SD-36

• Description:

  SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM) . SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase[1]. SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

• UNSPSC:

  12352005

• Hazard Statement:

  H315-H319-H320

• Target:

  Apoptosis; PROTACs; STAT

• Type:

  Reference compound

• Related Pathways:

  Apoptosis; JAK/STAT Signaling; PROTAC; Stem Cell/Wnt

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/sd-36.html

• Purity:

  99.73

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C([C@@H](NC([C@@H]1CC[C@H](CCN(C(CCCCCC#CC2=CC=CC3=C2CN(C4CCC(NC4=O)=O)C3=O)=O)C[C@@H]5NC(C6=CC(C=C(C(F)(P(O)(O)=O)F)C=C7)=C7N6)=O)N1C5=O)=O)CCC(N)=O)NC(C8=CC=CC=C8)C9=CC=CC=C9

• Molecular Formula:

  C59H62F2N9O12P

• Molecular Weight:

  1158.15

• Precautions:

  P264-P280-P302+P352-P305+P351+P338-P362

• References & Citations:

  [1]Bai L, et al. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo. Cancer Cell. 2019 Nov 11;36 (5) :498-511.e17.

• Shipping Conditions:

  Dry Ice

• Storage Conditions:

  -80°C, stored under nitrogen

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  Cereblon; STAT3

• CAS Number:

  [2429877-44-9]