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Documentos Principais

SML2926

Sigma-Aldrich

FT895

≥98% (HPLC)

Sinônimo(s):

2,3-Dihydro-N-hydroxy-1,1-dimethyl-2-[5-(trifluoromethyl)-2-pyrazinyl]-1H-isoindole-4-carboxamide, FT 895, FT-895, HDTK 070, HDTK-070, HDTK070, N-Hydroxy-1,1-dimethyl-2-(5-(trifluoromethyl)pyrazin-2-yl)isoindoline-4-carboxamide

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About This Item

Fórmula empírica (Notação de Hill):
C16H15F3N4O2
Número CAS:
Peso molecular:
352.31
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

Ensaio

≥98% (HPLC)

Formulário

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

FC(F)(F)c1ncc(nc1)N2C(c3c(c(ccc3)C(=O)NO)C2)(C)C

chave InChI

XCLPBILTRRWOIL-UHFFFAOYSA-N

Ações bioquímicas/fisiológicas

FT895 is a potent and highly selective HDAC11 inhibitor (IC50 = 3 nM/HDAC11, 5.6 μM/HDAC8, >10 μM/HDAC1-7, HDAC9 & HDAC10) with a deacetylase active site Zn2+-targeting hydroxamate. FT895 exhibits antiproliferation potency against myeloproliferative neoplasm (MPN) cultures (IC50 = 3.00 μM/JAK2(V617F) Ba/F3, 4.94 μM/HEL92.1.7, 6.49 μM/MPL(W515L) Ba/F3) and reduces stem-like properties of CSCs (42/62/85/100% inhibtion of H1650 Sphere formation at 0.5/1/2/5 μM).
Potent and highly selective HDAC11 inhibitor that reduces myeloproliferative neoplasm (MPN) proliferation and CSCs stem-like properties.

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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Se In Son et al.
ACS chemical biology, 14(7), 1393-1397 (2019-07-03)
Mammalian histone deacetylases (HDACs) are a class of enzymes that play important roles in biological pathways. Existing HDAC inhibitors target multiple HDACs without much selectivity. Inhibitors that target one particular HDAC will be useful for investigating the biological functions of
Matthew W Martin et al.
Bioorganic & medicinal chemistry letters, 28(12), 2143-2147 (2018-05-20)
N-Hydroxy-2-arylisoindoline-4-carboxamides are potent and selective inhibitors of HDAC11. The discovery, synthesis, and structure activity relationships of this novel series of inhibitors are reported. An advanced analog (FT895) displays promising cellular activity and pharmacokinetic properties that make it a useful tool
Lanzhu Yue et al.
Blood, 135(3), 191-207 (2019-11-22)
Protein acetylation is an important contributor to cancer initiation. Histone deacetylase 6 (HDAC6) controls JAK2 translation and protein stability and has been implicated in JAK2-driven diseases best exemplified by myeloproliferative neoplasms (MPNs). By using novel classes of highly selective HDAC
Namrata Bora-Singhal et al.
Scientific reports, 10(1), 4722-4722 (2020-03-15)
Non-small cell lung cancer (NSCLC) is known to have poor patient outcomes due to development of resistance to chemotherapy agents and the EGFR inhibitors, which results in recurrence of highly aggressive lung tumors. Even with recent success in immunotherapy using

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