SYHA1815 (SYHA-1815) is a novel potent, selective RET inhibitor, inhibits the kinase activity of RET wild type (IC50=0.9 nM) and V804 mutant (IC50=3.1 nM).SYHA1815 demonstrated approximately 20-fold selectivity for RET over KDR, exhibited a favorable selectivity profile, with> 100-fold selectivity over 347 kinases, and >10-fold selectivity over 44 other kinases in a panel of 395 kinases.SYHA1815 significantly inhibited RET phosphorylation and activation of its key adaptor protein SHC and the downstream signaling molecules p-AKT and p-ERK1/2 in classical RET mutant-driven MTC cell line TT (RETC634W), effectively inhibited p-RET, p-SHC, and downstream p-AKT and p-ERK activity.SYHA1815 inhibited RET-induced cell proliferation and overcame V804 mutants (TT cell proliferation IC50<1.6 nM), suppressed RET-driven cell proliferation via cell-cycle arrest through c-Myc downregulation.SYHA1815 showed potent antitumor efficacy against RET- and RET gatekeeper mutant-driven cancers in vivo.

Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.