BLU-667 (Pralsetinib) | B2548

BLU-667 (Pralsetinib) is a highly potent and selective, next generation RET inhibitor with IC₅₀ of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion. In vivo, BLU-667 potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR2.

LU-667 (Pralsetinib) is a highly potent and selective, next generation RET inhibitor with IC₅₀ of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion. In vivo, BLU-667 potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR2.

B2548 | BLU-667 (Pralsetinib) DataSheet

Alternate Name/Synonyms: Pralsetinib free base; cis-N-{(1S)-1-[6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethyl}-1-methoxy-4-{4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl}cyclohexane-1-carboxamide; BLU 667; BLU667

Appearance: Crystalline solid

Formulation:

CAS Number: 2097132-94-8

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₇H₃₂FN₉O₂

Molecular Weight: 533.6

Cell-Permeable?: True

Purity: ≥98% by HPLC

Solubilities: >50 mg/ml in DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A highly potent, selective, next generation RET inhibitor

MDL Number:

PubChem CID: 129073603

SMILES: CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)NC(C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC

InChi: InChI=1S/C27H32FN9O2/c1-16-11-22(33-23-12-17(2)35-36-23)34-25(31-16)19-7-9-27(39-4,10-8-19)26(38)32-18(3)20-5-6-24(29-13-20)37-15-21(28)14-30-37/h5-6,11-15,18-19H,7-10H2,1-4H3,(H,32,38)(H2,31,33,34,35,36)/t18-,19?,27?/m0/s1

InChi Key: GBLBJPZSROAGMF-SIYOEGHHSA-N