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LY 3009120 - ≥98%(HPLC), high purity , CAS No.1454682-72-4, Inhibitor of A-Raf proto-oncogene; serine/threonine kinase;Inhibitor of B-Raf proto-oncogene; serine/threonine kinase;Inhibitor of Raf-1 proto-oncogene; serine/threonine kinase

Item Number
L288815
Grouped product items
SKUSizeAvailabilityPrice Qty
L288815-5mg
5mg
In stock
$53.90
L288815-10mg
10mg
In stock
$97.90
L288815-25mg
25mg
In stock
$227.90
L288815-50mg
50mg
In stock
$434.90
L288815-100mg
100mg
In stock
$739.90
L288815-250mg
250mg
In stock
$1,665.90

Potent pan-Raf kinase inhibitor

Basic Description

Synonyms1454682-72-4 | C72761 | Pan-raf inhibitor ly3009120 | SCHEMBL15241297 | 1-(3,3-dimethylbutyl)-3-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]urea | B2693-470864 | 1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2
Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsLY3009120 is an orally active, potent and selective pan-RAF type II inhibitor (IC50 = 4.3 nM/CRAF (c-Raf, Raf-1), 5.8 nM/BRAF(V600E), 15 nM/BRAF (b-Raf) by kinase assay with 1 mM ATP; IC50 = 44 nM/ARAF, 31-47 nM/BRAF, 42 nM/CRAF, >1 μM/155 other kinases b
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of A-Raf proto-oncogene; serine/threonine kinase;Inhibitor of B-Raf proto-oncogene; serine/threonine kinase;Inhibitor of Raf-1 proto-oncogene; serine/threonine kinase

Associated Targets(Human)

EPHA2 Tclin Ephrin type-A receptor 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RAF1 Tclin RAF proto-oncogene serine/threonine-protein kinase (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KRAS Tclin GTPase KRas (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BRAF Tclin Serine/threonine-protein kinase B-raf (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ARAF Tchem Serine/threonine-protein kinase A-Raf (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RAF1 Tclin Serine/threonine-protein kinase RAF (4169 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FYN Tclin Tyrosine-protein kinase FYN (5308 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP3K1 Tchem Mitogen-activated protein kinase kinase kinase 1 (590 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
IRAK1 Tchem Interleukin-1 receptor-associated kinase 1 (1749 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP3K20 Tchem Mixed lineage kinase 7 (1473 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EPHA2 Tclin Ephrin type-A receptor 2 (3499 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 (1523 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Homo sapiens (32628 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
A-375 (9258 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HT-29 (80576 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SK-MEL-2 (46422 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
A549 (127892 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCT-116 (91556 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRAF Tclin Serine/threonine-protein kinase B-raf (11587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EPHB4 Tchem Ephrin type-B receptor 4 (3198 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MV4-11 (7307 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EIF2AK4 Tchem Eukaryotic translation initiation factor 2-alpha kinase 4 (471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ARAF Tchem Serine/threonine-protein kinase A-Raf (405 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK13 Tchem MAP kinase p38 (1586 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK8 Tchem c-Jun N-terminal kinase, JNK (688 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase; MEK1/2 (426 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KRAS Tclin GTPase KRas (1864 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rhesus monkey (3147 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDCK (10148 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences
Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Expert: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Expert: [1]


FDA: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Wikipedia: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Other: [1] , [2]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

ClinicalTrials: [1]


PubMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

PubMed: [1] , [2]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DOI: [1]


Other: [1]


PubMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

PubMed: [1]


Names and Identifiers

Pubchem Sid488202289
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488202289
IUPAC Name 1-(3,3-dimethylbutyl)-3-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]urea
INCHI InChI=1S/C23H29FN6O/c1-13-9-18(24)19(29-22(31)26-8-7-23(3,4)5)11-16(13)17-10-15-12-27-21(25-6)30-20(15)28-14(17)2/h9-12H,7-8H2,1-6H3,(H2,26,29,31)(H,25,27,28,30)
InChi Key HHCBMISMPSAZBF-UHFFFAOYSA-N
Canonical SMILES CC1=CC(=C(C=C1C2=C(N=C3C(=C2)C=NC(=N3)NC)C)NC(=O)NCCC(C)(C)C)F
Isomeric SMILES CC1=CC(=C(C=C1C2=C(N=C3C(=C2)C=NC(=N3)NC)C)NC(=O)NCCC(C)(C)C)F
PubChem CID 71721540
Molecular Weight 424.52

Certificates

C of A & Other Certificates

Find and download the COA for your product by matching the lot number on the packaging.

12 results found

Lot NumberCertificate TypeDateItem
D23141756Certificate of AnalysisMar 07, 2023 L288815
D23141764Certificate of AnalysisMar 07, 2023 L288815
D23141769Certificate of AnalysisMar 07, 2023 L288815
D23141772Certificate of AnalysisMar 07, 2023 L288815
D23141776Certificate of AnalysisMar 07, 2023 L288815
D23141777Certificate of AnalysisMar 07, 2023 L288815
D23141784Certificate of AnalysisMar 07, 2023 L288815
D23141785Certificate of AnalysisMar 07, 2023 L288815
D23141798Certificate of AnalysisMar 07, 2023 L288815
D23141981Certificate of AnalysisMar 07, 2023 L288815
D23142188Certificate of AnalysisMar 07, 2023 L288815
D23142236Certificate of AnalysisMar 07, 2023 L288815

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Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 4.25, Max Conc. mM: 10 with gentle warming

Related Documents

References

1. Peng SB, Henry JR, Kaufman MD, Lu WP, Smith BD, Vogeti S, Rutkoski TJ, Wise S, Chun L, Zhang Y et al..  (2015)  Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers..  Cancer Cell,  28  (3): (384-98).  [PMID:26343583] [10.1021/op500134e]

Solution Calculators