PROTAC STAT3 degrader-2 

PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC₅₀ of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research^[1]. PROTAC STAT3 degrader-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

PROTAC STAT3 degrader-2 (compound 27; 4 days) has cell growth-inhibitory activities in the Molm-16 with an IC₅₀ of 0.582 μM and has no effect on SU-DHL-1 cell lines with an IC₅₀ of >10 μM, respectively^[1].
PROTAC STAT3 degrader-2 is ineffective in reducing the levels of STAT3 and pSTATSY705 proteins in SU-DHL-1 cells up to 5 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1172.13

C₅₉H₆₀F₂N₉O₁₃P

2429877-78-9

Solid

White to off-white

O=C1C2=C(C#CCCCCCC(N3C[C@@H](C(N4[C@@](CC[C@H]4C(N[C@@H](CCC(N)=O)C(NC(C5=CC=CC=C5)C6=CC=CC=C6)=O)=O)([H])CC3)=O)NC(C7=CC8=CC(C(F)(F)P(O)(O)=O)=CC=C8N7)=O)=O)C=CC=C2C(N1C9C(NC(CC9)=O)=O)=O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Haibin Zhou, et al. Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein. J Med Chem. 2019 Dec 26;62(24):11280-11300.  [Content Brief]