Drug Information

Drug (ID: DG01660) and It's Reported Resistant Information

Name	JBJ-04-125-02
Synonyms	JBJ-04-125-02; (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-{1-oxo-6-[4-(piperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindol-2-yl}-N-(1,3-thiazol-2-yl)acetamide; 2060610-53-7; (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-[3-oxo-5-(4-piperazin-1-ylphenyl)-1H-isoindol-2-yl]-N-(1,3-thiazol-2-yl)acetamide; SCHEMBL18360815; BCP32863; EX-A4047; HY-135805; CS-0114212 Click to Show/Hide
Structure
Drug Resistance Disease(s)	Disease(s) with Clinically Reported Resistance for This Drug (1 diseases) Solid tumour/cancer [ICD-11: 2A00-2F9Z] [1]
Target	.	NOUNIPROTAC	[1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula	6
IsoSMILES	C1CN(CCN1)C2=CC=C(C=C2)C3=CC4=C(CN(C4=O)[C@H](C5=C(C=CC(=C5)F)O)C(=O)NC6=NC=CS6)C=C3
InChI	InChI=1S/C29H26FN5O3S/c30-21-5-8-25(36)24(16-21)26(27(37)33-29-32-11-14-39-29)35-17-20-2-1-19(15-23(20)28(35)38)18-3-6-22(7-4-18)34-12-9-31-10-13-34/h1-8,11,14-16,26,31,36H,9-10,12-13,17H2,(H,32,33,37)/t26-/m1/s1
InChIKey	VHQVOTINPRYDAO-AREMUKBSSA-N
PubChem CID	124173751

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

Click to Show/Hide the Resistance Disease of This Class

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

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Drug Resistance Data Categorized by Their Corresponding Mechanisms
Aberration of the Drug's Therapeutic Target (ADTT)		Click to Show/Hide
Key Molecule: Epidermal growth factor receptor (EGFR)			[1]
Molecule Alteration	IF-deletion	p.E746_A750delELREA (c.2236_2250del15)	Molecule Info
Resistant Disease	Solid tumour/cancer [ICD-11: 2A00-2F9Z]		Disease Info
Experimental Note	Identified from the Human Clinical Data

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
Aberration of the Drug's Therapeutic Target (ADTT)			Click to Show/Hide
Key Molecule: Epidermal growth factor receptor (EGFR)				[1]
Molecule Alteration	Missense mutation		p.L858R (c.2573T>G)	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	H1975 cells	Lung	Homo sapiens (Human)	CVCL_1511
	Ba/F3 cells	Colon	Homo sapiens (Human)	CVCL_0161
	NIH 3T3 cells	Colon	Homo sapiens (Human)	CVCL_0594
In Vivo Model	Genetically engineered mouse xenograft model			Mus musculus
Experiment for Drug Resistance	MTS assay

References

Ref 1	Single and Dual Targeting of Mutant EGFR with an Allosteric InhibitorCancer Discov. 2019 Jul;9(7):926-943. doi: 10.1158/2159-8290.CD-18-0903. Epub 2019 May 15.