LGH-447

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National Institutes of Health Divider Arrow

NCATS

Investigational

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C24H23F3N4O
Molecular Weight	440.4608
Optical Activity	UNSPECIFIED
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of LGH-447

Structure Search

SMILES

C[C@@H]1C[C@H](N)C[C@@H](C1)C2=C(NC(=O)C3=NC(=C(F)C=C3)C4=C(F)C=CC=C4F)C=NC=C2

InChI

InChIKey=VRQXRVAKPDCRCI-ZNMIVQPWSA-N

InChI=1S/C24H23F3N4O/c1-13-9-14(11-15(28)10-13)16-7-8-29-12-21(16)31-24(32)20-6-5-19(27)23(30-20)22-17(25)3-2-4-18(22)26/h2-8,12-15H,9-11,28H2,1H3,(H,31,32)/t13-,14+,15-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C24H23F3N4O
Molecular Weight	440.4608
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	3 / 3
E/Z Centers	0
Optical Activity	UNSPECIFIED

Approval Year

Targets

Targets

Primary Target	Pharmacology	Condition	Potency
Serine/threonine-protein kinase PIM 1 Target ID: CHEMBL3559682 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27471867 \| https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C106259	Inhibitor 8297

Substance Class	Chemical Created by `admin` on `Sat Dec 16 11:20:59 UTC 2023` Edited by `admin` on `Sat Dec 16 11:20:59 UTC 2023`
Record UNII	9TG5O4V25H
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

LGH-447

Code

English

N-(4-((1R,3S,5S)-3-AMINO-5-METHYLCYCLOHEXYL)-3-PYRIDINYL)-6-(2,6-DIFLUOROPHENYL)-5-FLUORO-2-PYRIDINECARBOXAMIDE

Systematic Name

English

PIM-447

Code

English

PIM KINASE INHIBITOR LGH447

Common Name

English

LGH447

Code

English

PIM 447 [WHO-DD]

Common Name

English

2-PYRIDINECARBOXAMIDE, N-(4-((1R,3S,5S)-3-AMINO-5-METHYLCYCLOHEXYL)-3-PYRIDINYL)-6-(2,6-DIFLUOROPHENYL)-5-FLUORO-

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1404

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

NCI_THESAURUS

C129825

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

Code System Code Type Description

NCI_THESAURUS

C106259

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

PRIMARY

CAS

1210608-43-7

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

PRIMARY

MANUFACTURER PRODUCT INFORMATION

LGH-447

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

PRIMARY

MedKoo CAT NO: 407201, CAS NO: 1210608-43-7Description: PIM447, also known as LGH447, is a potent Moloney murine leukemia (PIM) 1, 2, and 3 kinase inhibitor. Pan proviral insertion site of Moloney murine leukemia (PIM) 1, 2, and 3 kinase inhibitors have recently begun to be tested in humans to assess whether pan PIM kinase inhibition may provide benefit to cancer patients. PIM447 demonstrates in vivo target modulation (pS6RP), single agent antitumor activity in a KG-1 AML mouse xenograft model, and druglike properties suitable for development. PIM447 advanced into humans in 2012 and is currently being assessed in several phase I trials. (last updated: 6/17/2016).

SMS_ID

100000178339

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

PRIMARY

FDA UNII

9TG5O4V25H

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

PRIMARY

ChEMBL

CHEMBL3545194

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

PRIMARY

EVMPD

SUB194067

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

PRIMARY

DRUG BANK

DB14943

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

PRIMARY

PUBCHEM

44814409

Created by admin on Sat Dec 16 11:20:59 UTC 2023 , Edited by admin on Sat Dec 16 11:20:59 UTC 2023

PRIMARY

Related Record Type Details


					5NJ22TAB5Y

SERINE/THREONINE-PROTEIN KINASE PIM-1

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Ki

Amount:


					2CI3BLM1YG

SERINE/THREONINE-PROTEIN KINASE PIM-3

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					1N1D7O62X2

SERINE/THREONINE-PROTEIN KINASE PIM-2

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Interaction Type:

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Amount:

Related Record Type Details


					9TG5O4V25H

LGH-447

ACTIVE MOIETY

Comments:

Drug: PIM 447(Primary); Indications: Acute myeloid leukaemia, Myelodysplastic syndromes; Focus: Adverse reactions; Sponsor: Novartis Pharmaceuticals; Most Recent Events: 05 Apr 2016 Status changed from recruiting to active, no longer recruiting as reported by ClinicalTrials.gov., 25 Jan 2016 Planned end date changed from 1 Jan 2016 to 1 Jul 2016, as reported by ClinicalTrials.gov., 25 Jan 2016 Planned primary completion date changed from 1 Jan 2016 to 1 Jul 2016, as reported by ClinicalTrials.gov.