FHD-286

Product Name: FHD-286
CAS No.: 2671128-05-3
Chemical Name: FHD-286
Synonyms: FHD-286;FHD-286 ，E1178;FHD-286, 10 mM in DMSO;Inhibitor,inhibit,FHD 286,FHD-286,Epigenetic Reader Domain,FHD286;N-[(S)-1-[[4-[6-[(2R,6S)-2,6-Dimethylmorpholino]-2-pyridyl]-2-thiazolyl]amino]-3-methoxy-1-oxo-2-propyl]-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide;N-[(1S)-2-[[4-[6-[cis-2,6-dimethylmorpholin-4-yl]-2-pyridyl]thiazol-2-yl]amino]-1-(methoxymethyl)-2-oxo-ethyl]-1-methylsulfonyl-pyrrole-3-carboxamide;N-[(2S)-1-[[4-[6-[(2S,6R)-2,6-dimethyl-4-morpholinyl]-2-pyridinyl]-2-thiazolyl]amino]-3-methoxy-1-oxopropan-2-yl]-1-methylsulfonyl-3-pyrrolecarboxamide;N-((S)-1-((4-(6-((2R,6S)-2,6-Dimethylmorpholino)pyridin-2-yl)thiazol-2-yl)amino)-3-methoxy-1-oxopropan-2-yl)-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide;1H-Pyrrole-3-carboxamide, N-[(1S)-2-[[4-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-2-pyridinyl]-2-thiazolyl]amino]-1-(methoxymethyl)-2-oxoethyl]-1-(methylsulfonyl)-
CBNumber: CB410298404
Molecular Formula: C24H30N6O6S2
Formula Weight: 562.66
MOL File: 2671128-05-3.mol

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FHD-286 Property

Density: 1.46±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : 250 mg/mL (444.32 mM; Need ultrasonic)
form: Solid
pka: 7.18±0.50(Predicted)
color: Off-white to light yellow
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

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Hazard and Precautionary Statements (GHS)

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FHD-286 Chemical Properties,Usage,Production

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.

Uses

FHD-286 is a selective, oral inhibitor of SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor. FHD-286 has the potential for the research of BAF (BRG1/BRM-associated factor)-related disorders such as acute myeloid leukemia[1].

in vivo

FHD-286 (1.5 mg/kg; oral administration; for 10 days) increases in IFNγ and Th1-type chemokine CXCL10 levels^[2].

Animal Model:	B16F10 tumor-bearing mice^[2]
Dosage:	1.5 mg/kg
Administration:	Oral administration; for 10 days
Result:	Increased in IFNγ and Th1-type chemokine CXCL10 levels.

References

[1] Warren C. Fiskus, et al. Abstract 1140: Pre-clinical efficacy of targeting BAF complexes through inhibition of the dual ATPases BRG1 and BRM by FHD-286 in cellular models of AML. Cancer Res (2023) 83 (7_Supplement): 1140.
[2] Kana Ichikawa, et al. Synergistic efficacy of the BRM/BRG1 ATPase inhibitor, FHD-286, and anti-PD-1 antibody in mouse syngeneic tumor models.

FHD-286 Preparation Products And Raw materials

Raw materials

Preparation Products

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FHD-286 Suppliers

China 56 United States 4 Global 60

Shanghai XingMo Biotechnology Co., Ltd.

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Shanghai Chaolan Chemical Technology Center

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2671128-05-3, FHD-286Related Search:

1H-Pyrrole-3-carboxamide, N-[(1S)-2-[[4-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-2-pyridinyl]-2-thiazolyl]amino]-1-(methoxymethyl)-2-oxoethyl]-1-(methylsulfonyl)-

FHD-286

Inhibitor,inhibit,FHD 286,FHD-286,Epigenetic Reader Domain,FHD286

N-[(1S)-2-[[4-[6-[cis-2,6-dimethylmorpholin-4-yl]-2-pyridyl]thiazol-2-yl]amino]-1-(methoxymethyl)-2-oxo-ethyl]-1-methylsulfonyl-pyrrole-3-carboxamide

N-[(S)-1-[[4-[6-[(2R,6S)-2,6-Dimethylmorpholino]-2-pyridyl]-2-thiazolyl]amino]-3-methoxy-1-oxo-2-propyl]-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide

N-[(2S)-1-[[4-[6-[(2S,6R)-2,6-dimethyl-4-morpholinyl]-2-pyridinyl]-2-thiazolyl]amino]-3-methoxy-1-oxopropan-2-yl]-1-methylsulfonyl-3-pyrrolecarboxamide

N-((S)-1-((4-(6-((2R,6S)-2,6-Dimethylmorpholino)pyridin-2-yl)thiazol-2-yl)amino)-3-methoxy-1-oxopropan-2-yl)-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide

FHD-286, 10 mM in DMSO

FHD-286 ，E1178

2671128-05-3

671128-05-3

C24H30N6O6S2