Drug Information

Drug (ID: DG01598) and It's Reported Resistant Information

Name	FIIN-1
Synonyms	FIIN-1; 1256152-35-8; CHEMBL2216830; 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; N-(3-{[3-(2,6-dichloro-3,5-dimethoxyphenyl)-7-{[4-(diethylamino)butyl]amino}-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl}phenyl)prop-2-enamide; FIIN1; SCHEMBL17010767; BDBM50403060; ZINC95564544; NCGC00378818-01; HY-15813; CS-0009282; N-[3-[[3-(2,6-dichloro-3,5-dimethoxyphenyl)-7-[4-(diethylamino)butylamino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]methyl]phenyl]prop-2-enamide Click to Show/Hide
Structure
Target	.	NOUNIPROTAC	[1]
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Formula	15
IsoSMILES	CCN(CC)CCCCNC1=NC=C2CN(C(=O)N(C2=N1)CC3=CC(=CC=C3)NC(=O)C=C)C4=C(C(=CC(=C4Cl)OC)OC)Cl
InChI	InChI=1S/C32H39Cl2N7O4/c1-6-26(42)37-23-13-11-12-21(16-23)19-41-30-22(18-36-31(38-30)35-14-9-10-15-39(7-2)8-3)20-40(32(41)43)29-27(33)24(44-4)17-25(45-5)28(29)34/h6,11-13,16-18H,1,7-10,14-15,19-20H2,2-5H3,(H,37,42)(H,35,36,38)
InChIKey	DNVFTXQYIYFQBW-UHFFFAOYSA-N
PubChem CID	53348188

Type(s) of Resistant Mechanism of This Drug

ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

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Solid tumour/cancer [ICD-11: 2A00-2F9Z]

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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
Aberration of the Drug's Therapeutic Target (ADTT)			Click to Show/Hide
Key Molecule: Fibroblast growth factor receptor 1 (FGFR1)				[1]
Molecule Alteration	Missense mutation		p.V561M (c.1681G>A)	Molecule Info
Sensitive Disease	Solid tumour/cancer [ICD-11: 2A00-2F9Z]			Disease Info
Experimental Note	Revealed Based on the Cell Line Data
In Vitro Model	Ba/F3 cells	Colon	Homo sapiens (Human)	CVCL_0161
Experiment for Drug Resistance	CellTiter-Glo Luminescent Cell Viability Assay
Mechanism Description	The missense mutation p.V561M (c.1681G>A) in gene FGFR1 cause the sensitivity of FIIN-1 by aberration of the drug's therapeutic target

Endometrial cancer [ICD-11: 2C76]

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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
Aberration of the Drug's Therapeutic Target (ADTT)			Click to Show/Hide
Key Molecule: Fibroblast growth factor receptor 2 (FGFR2)				[1]
Molecule Alteration	Missense mutation		p.N549K (c.1647T>G)	Molecule Info
Sensitive Disease	Endometrial adenocarcinoma [ICD-11: 2C76.0]			Disease Info
Experimental Note	Revealed Based on the Cell Line Data
In Vitro Model	Ba/F3 cells	Colon	Homo sapiens (Human)	CVCL_0161
Experiment for Drug Resistance	CellTiter-Glo Luminescent Cell Viability Assay
Mechanism Description	The missense mutation p.N549K (c.1647T>G) in gene FGFR2 cause the sensitivity of FIIN-1 by aberration of the drug's therapeutic target

References

Ref 1	A structure-guided approach to creating covalent FGFR inhibitorsChem Biol. 2010 Mar 26;17(3):285-95. doi: 10.1016/j.chembiol.2010.02.007.