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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

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

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1610 ng/mL
EXPERIMENT
https://link.springer.com/article/10.1007/s12185-021-03096-9
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4260 ng/mL
EXPERIMENT
https://link.springer.com/article/10.1007/s12185-021-03096-9
250 mg 1 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1800 ng/mL
EXPERIMENT
https://link.springer.com/article/10.1007/s12185-021-03096-9
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7600 ng/mL
EXPERIMENT
https://link.springer.com/article/10.1007/s12185-021-03096-9
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1480 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/31092894/
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4220 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/31092894/
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
22800 ng × h/mL
EXPERIMENT
https://link.springer.com/article/10.1007/s12185-021-03096-9
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
105000 ng × h/mL
EXPERIMENT
https://link.springer.com/article/10.1007/s12185-021-03096-9
250 mg 1 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
26100 ng × h/mL
EXPERIMENT
https://link.springer.com/article/10.1007/s12185-021-03096-9
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
88500 ng × h/mL
EXPERIMENT
https://link.springer.com/article/10.1007/s12185-021-03096-9
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
22100 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/31092894/
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
83400 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/31092894/
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
51 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/31092894/
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
43 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/31092894/
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LGH-447 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
5%
EXPERIMENT
https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.5b01275
single, unknown
 LGH-447 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Substance Class Chemical
Created
by admin
on Tue Apr 01 16:21:31 GMT 2025
Edited
by admin
on Tue Apr 01 16:21:31 GMT 2025
Record UNII
9TG5O4V25H
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LGH447
Preferred Name English
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
PIM447
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 Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
NCI_THESAURUS C129825
Created by admin on Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
Code System Code Type Description
NCI_THESAURUS
C106259
Created by admin on Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
PRIMARY
CAS
1210608-43-7
Created by admin on Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
PRIMARY
MANUFACTURER PRODUCT INFORMATION
LGH-447
Created by admin on Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
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 Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
PRIMARY
FDA UNII
9TG5O4V25H
Created by admin on Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
PRIMARY
ChEMBL
CHEMBL3545194
Created by admin on Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
PRIMARY
EVMPD
SUB194067
Created by admin on Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
PRIMARY
DRUG BANK
DB14943
Created by admin on Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
PRIMARY
PUBCHEM
44814409
Created by admin on Tue Apr 01 16:21:31 GMT 2025 , Edited by admin on Tue Apr 01 16:21:31 GMT 2025
PRIMARY
Related Record Type Details
SERINE/THREONINE-PROTEIN KINASE PIM-1
TARGET -> INHIBITOR
COMPETITIVE INHIBITOR
Ki
SERINE/THREONINE-PROTEIN KINASE PIM-3
TARGET -> INHIBITOR
COMPETITIVE INHIBITOR
Ki
SERINE/THREONINE-PROTEIN KINASE PIM-2
TARGET -> INHIBITOR
COMPETITIVE INHIBITOR
Ki
Related Record Type Details
Structure of LGH-447
ACTIVE MOIETY
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.
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