Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMZIM37)

Drug Name

CP-868596 Drug Info

Synonyms

Crenolanib; 670220-88-9; Crenolanib (CP-868596); ARO-002; UNII-LQF7I567TQ; LQF7I567TQ; CP-868596 (Crenolanib); CP-868,596; [1-[2-[5-(3-Methyloxetan-3-ylmethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-yl]amine; 1-(2-(5-((3-Methyloxetan-3-yl)methoxy)-1H-benzo-[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine; CP868569; 1-[2-[5-[(3-Methyl-3-oxetanyl)methoxy]-1-benzimidazolyl]-8-quinolyl]-4-piperidinamine; J-502712; 1-[2-[5-[(3-methyloxetan-3-yl)methoxy]benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine

Indication

Disease Entry	ICD 11	Status	REF
Gastrointestinal cancer	2C11	Phase 3	[1] , [2]
Gastrointestinal stromal tumour	2B5B	Phase 3	[3]
Acute myelogenous leukaemia	2A41	Phase 2	[4]
Acute myeloid leukaemia	2A60	Phase 2	[3]
Malignant glioma	2A00.0	Phase 1	[4]

Therapeutic Class

Anticancer Agents

Cross-matching ID

PubChem CID: 10366136
ChEBI ID: CHEBI:145365
CAS Number: CAS 670220-88-9
TTD Drug ID: DMZIM37

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Platelet-derived growth factor receptor alpha (PDGFRA)	TT8FYO9	PGFRA_HUMAN	Modulator	[5] , [6]
Proto-oncogene c-Src (SRC)	TT6PKBN	SRC_HUMAN	Inhibitor	[3]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Platelet-derived growth factor receptor alpha (PDGFRA)	DTT	PDGFRA	6.189	7.636	7.84	7.086
Proto-oncogene c-Src (SRC)	DTT	SRC	2.907	3.35	3.498	4.75

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Gastrointestinal cancer

ICD Disease Classification

2C11

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Platelet-derived growth factor receptor alpha (PDGFRA)	DTT	PDGFRA	3.46E-01	-0.23	-1.55

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7882).
2	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015430)
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5	The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.Invest New Drugs.2015 Apr;33(2):300-9.
6	Crenolanib, a PDGFR inhibitor, suppresses lung cancer cell proliferation and inhibits tumor growth in vivo.Onco Targets Ther.2014 Sep 26;7:1761-8.