FHD-286 Chemical Properties

Density 

1.46±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 250 mg/mL (444.32 mM; Need ultrasonic)

pka

7.18±0.50(Predicted)

form 

Solid

color 

Off-white to light yellow

InChI

InChI=1S/C24H30N6O6S2/c1-15-10-29(11-16(2)36-15)21-7-5-6-18(25-21)20-14-37-24(27-20)28-23(32)19(13-35-3)26-22(31)17-8-9-30(12-17)38(4,33)34/h5-9,12,14-16,19H,10-11,13H2,1-4H3,(H,26,31)(H,27,28,32)/t15-,16+,19-/m0/s1

InChIKey

JBLQNFBXKOAIHG-FCEWJHQRSA-N

SMILES

N1(S(C)(=O)=O)C=CC(C(N[C@@H](COC)C(NC2=NC(C3=NC(N4C[C@H](C)O[C@H](C)C4)=CC=C3)=CS2)=O)=O)=C1

FHD-286 Usage And Synthesis

Description

FHD-286 is a highly potent, selective, allosteric and orally available, small-molecule, enzymatic inhibitor of BRG1 (SMARCA4) and BRM (SMARCA2), two highly similar proteins that are the ATPases, or the catalytic engines of the BAF complex, one of the critical regulators within the chromatin regulatory system. In preclinical studies, FHD-286 has shown anti-tumour activity across a broad range of malignancies, including hematologic and solid tumours. FHD-286 is being developed for relapsed and/or refractory AML.