BBT594 is an inhibitor of Bcr-AblT315I (IC50 = 44 nM), a form of the Bcr-Abl fusion protein containing a tyrosine-to-isoleucine substitution at position 315. It decreases proliferation in mouse Ba/F3 hematopoietic cells expressing Bcr-AblT315I (GI50 = 117 nM). BBT594 (1 or 5 µM) also inhibits phosphorylation of Jak2...

Description: BBT594 (NVP-BBT594)(NVP-BBT594) is a potent inhibitor of receptor tyrosine kinase RET,Treatment of cancer. Target: c-RET. Smiles: CN1CCN(Cc2ccc(NC(=O)N3CCc4cc(Oc5cc(NC(C)=O)ncn5)ccc34)cc2C(F)(F)F)CC1. References: Zhang Q , Shi C , Han L , et al. Inhibition of mTORC1/C2 signaling improves anti-leukemia...

CFI-400437 is a potent PLK4 inhibitor (IC50=0.6nM) and selective against other members of the PLK family (>10µM). Against a broad panel of kinases, only a small subset is significantly inhibited. CFI-400437 is a potent inhibitor of MCF-7, MDA-MB-468 and MDA-MB-231 cell growth and very effective in a mouse xenograft...

BBT594 (NVP-BBT594) is a potent and selective inhibitor of RET and JAK2. BBT594 impairs "glial-derived neurotrophic factor" (GDNF)-RET signaling and GDNF-dependent growth in specific in vitro models. Direct inhibition of GDNF-RET signaling by BBT594 in ER+ breast cancer cells enhances the sensitivity to aromatase...