Description: BGG463 (K 0859) can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 µM, 0.09 µM and 0.590 µM, respectively. Target: CDK, Bcr-Abl. Smiles: CN1CCN(Cc2ccc(NC(=O)c3cccc4cc(Oc5cc(NC(C)=O)ncn5)ccc34)cc2C(F)(F)F)CC1. References: Alexander LT, et al....

BGG463 is a derivative of BBT594, an inhibitor of the fusion protein Bcr-AblT315I.Formal Name: 6-[[6-(acetylamino)-4-pyrimidinyl]oxy]-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-1-naphthalenecarboxamide. CAS Number: 890129-26-7. Synonyms: K03859, NVP-BGG463. Molecular Formula: C30H29F3N6O3....

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...

BGG463 (NVP-BGG463) was generated by a rational 'hybrid design' approach. Like Imatinib, BGG463 disrupts the assembly of the hydrophobic spine, a characteristic feature of the active state of several kinases, thereby locking the kinase in an inactive 'DFG-out' conformation. BGG463 can inhibit c-ABL-T334I, BCR-ABL...