Pralsetinib (BLU 667)

InvivoChem Cat #:V4830CAS #:2097132-94-8 (free base)Purity >=98%

Description: Pralsetinib (GAVRETO; BLU-667) is a novel, highly potent, selective, FDA approved RET inhibitor with IC50 of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion.. BLU-667 is a potent and selective inhibitor of RET mutations, fusions, and predicted resistant mutants. RET fusions are key drivers of multiple cancers, including lung and thyroid cancer, and our research suggests that RET also plays a key role in some colon and breast cancers. By simultaneously targeting the primary driver and predicted resistant mutants that render cancer cells insensitive to treatment with currently approved drugs. On September 4, 2020, the Food and Drug Administration grantedaccelerated approval to pralsetinib (GAVRETO) for adult patients with metastatic RET fusion-positivenon-small cell lung cancer (NSCLC) as detected by an FDA approved test.

References: American Association for Cancer Research. 10.1158/2159-8290.CD-18-0338.

Related CAS : 2097132-94-8 (free base); 2097132-93-7 (trans-isomer)

-20C for 3 years in powder form

Synonym: BLU-667; BLU 667; BLU667; Gavreto
Chemical Name: 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
InChi Key: MXSCYXULRDBMTH-RWYJCYHVSA-N
InChi Code: InChI=1S/C27H32FN9O2/c1-16-11-23(33-25(32-16)19-7-9-27(39-4, 10-8-19)26(29)38)37(24-12-17(2)34-35-24)18(3)20-5-6-22(30-13-20)36-15-21(28)14-31-36/h5-6, 11-15, 18-19H, 7-10H2, 1-4H3, (H2, 29, 38)(H, 34, 35)/t18-, 19-, 27+/m0/s1
SMILES Code: O=C([C]1(OC)CC[CH](C2=NC(NC3=NNC(C)=C3)=CC(C)=N2)CC1)N[CH](C4=CC=C(N5N=CC(F)=C5)N=C4)C