Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : SIAIS562055
Catalog No.: PC-23302Not For Human Use, Lab Use Only.
SIAIS562055 is a potent, selective SOS1 PROTAC degrader (KD=95.9 nM) which is designed by connecting a CRBN ligand to an analogue of the SOS1 inhibitor BI-3406, selectively degrades SOS1 with DC50 values of 62.5 nM and 8.4 nM in K562 and KU812 cells.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
SIAIS562055 is a potent, selective SOS1 PROTAC degrader (KD=95.9 nM) which is designed by connecting a CRBN ligand to an analogue of the SOS1 inhibitor BI-3406, selectively degrades SOS1 with DC50 values of 62.5 nM and 8.4 nM in K562 and KU812 cells.
SIAIS562055 effectively blocks the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively.
SIAIS562055 does not affect GSPT1 and IKZF1/3 protein level in MIA PaCa-2 cells.
SIAIS562055 inhibits ERK phosphorylation, suppresses the proliferation of BCR-ABL+ CML cells, inhibits the proliferation of K562 and KU812 cells, with IC50 values of 201.1 nM and 45.6 nM, respectively.
SIAIS562055 enhances the sensitivity of CML cell to BCR-ABL inhibitors by SLC22A4-mediated cellular uptake transport.
Combination of SIAIS562055 and imatinib exerts synergistic antitumor efficacy in mouse model and primary CML patient samples.
| M.Wt | 918.13 | |
| Formula | C49H62F3N7O5S | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
1. Luo Z, et al. Cancer Res. 2024 Oct 22. doi: 10.1158/0008-5472.CAN-24-1093.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
