R8907
RPI-1
≥98% (HPLC)
Synonym(e):
1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-H-indol-2-one
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Empirische Formel (Hill-System):
C17H15NO4
CAS-Nummer:
Molekulargewicht:
297.31
UNSPSC Code:
12352200
PubChem Substance ID:
MDL number:
Technischer Dienst
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Unterstützung erhaltenassay
≥98% (HPLC)
form
powder
color
orange
solubility
DMSO: >20 mg/mL
storage temp.
2-8°C
SMILES string
COc1cc2NC(=O)C(=Cc3ccc(O)cc3)c2cc1OC
InChI
1S/C17H15NO4/c1-21-15-8-12-13(7-10-3-5-11(19)6-4-10)17(20)18-14(12)9-16(15)22-2/h3-9,19H,1-2H3,(H,18,20)
InChI key
JGSMCYNBVCGIHC-UHFFFAOYSA-N
Biochem/physiol Actions
RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor.
RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor. Recently it was discover that the compound also inhibits c-Met. Increased tumorigenicity, motility, and invasiveness have been described as biological consequences of HGF/Met deregulation in tumor cells, thus not surprisingly RPI-1 treatment of H460 cells resulted in a strong reduction of both colony number and size (IC50 = 24.5 + 0.5 microM). Compound is also active at mouse NSCLC H460 xenograft tumor and metastasis model. Mechanistically RPI-1 inhibits Met phosphorylation at Tyr1234/Tyr1235, known to activate the intrinsic kinase activity. It appears that " Ret/ptc1 cross talks with Met at transcriptional and signaling levels and promotes ?-catenin transcriptional activity to drive thyrocyte neoplastic transformation". It appears that we do not have anything specific in Ret area. Handbook lists RPI-1 as Ret inhibitor.
Features and Benefits
This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
Lagerklasse
13 - Non Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
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