L-779450 - 96% (HPLC), high purity , CAS No.303727-31-3, Inhibitor of B-Raf proto-oncogene; serine/threonine kinase;Inhibitor of Raf-1 proto-oncogene; serine/threonine kinase

In stock
Item Number
L169419
Grouped product items
SKUSizeAvailabilityPrice Qty
L169419-5mg
5mg
3
$83.90
L169419-25mg
25mg
2
$378.90
L169419-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$711.90

Potent Raf kinase inhibitor

Basic Description

Synonyms2-chloro-5-(2-phenyl-5-pyridin-4-yl-1H-imidazol-4-yl)phenol | HMS2847J19 | BDBM26041 | SCHEMBL7643418 | AC-35772 | HY-12787 | s6680 | BIPERIDEN LACTATE [WHO-DD] | compound 1 [PMID:18346893] | Raf Kinase Inhibitor IV | 2-chloro-5-[2-phenyl-5-(pyridin-4-yl)
Specifications & PurityMoligand™, ≥96%(HPLC)
Biochemical and Physiological MechanismsPotent Raf kinase inhibitor (IC 50 = 10 nM). Inhibits Raf-1 activation. Competes for ATP at the protein kinase catalytic site. Supresses DNA synthesis and induces apoptosis. Additionally inhibits p38.
Storage TempStore at 2-8°C
Shipped InWet ice
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of B-Raf proto-oncogene; serine/threonine kinase;Inhibitor of Raf-1 proto-oncogene; serine/threonine kinase
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

Associated Targets(Human)

RAF1 Tclin RAF proto-oncogene serine/threonine-protein kinase (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BRAF Tclin Serine/threonine-protein kinase B-raf (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAPK11 Tchem MAP kinase p38 beta (2785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RAF1 Tclin Serine/threonine-protein kinase RAF (4169 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK13 Tchem MAP kinase p38 delta (2605 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPKAPK2 Tchem MAP kinase-activated protein kinase 2 (4814 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPKAPK5 Tchem MAP kinase-activated protein kinase 5 (2831 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ROCK2 Tclin Rho-associated protein kinase 2 (6206 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 (4127 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PRKCA Tchem Protein kinase C alpha (5923 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK8 Tchem c-Jun N-terminal kinase 1 (5038 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AKT1 Tchem Serine/threonine-protein kinase AKT (9192 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SGK1 Tchem Serine/threonine-protein kinase Sgk1 (2343 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHEK1 Tchem Serine/threonine-protein kinase Chk1 (6846 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK12 Tchem MAP kinase p38 gamma (2776 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
PRKACB Tchem cAMP-dependent protein kinase (PKA) (929 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK2B Tbio Casein kinase II (1406 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PRKAA2 Tchem AMP-activated protein kinase, AMPK (12273 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PHKG2 Tchem Phosphorylase kinase (51 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RPS6KB2 Tchem Ribosomal protein S6 kinase (P70S6K) (90 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hippocampus (57 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

Pubchem Sid504765143
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/504765143
IUPAC Name 2-chloro-5-(2-phenyl-5-pyridin-4-yl-1H-imidazol-4-yl)phenol
INCHI InChI=1S/C20H14ClN3O/c21-16-7-6-15(12-17(16)25)19-18(13-8-10-22-11-9-13)23-20(24-19)14-4-2-1-3-5-14/h1-12,25H,(H,23,24)
InChi Key WXJLXRNWMLWVFB-UHFFFAOYSA-N
Canonical SMILES C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC(=C(C=C4)Cl)O
Isomeric SMILES C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC(=C(C=C4)Cl)O
PubChem CID 9950176
Molecular Weight 347.8

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

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

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Lot NumberCertificate TypeDateItem
D2027111Certificate of AnalysisFeb 22, 2024 L169419

Chemical and Physical Properties

Molecular Weight347.800 g/mol
XLogP34.200
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count3
Rotatable Bond Count3
Exact Mass347.083 Da
Monoisotopic Mass347.083 Da
Topological Polar Surface Area61.800 Ų
Heavy Atom Count25
Formal Charge0
Complexity425.000
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
The total count of all stereochemical bonds0
Covalently-Bonded Unit Count1

Specifications

References

1. Zhu T, Jiao Y, Chen YD, Wang X, Li HF, Zhang LY, Lu T.  (2008)  Pharmacophore identification of Raf-1 kinase inhibitors..  Bioorg Med Chem Lett,  18  (7): (2346-50).  [PMID:18346893] [10.1021/op500134e]
2. Takle AK, Brown MJ, Davies S, Dean DK, Francis G, Gaiba A, Hird AW, King FD, Lovell PJ, Naylor A et al..  (2006)  The identification of potent and selective imidazole-based inhibitors of B-Raf kinase..  Bioorg Med Chem Lett,  16  (2): (378-81).  [PMID:16260133] [10.1021/op500134e]
3. Fritsche-Guenther R et al..  (2016)  Effects of RAF inhibitors on PI3K/AKT signalling depend on mutational status of the RAS/RAF signalling axis..  Oncotarget,  (7): (7960-9).  [PMID:26799289]
4. Keshmiri Neghab H et al..  (2019)  Modulation of cardiac optogenetics by vitamin A..  Biofactors,  45  (6): (983-990).  [PMID:31509323]
5. Keshmiri Neghab H et al..  (2021)  Optogenetic Stimulation of Primary Cardiomyocytes Expressing ChR2..  J Lasers Med Sci,  12  (e32).  [PMID:34733755]

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