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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. Pralsetinib (Blu-667) potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2). Pralsetinib (Blu-667) shows dose dependent activity against both KIF5B-RET Ba/F3 and KIF5B-RET V804L Ba/F3 allograft tumors with doses as low as 10 mg/kg twice-daily.
| Molecular Weight | 533.6 |
| Formula | C27H32FN9O2 |
| CAS Number | 2097132-94-8 |
| Solubility (25°C) | DMSO ≥ 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Subbiah V, et al. Cancer Discov. Precision Targeted Therapy with BLU-667 for RET-Driven Cancers.
| Related RET Products |
|---|
| RPI-1
RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor. |
| 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. |
| 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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