2703834-25-5
Chemical Structure
PROTAC BCR-ABL Degrader-2
- CAS No.: 2703834-25-5
- Formula:C48H46F3N9O6
- Molecular Weight:901.93
InChIKey: HNQVKMYCDZGKOD-UHFFFAOYSA-N
SMILES: O=C(C1=CC=C(C)C(C#CC2=CC3=C(NN=C3)N=C2)=C1)NC4=CC=C(CN5CCN(CCCCCCC(NC6=CC=CC(C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O)=O)CC5)C(C(F)(F)F)=C4
Biological Activity: PROTAC BCR-ABL Degrader-2 is a selective Bcr-AblT315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research[1][2].
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PROTAC BCR-ABL Degrader-2 | PROTAC BCR-ABL Degrader-2 is a selective Bcr-AblT315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research. | |||||||||||||||||||||
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References
- [1]. Jiang L, et al. Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation. Acta Pharm Sin B. 2021 May;11(5):1315-1328. [Content Brief]
- [2]. Chen X, et al. Mighty mini-PROTACs: an emerging class of degraders. Eur J Med Chem. 2026 Jan 5;301:118202. [Content Brief]
