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

General Information of Drug (ID: DM6NX4H)

Drug Name

PKI-402 Drug Info

Synonyms

PKI-402; 1173204-81-3; PKI402; PKI 402; CHEMBL589258; 1-(4-(3-ethyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl)-3-(4-(4-methylpiperazine-1-carbonyl)phenyl)urea; 1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea; J-504117; ZAXFYGBKZSQBIV-UHFFFAOYSA-N; MLS006010978; SCHEMBL3401810; DTXSID30657809; EX-A040; MolPort-022-902-305; BCP02609; C29H34N10O3; s2739; BDBM50308767; ZINC49745945; ABP000110; AKOS022526182; QC-7256; RL00651

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Investigative	[1]

Cross-matching ID

PubChem CID: 44187953
CAS Number: CAS 1173204-81-3
TTD Drug ID: DM6NX4H

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting PI3-kinase gamma (PIK3CG)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 80-6946	DMLOS5R	Follicular lymphoma	2A80	Approved	[2]
IPI-145	DMWA24P	Follicular lymphoma	2A80	Approved	[3]
Buparlisib	DM1WEHC	Breast cancer	2C60-2C65	Phase 3	[4]
Enzastaurin	DM5H0R9	Diffuse large B-cell lymphoma	2A81	Phase 3	[5]
Rigosertib	DMOSTXF	Myelodysplastic syndrome	2A37	Phase 3	[6]
GDC-0032	DMT4QHD	Breast cancer	2C60-2C65	Phase 3	[5]
PQR309	DMMCYZ8	Squamous head and neck cell carcinom	2D60.0	Phase 2	[7]
SAR245409	DMQM7IL	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
XL147	DMML7BE	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
SF1126	DML10K3	Head and neck cancer	2D42	Phase 2	[9]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
PI3-kinase gamma (PIK3CG)	TTHBTOP	PK3CG_HUMAN	Inhibitor	[1]

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References

1	Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: di... J Med Chem. 2010 Jan 28;53(2):798-810.
2	BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110 and p110 activities in tumor cell lines and xenograft models.Mol Cancer Ther.2013 Nov;12(11):2319-30.
3	PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
4	Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
5	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
6	Phase I study of oral rigosertib (ON 01910.Na), a dual inhibitor of the PI3K and Plk1 pathways, in adult patients with advanced solid malignancies. Clin Cancer Res. 2014 Mar 15;20(6):1656-65.
7	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. (Target id: 2155).
8	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. (Target id: 2156).
9	An integrin-targeted, pan-isoform, phosphoinositide-3 kinase inhibitor, SF1126, has activity against multiple myeloma in vivo.Cancer Chemother Pharmacol.2013 Apr;71(4):867-81.