TO-1187 (TFA)

TO-1187 TFA is a selective HDAC6 PROTAC degrader (DC50: 5.81 nM) . TO-1187 TFA promotes the ubiquitination and degradation of HDAC6 and can be used in the study of hematological malignancies and solid tumors (Pink: HDAC6 ligand (HY-173386) ; Blue: CRBN ligase ligand (HY-41547) ; Black: linker (HY-140212) ) [1].

Product Specifications

UNSPSC

12352005

Target

HDAC; PROTACs

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; PROTAC

Field of Research

Cancer; Neurological Disease

Purity

98.41

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C=C1)CN(CC2=CN=CC=C2)CC3=CN(N=N3)CCOCCNC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)NO.OC(C(F)(F)F)=O

Molecular Formula

C36H36F3N9O9

Molecular Weight

795.72

References & Citations

[1]Kollmannsberger C, et al. A Randomized Phase II Study of AGS-16C3F Versus Axitinib in Previously Treated Patients with Metastatic Renal Cell Carcinoma. Oncologist. 2021 Mar;26 (3) :182-e361.