Taselisib has a dual mechanism of action, both blocking kinase signaling and inducing down-regulation of the mutant p110alpha protein level in a dose-dependent and time-dependent manner. The taselisib-induced degradation of mutant p110a protein is ubiquitin-mediated and proteasome-dependent.
| Product Name | Taselisib |
| Synonyms | |
| CAS Number | 1282512-48-4 |
| Related CAS | |
| Molecular Formula | C24H28N8O2 |
| Molecular Weight | 460.542 |
| SMILES | CC(C)N1N=C(C)N=C1C1=CN2CCOC3=CC(=CC=C3C2=N1)C1=CN(N=C1)C(C)(C)C(N)=O |
| Purity (HPLC) | >= 95% |
| Physical Appearance | White solid |
| Solubility | DMSO, DMF |
| Shipping Conditions | Room Temperature |
| Storage Conditions | Refrigerated |
| Shelf Life | 12 months after the date of delivery |
| Regulatory Statement | For Research Use Only |
References
Li, H., Dong, J., Cai, M., Xu, Z., Cheng, X.-D.,Qin, J.-J., Protein degradation technology: a strategic paradigm shift in drug discovery. Journal of Hematology & Oncology 2021, 14, 138.Friedman, L., Edgar, K., Song, K., Schmidt, S., Kirkpatrick, D., Phu, L., Nannini, M., Hong, R., Cheng, E., Crocker, L., Young, A.,Sampath, D., Abstract S6-04: The PI3K inhibitor, taselisib, has enhanced potency in PIK3CA mutant models through a unique mechanism of action. Cancer Research 2017, 77, S6-04-S6-04.
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