欢迎访问ProbeChem中文网站,英文网站请访问www.probechem.com

首页-抗体药物偶连体和PROTACs-PROTAC-SIAIS562055
SIAIS562055

Chemical Structure : SIAIS562055

CAS No.:

SIAIS562055 (SIAIS 562055)

货号: 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.

规格 价格 库存 数量
25 mg Get quote
50 mg Get quote
100 mg Get quote

大包装,大折扣!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 918.13
分子式 C49H62F3N7O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(4-((12-(4-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)piperidin-1-yl)dodecyl)thio)-1-oxoisoindolin-2-yl)piperidine-2,6-dione

参考文献

1. Luo Z, et al. Cancer Res. 2024 Oct 22. doi: 10.1158/0008-5472.CAN-24-1093.

备案号:沪ICP备16042516号-1 Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

联系我们 sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

询单

  • *产品名称:
  • *姓名:
  • *邮箱:
  • *公司名称:
  • *询单数量:
  • *国籍:
  • 询单信息: