on Sat Dec 16 18:16:33 UTC 2023

PRIMARY

FDA UNII

TN7CUD1NGA

Created by admin on Sat Dec 16 18:16:33 UTC 2023 , Edited by admin on Sat Dec 16 18:16:33 UTC 2023

PRIMARY

PUBCHEM

78323434

Created by admin on Sat Dec 16 18:16:33 UTC 2023 , Edited by admin on Sat Dec 16 18:16:33 UTC 2023

PRIMARY

INN

11580

Created by admin on Sat Dec 16 18:16:33 UTC 2023 , Edited by admin on Sat Dec 16 18:16:33 UTC 2023

PRIMARY

INN

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ACTIVE MOIETY

Comments:

E7090 is an orally available, selective and potent inhibitor of FGFR1, 2 and 3 tyrosine kinase activities. E7090 displayed inhibition of FGFR1, 2, and 3 kinase activities with the IC50 values of approximately 1 nmol/L. E7090 also inhibited the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC50 value of 3 nmol/L. This activity was about 60-fold stronger than that against VEGF-stimulated HUVEC growth. Kinase profiling assay consisting of 93 kinases including non-receptor and serine/threonine kinases, also demonstrated that E7090 inhibited limited kinases including FGFR-1, -2 and -3. In addition, E7090 inhibited proliferation of human cancer cell lines harboring various types of FGFRs gene abnormalities such as amplification, mutation, or translocation in vitro, which are confirmed by the inhibition of FGFR signaling.

Amount: