Description
FB23-2 is a potent and selective inhibitor of mRNA N6-methyladenosine (m6A) demethylase FTO, with an IC50 of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML).
Product information
CAS Number: 2243736-45-8
Molecular Weight: 392.24
Formula: C18H15Cl2N3O3
Chemical Name: 2-{[2,6-dichloro-4-(3,5-dimethyl-1,2-oxazol-4-yl)phenyl]amino}-N-hydroxybenzamide
Smiles: CC1ON=C(C)C=1C1=CC(Cl)=C(NC2=CC=CC=C2C(=O)NO)C(Cl)=C1
InChiKey: ILHNIWOZZKIBNW-UHFFFAOYSA-N
InChi: InChI=1S/C18H15Cl2N3O3/c1-9-16(10(2)26-23-9)11-7-13(19)17(14(20)8-11)21-15-6-4-3-5-12(15)18(24)22-25/h3-8,21,25H,1-2H3,(H,22,24)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 62.5 mg/mL (159.34 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
FB23-2 dramatically suppresses proliferation and promotes the differentiation/apoptosis of human AML cell line cells and primary blast AML cells. FB23 inhibits the proliferation of NB4 and MONOMAC6 cells, with IC50 values of 0.8 μM and 1.5 μM. FB23-2 (20 μM; 72 hours) displays anti-proliferation effect via upregulating global m6A levels. FB23-2 (0.5-5 μM; 24-72 hours) significantly suppresses the proliferation of BM cells from these two models in a dose-dependent manner. FB23-2 exhibits FTO-dependent anti-proliferation activity and promotes myeloid differentiation and apoptosis. FB23-2 (1-20 μM; 72 hours) significantly increases the mRNA and protein levels of ASB2 and RARA in NB4 and MONOMAC6 cells. FB23-2 induces apoptosis (1-20 μM; 48-72 hours) and cell cycle arrest (5-20 μM; 24 hours) at G1 stage in AML cells.
In Vivo:
FB23-2 (2 mg/kg; i.p.; daily; for 10 days) substantially suppresses leukemia progression and prolongs survival. FB23-2 exhibits elimination half-life (rat 6.7 h) and Cmax (rat 2421.3 ng/mL) following intraperitoneal injection (rat 3 mg/kg).
Products are for research use only. Not for human use.
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