Drug Information

Drug (ID: DG02037) and It's Reported Resistant Information

Name	TVB-3166
Synonyms	FASN inhibitor 1\|TVB-3166\|FASN-IN-3\|1533438-83-3\|2097262-60-5\|4-(1-(5-(3,4-Dimethyl-1H-pyrazol-5-yl)-2,4-dimethylbenzoyl)azetidin-3-yl)benzonitrile\|4-[1-[5-(4,5-dimethyl-1H-pyrazol-3-yl)-2,4-dimethylbenzoyl]-3-azetidinyl]-benzonitrile\|4-[1-[5-(4,5-dimethyl-1H-pyrazol-3-yl)-2,4-dimethylbenzoyl]azetidin-3-yl]benzonitrile\|4-(1-(5-(4,5-Dimethyl-1H-pyrazol-3-yl)-2,4-dimethylbenzoyl)azetidin-3-yl)benzonitrile\|4-{1-[5-(4,5-Dimethyl-2H-pyrazol-3-yl)-2,4-dimethyl-benzoyl]-azetidin-3-yl}-benzonitrile\|4-{1-[5-(4,5-dimethyl-1H-pyrazol-3-yl)-2,4-dimethylbenzoyl]azetidin-3-yl}benzonitrile\|starbld0000754\|CHEMBL3923704\|SCHEMBL15559827\|BDBM244633\|GLXC-10018\|EX-A4622\|XID26260\|HY-U00436\|TVB-3166?\|AKOS040733375\|AKOS040742789\|BS-45242\|DA-63382\|DB-153395\|CS-0035379\|TVB-3166, >=98% (HPLC)\|E74928\|US9428502, 242\|4-[1-[5-(4,5-Dimethyl-1H-pyrazol-3-yl)-2,4-dimethylbenzoyl]-3-azetidinyl]benzonitrile Click to Show/Hide
Indication	In total 1 Indication(s) . . .
Structure
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Formula	C24H24N4O
IsoSMILES	CC1=CC(=C(C=C1C2=NNC(=C2C)C)C(=O)N3CC(C3)C4=CC=C(C=C4)C#N)C
InChI	InChI=1S/C24H24N4O/c1-14-9-15(2)22(10-21(14)23-16(3)17(4)26-27-23)24(29)28-12-20(13-28)19-7-5-18(11-25)6-8-19/h5-10,20H,12-13H2,1-4H3,(H,26,27)
InChIKey	ICDQFUFDAFKCAX-UHFFFAOYSA-N
PubChem CID	72947731

Type(s) of Resistant Mechanism of This Drug

MRAP: Metabolic Reprogramming via Altered Pathways

Drug Resistance Data Categorized by Their Corresponding Diseases

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

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Bladder cancer [ICD-11: 2C94]

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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
Metabolic Reprogramming via Altered Pathways (MRAP)			Click to Show/Hide
Key Molecule: Fatty acid synthase (FASN)				[1]
Metabolic Type	Lipid metabolism
Sensitive Disease	Bladder cancer [ICD-11: 2C94.0]			Disease Info
Molecule Alteration	Expression		Down-regulation	Molecule Info
Experimental Note	Revealed Based on the Cell Line Data
In Vitro Model	T24 cells	Bladder	Homo sapiens (Human)	CVCL_0554
	UMUC3-R cells	Bladder	Homo sapiens (Human)	CVCL_1783
Experiment for Molecule Alteration	RNA sequencing
Experiment for Drug Resistance	CCK8 assay
Mechanism Description	Further in vitro and in vivo studies were implemented using Fatty Acid Synthase (FASN), a representative gene, which promotes gemcitabine resistance, and its inhibitor (TVB-3166) that can reverse this resistance effect.

References

Ref 1	Metabolic reprogramming based on RNA sequencing of gemcitabine-resistant cells reveals the FASN gene as a therapeutic for bladder cancer. J Transl Med. 2024 Jan 13;22(1):55.