FB23-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FB23-2 是 mRNA N 6-甲基腺苷 (m 6A) 脱甲基酶 FTO 的有效选择性抑制剂。

FB23-2 is a potent, selective inhibitor of the mRNA N 6-methyladenosine (m 6A) demethylase FTO, directly bind to FTO, inhibits FTO demethylation of m6 A in RNA in vitro with IC50 of 2.6 uM; demonstrates significantly improved anti-proliferative activity on NB4 and MONOMAC6 cells with IC50 of 0.8-1.5 uM, compared with parental compound FB23; dramatically suppresses proliferation and promotes the differentiation/apoptosis of human acute myeloid leukemia (AML) cell line cells and primary blast AML cells in vitro; FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice.

Cell Proliferation Assay Cell Line:MA9 cells, FLT3ITD/NPM1 cells (mouse BM cells)Concentration:0.5 μM, 2 μM, 5 μMIncubation Time:24 hours, 48 hours, 72 hours Result:Suppressed the proliferation of BM cells.RT-PCRCell Line:NB4 cells, MONOMAC6 cells Concentration:1 μM, 5 μM , 20 μM Incubation Time:72 hours Result:Significantly increased ASB2 and RARA mRNA levels.Apoptosis Analysis Cell Line:NB4 cells, MONOMAC6 cells Concentration:1 μM, 5 μM , 20 μM Incubation Time:48 hours (NB4 cells),72 hours (MONOMAC6 cells)Result:Induced apoptosis.Cell Cycle Analysis Cell Line:MONOMAC6 cells Concentration:5 μM , 20 μM Incubation Time:24 hours Result:Induced cell cycle arrest at G1 stage.

Animal Model:NOD/LtSz-scid IL2RG-SGM3 (NSGS) mice, xeno-transplanted with MONOMAC6 AML cells Dosage:2 mg/kg Administration:Intraperitoneal injection, daily, for 10 days Result:Delayed the onset of full-blown leukemic symptoms and significantly prolonged survival by almost doubling the median survival.Animal Model:Sprague Dawley (SD) rats Dosage:3 mg/kg (Pharmacokinetic Analysis)Administration:Intraperitoneal injection Result:T1/2 (6.7 hours), Cmax (2421.3 ng/mL).

FTO Demethylase inhibitor FB23-2

Chromatin/Epigenetic

Histone Demethylase

Histone Demethylase

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2243736-45-8

392.236

C18H15Cl2N3O3

>98% (HPLC)

DMSO : 62.5 mg/mL 159.34 mM

O=C(NO)C1=CC=CC=C1NC2=C(Cl)C=C(C3=C(C)ON=C3C)C=C2Cl

2-((2,6-dichloro-4-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-N-hydroxybenzamide

(-20℃)

With Ice Pack

≥ 2 years