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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.
| Molecular Weight | 297.31 |
| Formula | C17H15NO4 |
| CAS Number | 269730-03-2 |
| Form | Solid |
| Solubility (25°C) | DMSO: ≥20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related RET Products |
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| SPP86
SPP86 is a potent cell permeable inihbitor of RET tyrosine kinase with an IC50 value of 8 nM and with some inhibitory activity at EphA1, FGFR1, Flt4, Lck and Yes. |
| Pralsetinib
Pralsetinib (BLU-667) is a next generation highly potent, selective RET inhibitor with IC50 of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion. |
| Selpercatinib (LOXO-292)
Selpercatinib (LOXO-292) is a first-in-class, highly selective and potent small molecule RET inhibitor with good blood-brain barrier (BBB) penetration. and RET (G810R) with IC50 values of 14.0 nM, 24.1 nM and 530.7 nM, respectively. |
| AD80
AD80 is a multikinase inhibitor, it potently targets human RET, BRAF, S6K, and SRC. |
| AST 487
AST 487 is a RET kinase inhibitor,IC50 880 nM, inhibits RET autophosphorylation, downstream effector activation, and also inhibits Flt-3,IC50 520 nM. |
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