| Hazard Information | Back Directory | [Description]
DAS-IAP is a novel PROTAC targeting drug-resistant BCR-ABL. | [Uses]
SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively[1]. | [IC 50]
Abl: 0.54 nM (IC50); cIAP1: 10 nM (IC50); cIAP2: 12 nM (IC50); XIAP: 50 nM (IC50); SNIPER; Abl: 10 nM (DC50) | [References]
[1] Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666. DOI:10.1111/cas.13284 |
|
|