R8907

RPI-1

≥98% (HPLC)

• Synonym(s): 1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-H-indol-2-one
• Empirical Formula (Hill Notation): C₁₇H₁₅NO₄
• CAS Number: 269730-03-2
• Molecular Weight: 297.31
• UNSPSC Code: 12352200
• PubChem Substance ID: 329824042
• MDL number: MFCD03852474

Properties

• assay: ≥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

Description

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

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Safety Information

• Storage Class: 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